Abstract
Extracellular signals, including neurotransmitters, hormones, cytokines, and growth factors, produce many of their physiological effects by regulating the state of phosphorylation of specific proteins in target cells (Walaas and Greengard, 1991). Inhibitors of protein kinases and protein phosphatases are useful tools in evaluating the physiological roles of protein phosphorylation signaling mechanisms, and may ultimately find therapeutic applications. Available inhibitors include natural and synthetic compounds, peptides, and proteins (MacKintosh and MacKintosh, 1994). Natural inhibitors include endogenous protein inhibitors of protein kinases (e.g., the protein kinase inhibitor [PKI] of cyclic AMP [cAMP]-dependent protein kinase [PKA]) and protein phosphatases (e.g., inhibitor-1, inhibitor-2, and DARPP-32), as well as toxins produced by bacteria, fungi, plants, dinoflagellates, and insects. Synthetic inhibitors include peptide analogs derived from intramolecular pseudosubstrate inhibitory domains of protein kinases and phosphatases, derivatives of natural toxins, and analogs and inhibitors of endogenous activators (e.g., cAMP analogs) or substrates (e.g., ATP analogs). This chapter will review the most widely available inhibitors with demonstrated utility, including their basic properties and applications relevant to their use in neuroscience research.
This is a preview of subscription content, log in via an institution to check access.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
References
Abdul-Ghani, M., Kravitz, E A., Meiri, H, and Rahamimoff, R (1991) Protein phosphatase inhibitor okadaic acid enhances transmitter release at neuromuscular junctions. Proc Natl. Acad. Sci USA 88, 1803–1807.
Abe, K., and Saito, H (1993) Tyrosine kinase inhibitors, herbimycin A and lavendustin A, block formation of long-term potentiation in the dentate gyrus in vivo. Brain Res. 621, 167–170
Abrahams, T. P. and Schofield, G. G (1992) Norepinephrine-induced Ca2+current inhibition in adult rat sympathetic neurons does not require protein kinase activation. Eur J Pharmacol 227, 189–197
Adams, W. B. and Levitan, I. B. (1982) Intracellular injection of protein kinase inhibitor blocks the serotonin-induced increase in K+ conductance in Aplysia neuron R15. Proc Natl. Acad Sci USA 79, 3877–3880.
Aflalo, E., Iftach, S., Segal, S., Gazit, A., and Priel E (1994) Inhibition of topoisomerase I activity by tyrphostin derivatives, protein tyrosine kinase blockers: mechanism of action. Cancer Res. 54, 5138–5142.
Agbotounou, W K., Umezawa, K., Jacquemin-Sablon, A, and Pierre, J. (1994) Inhibition by two lavendustins of the tyrosine kinase activity of pp60F527 in vitro and in intact cells Eur J Pharmacol 269, 1–8
Aitken, A. and Cohen, P. (1982) Isolation and characterisation of active fragments of protein phosphatase inhibitor-1 from rabbit skeletal muscle. FEBS Lett 147, 54–58
Akasu, T., Ito, M., Nakano, T., Schneider, C.R, Simmons, M. A., Tanaka, T., Tokimasa, T., and Yoshida, M (1993) Myosin light chain kinase occurs in bullfrog sympathetic neurons and may modulate voltage-dependent potassium currents. Neuron 11, 1133–1145.
Akiyama, T., and Ogawara, H. (1991) Use and specificity of genistein as inhibitor of protein-tyrosine kinases. Methods Enzymol 201, 362–370.
Akiyama, T., Ishida, J., Nakagawa, S., Ogawara, H., Watanabe, S.-I., Itoh, N., Shibuya, M., and Fukami, Y (1987) Genistein, a specific inhibitor of tyrosine-specific protein kinases. J Biol. Chem. 262, 5592–5595.
Alessi, D. R, Cuenda, A., Cohen, P., Dudley, D. T, and Saltiel, A. R (1995) PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase in vitro and in vivo. J Biol.. Chem 270, 27,489–27,494.
Aloyo, V. J. (1995) Modulation of mu opioid binding by protein kinase inhibitors. Biochem Pharmacol. 49, 17–21
Anderson, M. E., Braun, A. P., Schulman, H., and Premack, B. A. (1994) Multifunctional Ca2+/calmoduhn-dependent protein kinase mediates Ca2+-induced enhancement of the L-type Ca2+ current in rabbit ventricular myocytes. Circ Res 75, 854–861
Antoni, F. A., Shipston, M. J., and Smith, S. M (1993) Inhibitory role for calcineurin in stimulus-secretion coupling revealed by FK506 and cyclosporin A in pituitary corticotrope tumor cells. Biochem. Biophys. Res. Commun 194, 226–233.
Aoyagi, A., Nishikawa, K., Saito, H., and Abe, K. (1994) Characteri-zation of basic fibroblast growth factor-mediated acceleration of axonal branching in cultured rat hippocampal neurons. Brain Res 661, 117–126.
Aperia, A., Fryckstedt, J., Svensson, L., Hemmmgs, H. C, Jr., Nairn, A. C, and Greengard, P. (1991) Phosphorylated Mr 32,000 dopamineand cAMP-regulated phosphoprotein inhibits Na+,K+-ATPase activity in renal tubule cells. Proc Natl Acad Sci USA 88, 2798–2801
Aperia, A., Ibarra, F., Svensson, L.-B, Klee, C, and Greengard, P (1992) Calcineurin mediates α-adrenergic stimulation of Na+,K+-ATPase activity in renal tubule cells. Proc. Natl. Acad Sci USA 89, 7394–7397.
Aprelikova, O., Xiong, Y., and Liu, E. T. (1995) Both pl6 and p21 fami-lies of cyclin-dependent kinase (CDK) inhibitors block the phosphorylation of cyclin-dependent kinases by the CDK-activating kinase. J Biol Chem. 270, 18,195–18,197.
Armstrong, D. L. (1995) Environmental toxins reveal ion channel regu-lation by protein phosphatases. Neuroprotocols 6, 62–71.
Balbi, D. and Allen, J. M. (1994) Role of protein kinase in mediating NGF effect on neuropeptide Y expression in PC12 cells. Mol Brain Res. 23, 310–316.
Baorto, D. M., Mellado, W., and Shelanski, M. L. (1992) Astrocyte process growth induction by actin breakdown. J Cell Biol. 117, 357–367
Bare, D. J., Ghetti, B., and Richter, J. A. (1995) The tyrosme kinase inhib-itor genistein increases endogenous dopamine release from normal and weaver mutant mouse striatal slices. J. Neurochem 65, 2096–2104.
Barret, J. M., Ernould, A. P., Ferry, G., Genton, A, and Boutin, J A. (1993) Integrated system for the screening of the specificity of protein ki-nase inhibitors. Biochem Pharmacol. 46, 439–448.
Bartschat, D. K. and Rhodes, T. E. (1995) Protein kinase modulates calcium channels in isolated presynaptic nerve terminals of rat hip-pocampus. J. Neurochem 64, 2064–2072.
Basudev, H., Jones, P. M., and Howell, S. L. (1995) Protein phosphoryla-tion in the regulation of insulin secretion: the use of site-directed inhibitory peptides in electrically permeabilised islets of Langerhans. Acta Diabetol. 32, 32–37.
Berg, M. M., Sternberg, D. W., Parada, L. F., and Chao, M. V. (1992) K-252a inhibits nerve growth factor-induced trk proto-oncogene tyrosine phosphorylation and kinase activity. J. Biol Chem. 267, 13–16.
Bishop, W. R., Petrin, J., Wang, L., Ramesh, U., and Doll, R. J. (1990) Inhibition of protein kinase by the tyrosine kinase inhibitor erbstatin. Biochem Pharmacol. 40, 2129–2135.
Bixby, J. L. and Jhabvala, P. (1992) Inhibition of tyrosine phosphoryla-tion potentiates substrate-induced neurite growth. J Neurobiol. 23, 468–480.
Botelho, L. H. P., Rothermel, J. D., Coombs, R V., and Jastorff, B. (1988) cAMP analog antagonists of cAMP action. Methods Enzymol 159, 159–172
Bowlby, M. R. and Levitan I B. (1995) Block of cloned voltage-gated potassium channels by the second messenger diacylglycerol independent of protein kinase J Neurophysiol. 73, 2221–2229.
Braun, A. P. and Schulman, H. (1995) The multifunctional calcium/calm-odulin-dependent protein kinase. from form to function. Ann Rev. Physiol 57, 417–445.
Brown, N A., and Seabrook, G. R. (1995) Phosphorylation-and voltage-dependent inhibition of neuronal calcium currents by activation of human D2(short) dopamine receptors Br J. Pharmacol. 115, 459–466.
Bruns, R. F., Miller, F. D., Merriman, R. L., Howbert, J. J., Heath, W. F., Kobayashi, E., Takahashi, I., Tamaoki, T., and Nakano, H (1991) Inhibition of protein kinase by calphostin is light-dependent. Biochem Btophys. Res. Commun 176, 288–293.
Buchdunger, E., Zimmerman, J., Mett, H., Meyer, T., Muller, M, Regenass, U., and Lydon, N. B. (1995) Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class. Proc Natl. Acad. Sci USA 92, 2558–2562.
Buchler, W., Walter, U., Jastoroff, B., and Lohmann, S. M. (1988) Catalytic subunit of cAMP-dependent protein kinase is essential for cAMP-mediated mammalian gene expression. FEBS Lett 228, 27–32.
Budworth, J. and Gescher, A. (1995) Differential inhibition of cytosolic and membrane-derived protein kinase activity by staurosporine and other kinase inhibitors. FEBS Lett. 362, 139–142.
Butt, E., Bemmelen, M., Fischer, L., Walter, U., and Jastorff, B. (1990) Inhibition of cGMP-dependent protein kinase by (Rp)-guanosine 3′,5′-monophosphorothioates. FEBS Lett 263, 47–50.
Butt, E., Eigenthaler, M., and Genieser, H.-G. (1994) (Rp)-8-pCPT-cGMPS, a novel cGMP-dependent protein kinase inhibitor. Eur J. Pharmacol. 269, 265–268.
Butt, E., Pöhler, D., Genieser, H.-G., Huggins, J. P., and Bucher, B. (1995) Inhibition of cyclic GMP-dependent protein kinase-mediated effects by (Rp)-8-bromo-PET-cyclic GMPS. Br J. Pharmacol. 116, 3110–3116.
Cabell, L. and Audesirk, G. (1993) Effects of selective inhibition of protein kinase C, cyclic AMP-dependent protein kinase, and Ca2+-calmodulin-dependent protein kinase on neurite development in cultured rat hippocampal neurons. Int. J. Dev. Neurosa 11, 357–368.
Calabresi, P., Pisani, A., Mercuri, N. B., and Bernardi, G. (1994) Post-receptor mechanism underlying striatal long-term depression. J Neurosci. 14, 4871–4881.
Campenot, R. B., Draker, D. D., and Senger, D. L. (1994) Evidence that protein kinase activates in regulating neurite growth are localized to distal neurites. J Neurochem. 63, 868–878.
Castellucci, V. F., Nairn, A., Greengard, P., Schwartz, J. H., and Kandel, E. R. (1982) Inhibitor of adenosine 3′:5′-monophosphate-dependent protein kinase blocks presynaptic facilitation in Aplysia. J Neurosa 2, 1673–1681.
Cataldi, M, Taglialatela, M, Guerriero, S., Amoroso, S., Lombardi, G., Di Renzo, G., and Annunziato, L. (1996) Protein-tyrosine kinases activate while protem-tyrosine phosphatases inhibit L-type calcium channel activity in pituitary GH3 cells. J Biol Chem. 271, 9441–9446.
Catarsi, S., Ching, S., Merz, D. C., and Drapeau, P. (1995) Tyrosine 1 phosphorylation during synapse formation between identified leech neurons. J Physiol. 485, 775–786.
Chang, H. Y, Takei, K., Sydor, A. M., Born, T., Rusnak, F., and Jay, D. G (1995) Asymmetric retraction of growth cone filopodia following focal inactivation of calcmeurin. Nature 376, 686–690.
Chen, G.-G., Chalazonitis, A, Shen, K.-F., and Crain, S. M. (1988) Inhib-itor of cyclic AMP-dependent protein kinase blocks opioid-induced prolongation of the action potential of mouse sensory ganglion neurons in dissociated cell cultures. Brain Res. 462, 372–377.
Chijiwa, T., Mishima, A., Hagiwara, M., Sano, M., and Hayashi, T. (1990) Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized inhibitor of cyclic AMP-dependent protein kinase, N-(2-[p-bromocinnamyl-amino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. J Biol. Chem 265, 5267–5272.
Chiou, J.-Y. and Westhead, E. W. (1992) Okadaic acid, a protein phos-phatase inhibitor, inhibits nerve growth factor-directed neurite outgrowth in PC12 cells. J Neurochem. 59, 1963–1966.
Cobb, M. H. and Goldsmith, E. J. (1995) How MAP kinases are regu-lated. J. Biol. Chem. 270, 14,843–14,846.
Coffey, E. T., Sihra, T. S., and Nicholls, D. G. (1993) Protein kinase and the regulation of glutamate exocytosis from cerebrocortical synaptosomes. J. Biol. Chem. 268, 21,060–21,065.
Cohen, P. (1991) Classification of protein-serine/threonine phosphatases: identification and quantitation in cell extracts. Methods Enzymol 201, 389–398.
Cohen, P., Klumpp, S., and Schelling, D. L. (1989) An improved proce-dure for identifying and quantitating protein phosphatases in mammalian tissues. FEBS Lett 250, 596–600.
Cohen, P., Foulkes, J, G., Holmes, C. F., Nimmo, G. A., and Tonks, N. K (1990) Protein phosphatase inhibitor-1 and inhibitor-2 from rabbit skeletal muscle. Methods Enzymol. 159, 427–437.
Colbran, R. J., Smith, M. K, Fong, Y. L., Schworer, C. M., and Soderling, T R. (1989) Regulatory domain of calcium/calmodulin-dependent protein kinase II. Mechanism of inhibition and regulation by phosphorylation J Biol. Chem 264, 4800–4804
Conrad, R., Keranen, L. M., Ellington, A. D., and Newton, A.C., (1994) Isozyme-specific inhibition of protein kinase by RNA aptamers J. Biol Chem. 269, 32,051–32,054
Conroy, L. A., Merritt, J. E., and Hallam, T. J. (1994) Regulation of T-cell-receptor-stimulated bivalent-cation entry in Jurkat E6 cells: role of protein kinase Biochem. J 303, 671–677.
Courage, C., Budworth, J., and Gescher, A (1995) Comparison of ability of protein kinase inhibitors to arrest cell growth and to alter cellular protein kinase localisation Br J Cancer 71, 697–704.
Crepel, F, Audinat, E., Daniel, H., Hemart, N., Jaillard, D., Rossier, J, and Lambolez, B. (1994) Cellular locus of the nitric oxide-synthase involved in cerebellar long-term depression induced by high external potassium concentration. Neuropharmacology 33, 1399–1405.
Daub, H., Weiss, F. U., Wallasch, C, and Ullrich, A (1996) Role of transactivation of the EGF receptor in signalling by G-proteincoupled receptors. Nature 379, 557–560.
Davis, P. D, Hill, C. H, Keech, E., Lawton, G, Nixon, J. S, Sedgwick, A D., Wadsworth, J., Westmacott, D., and Wilkinson, S. E. (1989) Potent selective inhibitors of protein kinase FEBS Lett 259, 61–63.
Davis, P D., Elliott, L. H, Harris, W., Hill, C. H., Hurst, S. A., Keech, E, Kumar, M. K. H., Lawton, G., Nixon, J S., and Wilkinson, S E (1992) Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity. J. Med Chem 35, 994–1001
Day, R. N, Walder, J. A, and Maurer, R A. (1989) A protein kinase inhibitor gene reduces both basal and multihormone-stimulated prolactin gene transcription. J Biol. Chem 264, 431–436.
Desdouits, F., Cheetham, J. S, and Huang, H.-B., Kwon, Y.-G., da Cruz e Silva, E F., Denefle, P., Ehrlich, M. E, Nairn, A.C., Greengard, P., and Girault, J. A (1995) Mechanism of inhibition of protein phosphatase-1 by DARPP-32: studies with recombinant DARPP-32 and synthetic peptides. Biochem. Biophys. Res. Commun 206, 652–658.
Dildy-Mayfield, J. E., and Harris, R. A(1995) Ethanol inhibits kainate responses of glutamate receptors expressed in Xenopus oocytes: role of calcium and protein kinase J Neurosci 15, 3162–3171.
Doherty, P, Furness, J, Williams, E J., and Walsh, F. S. (1994) Neurite outgrowth stimulated by the tyrosine kinase inhibitor herbimycin A requires activation of tyrosine kinases and protein kinase J Neurochem. 62, 2124–2131.
Dolphin, A. C. (1992) The effect of phosphatase inhibitors and agents increasing cyclic-AMP-dependent phosphorylation on calcium channel currents in cultured rat dorsal root ganglion neurones. interaction with the effect of G protein activation. Pflugers Arch 421, 138–145
Dorée, M., and Galas, S. (1994) The cyclin-dependent protein kinases and the control of cell division. FASEB J. 8, 1114–1121.
Dostmann, W R G, Taylor, S. S., Genieser, H.-G., Jastorff, B., Doskeland, S. O., and ∅greid, D. (1990) Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinase I and II with analogs of adenosine 3′,5′-cyclic phosphorothioates. J Biol Chem. 265, 10,484–10,491.
Dudley, D. T, Pang, L., Decker, S. J., Bridges, A. J., and Saltiel, A. R. (1995) A synthetic inhibitor of the mitogen-activated protein kinase cascade Proc. Natl Acad Sci. USA 92, 7686–7689.
Eboli, M. L., Mercanti, D, Ciotti, M. T., Aquino, A., and Castellani, L. (1994) Glutamate-induced protein phosphorylation in cerebellar granule cells: role of protein kinase C. Neurochem. Res. 19, 1257–1264.
Edelman, A. M., Higgins, D. M., Bowman, C. L., Haber, S. N., Rabin, R. A, and Cho-Lee, J (1992) Myosin light chain kinase is expressed in neurons and glia · immunoblotting and immunocytochemical studies. Mol Brain Res 14, 27–34.
Eichholtz, T., de Bont, D B. A., de Widt, J., Liskamp, R M J., and Ploegh, H. L. (1993) A myristoylated pseudosubstrate peptide, a novel protein kinase inhibitor J. Biol. Chem. 268, 1982–1986
Enan, E. and Matsumura, F (1992) Specific inhibition of calcineurin by type II synaptic pyrethroid insecticides. Biochem. Pharmacol. 43, 1777–1784.
Endo, S, Critz, S. D, Byrne, J. H., and Shenolikar, S. (1995) Protein phos-phatases-1 regulates outward K+ currents in sensory neurons of Aplysia califormca J Neurochem 64, 1833–1840.
Enslen, H. and Soderling, T. R. (1994) Roles of calmodulin-dependent protein kmases and phosphatase in calcium-depenent transcription of immediate early genes. J Biol Chem. 33, 20,872–20,877.
Enslen, H., Sun, P., Brickey, D., Soderling, T. H., Klamo, E., and Soder-ling, T. R. (1994) Characterization of Ca2+/calmodulin-dependent protein kinase IV. Role in transcriptional regulation. J Biol. Chem. 269, 15,520–15,527.
Erneux, C., Van Sande, J., Jastorff, B., and Dumont, J. E. (1986) Modula-tion of cyclic AMP action in the dog thyroid by its agonist and antagonist Sp-and. Rp-adenosine 3′,5′-monophosphorothioate. Biochem J. 234, 193–197.
Evans, G. A., Garcia, G. G., Erwin, R., Howard, O. M., and Farrar, W. L. (1994) Pervanadate stimulates the effects of interleukin-2 (IL-2) in human T cells and provides evidence for the activation of two distinct tyrosine kinase pathways by IL-2. J. Biol Chem. 269, 23,407–23,412.
Fackler, M. J., Civin, C. I., and May, W. S. (1992) Up-regulation of sur-face CD34 is associated with protein kinase C-mediated hyperphosphorylation of CD34. J. Biol. Chem. 267, 17,540–17,546.ss
Fantl, W. J., Johnson, D E., and Williams, L. T. (1993) Signalling by recep-tor tyrosine kinases. Ann. Rev Biochem 62, 453–481.
Feinstein, D L., Galea, E., Cermak, J., Chugh, P., Lyandvert, L., and Reis, D. J. (1994) Nitric oxide synthase expression in glial cells suppression by tyrosine kinase inhibitors. J Neurochem` 62, 811–814.
Felipo, V., Minana, M. D., and Grisolia, S. (1993) Inhibitors of protein kinase prevent the toxicity of glutamate in primary neuronal cultures. Brain Res 604, 192–196
Fernandez, A., Mery, J., Vandromme, M., Basset, M., and Cavadore, J-C. (1991) Effective intracellular inhibition of the cAMP-dependent protein kinase by microinjection of a modified form of the specific inhibitor peptide PKI in living fibroblasts. Exp Cell Res. 195, 468–477.
ffrench-Mullen, J. M., Danks, P., and Spence, K. T. (1994) Neurosteroids modulate calcium currents in hippocampal CAI neurons via a pertussis toxin-sensitive G-protein-coupled mechanism. J Neurosci 14, 1963–1977.
Figurov, A., Boddeke, H., and Muller, D. (1993) Enhancement of AMPA-mediated synaptic transmission by the protein phosphatase inhibitor calyculin A in rat hippocampal slices. Eur J Neurosa 5, 1035–1041
Foulkes, J. G, Strada, S. J, Henderson, P. J, and Cohen, P. (1983) A kinetic analysis of the effects of inhibitor-1 and inhibitor-2 on the activity of protein phosphatase-1. Eur J Biochem. 132, 309–313.
Fry, D. W, Kraker, A. J., McMichael, A., Ambroso, L. A., Nelson, J. M., Leopold, W. R., Connors, R. W., and Bridges, A. J. (1994) A specific inhibitor of the epidermal growth factor receptor tyrosine kinase Science 265, 1093–1095.
Funauchi, M., Haruta, H., and Tsumoto, T. (1994) Effects of an inhibitor for calcium/calmodulin-dependent protein phosphatase, calcineurin, on induction of long-term potentiation in rat visual cortex. Neurosa. Res 19, 269–278.
Gadbois, D. M., Hamaguchi, J. R., Swank, R. A., and Bradbury, E. M. (1992) Staurosporine is a potent inhibitor of p34cdc2 and p34cdc2-like kinases. Biochem Btophys. Res. Commun 184, 80–85.
Garcia-Morales, P., Minami, Y., Luong, E., Klausner, R. D., and Smaelsin, L. E. (1990) Tyrosine phosphorylation in T cells is regulated by phosphatase activity: studies with phenylarsine oxide. Proc Natl Acad Sci USA 87, 9255–9259.
Garver, T. D, Oyler, G. A., Harris, K. A., Polavarapu, R., Damuni, Z., Lehman, R. A. W., and Billingsley, M. L. (1995) Tau phosphorylation in brain slices: pharmacological evidence for convergent effects of protein phosphatases on tau and mitogen-activated protein kinase. Mol Pharmacol 47, 745–756.
Gazit, A., Yaish, P., Gilon, C, and Levitazki, A. (1989) Tyrphostins I synthesis and biological activity of protein tyrosine kinase inhibitors. J. Med. Chem. 32, 2344–2352.
Gazit, A., Osherov, N., Posner, I., Yaish, P., Poradosu, E., Gilon, C, and Levitzki, A. (1991) Tyrphostms. 2. Heterocyclic and a-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J. Med. Chem. 34, 1896–1907.
Gjertsen, B. T., Mellgren, G., Otten, A., Maronde, E., Genieser, H.-G, Jastorff, B., Vintermyr, O K, McKnight, G. S., and Doskeland, S. O., (1995) Novel (Rp)-cAMPS analogs as tools for inhibition of cAMP-kinase in cell culture. J Biol. Chem 270, 20,599–20,607.
Glass, D. B. Cheng, H.-C, Kemp, B. E., and Walsh, D. A. (1986) Differ-ential and common recognition of the catalytic sites of cGMP-dependent and cAMP-dependent protein kinases by inhibitory peptides derived from the heat-stable inhibitor protein. J. Biol. Chem 261, 12,166–12,171
Glass, D.B., Cheng, H.-C, Mende-Mueller, L., Reed, J., and Walsh, D. A. (1989) Primary structural determinants essential for potent inhibition of cAMP-dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitor protein. J Biol Chem 264, 8802–8810.
Golard, A., Role, L., and Siegelbaum, S. A. (1994) Substance P potenti-ates calcium channel modulation by somatostatin in chick sympathetic ganglia. J Neurophysiol. 72, 2683–2690.
Goldberg, D. J. and Wu, D. Y. (1995) Inhibition of formation of filopodia after axotomy by inhibitors of protein tyrosine kinases. J Neurobiol 27, 553–560.
Golowash, J., Paupardin-Tritsch, D., and Gerschenfeld, H. M. (1995) En-hancement by muscarinic agonists of a high voltage-activated Ca2+ current via phosphorylation in a snail neuron. J Physiol. 485, 21–28.
Gong, M. C., Cohen, P., Kitazawa, T., Ikebe, M., Masuo, M., Somlyo, A. P., and Somlyo, A. V. (1992) Myosin light chain phosphatase activities and the effects of phosphatase inhibitors in tonic and phasic smooth muscle. J. Biol. Chem 267, 14,662–14,668.
Gordon, J. A. (1991) Use of vanadate as protein-tyrosine phosphatase inhibitor. Methods Enzymol 201, 477–482.
Gordon, S. E., Brautigan, D L., and Zimmerman, A. L. (1992) Protein phosphatases modulate the apparent agonist affinity of the lightregulated ion channel in retinal rods. Neuron 9, 739–748.
Grider, J. R. (1993) Interplay of VIP and nitric oxide in regulation of the descending relaxation phase of peristalsis. Am J Physiol. 264, G334–G340.
Griffith, L. C., Verselis, L. M., Aitken, K. M., Kyriacou, C. P., Danho, W., and Greenspan, R. J. (1993) Inhibition of calcium/calmodulin-dependent protein kinase in Drosophila disrupts behavioral plasticity. Neuron 10, 501–509.
Groschner, K., Schuhmann, K., Baumgartner, W., Pastushenko, V., Schindler, H., and Romanin, C. (1995) Basal dephosphorylation controls slow gating of L-type Ca2+ channels in human vascular smooth muscle. FEBS Lett 373, 30–34
Grove, J. R., Deutsch, P. J, Price, D. J, Habener, J. F., and Avruch, J. (1989) Plasmids encoding PKI(1–31), a specific inhibitor of cAMP-stimulated gene expression, inhibit the basal transcriptional activity of some but not all cAMP-regulated DNA response elements in JEG-3 cells. J. Biol. Chem 264, 19,506–19,513.
Gschwendt, M., Leibersperger, H., Kittstein, W., and Marks, F (1992) Protein kinase Cζ and η in murine epidermis. TPA induces downregulation of PKCη but not PKCζ. FEBS Lett 307, 151–155.
Gschwendt, M, Furstenberger, G, Leibersperger, H., Kittstein, W., Lindner, D., Rudolph, C, Barth, H., Kleinschroth, J., Marmé, D., Schachtele, C, and Marks, F. (1995) Lack of an effect of novel inhibitors with high specificity for protein kinase on the action of the phorbol ester 12-O-tetradecanoylphorbol-13-acetate on mouse skin in vivo Carcinogenesis 16, 107–111.
Gutierrez, L. M., Viniegra, S., Quintanar, J. L., Reig, J A, and Sala, F. (1994) Calyculin A blocks bovine chromaffin cell calcium channels independently of phosphatase inhibition. Neurosa. Lett 178, 55–58.
Haavik, J., Schelling, D. L., Campbell, D. G., Andersson, K. K., Flatmark, T., and Cohen, P (1989) Identification of protein phosphatase 2A as the major tyrosine hydroxylase phosphatase in adrenal medulla and corpus striatum: evidence from the effects of okadaic acid. FEBS Lett. 251, 36–42.
Hack, N., Hidaka, H., Wakefield, M. J., and Balaázs, R. (1993) Promotion of granule cell survival by high K+ or excitatory ammo acid treatment and Ca2+ / calmodulin-dependent protein kinase activity. Neuroscience 57, 9–20.
Hajimohammadreza, I., Probert, A W., Coughenour, L. L., Borosky, S A, Marcoux, F W., Boxer, P. A., and Wang, K. K. W. (1995) A specific inhibitor of calcium/calmodulin-dependent protein kinase-II provides neuroprotection against NMD A-and hypoxia/hypoglycemia-induced cell death. J Neurosa 15, 4093–4104
Han, Y. F. and Dokas, L. A. (1991) Okadaic acid-induced inhibition of B-50 dephosphorylation by presynaptic membrane-associated pro-tein phosphatases. J. Neurochem 57, 1325–1331.
Hanks, S. K., Quinn, A. M., and Hunter, T. (1988) The protein kinase family: conserved features and deduced phylogeny of the catalytic domains. Science 241, 42–52
Hannun, Y. A., Merrill, A. H., Jr., and Bell, R. M. (1991) Use of sphingosine as inhibitor of protein kinase C. Methods Enzymol. 201, 316–328.
Hardie, D. G., Haystead, T. A. J., and Sim, A. T. R. (1991) Use of okadaic acid to inhibit protein phosphatases in intact cells. Methods Enzymol 201, 469–477.
Hashimoto, Y., Perrino, B. A., and Soderling, T. R. (1990) Identification of an autoinhibitory domain in calcineurin. J. Biol Chem. 265, 1924–1927.
Helmeste, D. M., and Tang, S. W. (1994) Kinase inhibitors compete with imipramine for binding and inhibition of serotonin transport. Eur J Pharmacol. 267, 239–242.
Hemmings, H. C., Jr. and Adamo, A. I. B. (1996) Activation of endog-enous protein kinase by halothane in synaptosomes. Anesthesiology 84, 652–662.
Hemmings, H. C, Jr., Greengard, P, Tung, H. Y. L., and Cohen, P. (1984) DARPP-32, a dopamine-regulated neuronal phosphoprotein, is a potent inhibitor of protein phosphatase-1. Nature 310, 503–505.
Hemmings, H. C, Jr., Nairn, A. C, Elliott, J. I., and Greengard, P (1990) Synthetic peptide analogs of DARPP-32 (Mr 32,000 dopamine-and cAMP-regulated phosphoprotein), an inhibitor of protein phosphatase-1: phosphorylation, dephosphorylation and inhibitory activity. J. Biol. Chem. 265, 20,369–20,376.
Hemmings, H. C, Jr., Desdouits, F., and Girault, J.-A. (1995) DARPP-32 (dopamine-and cyclic AMP-regulated phosphoprotein, Mr 32,000), a neuronal protein phosphatase-1 inhibitor: preparation and biochemical analysis. Neuroprotocols 6, 35–45.
Herbert, J. M., Augereau, J. M., Gleye, J., and Maffrand, J. P. (1990) Chelerythnne is a potent and specific inhibitor of protein kinase C. Biochem Biophys Res. Commun. 172, 993–999.
Herzig, S., Meier, A., Pfeiffer, M, and Neumann, J. (1995) Stimulation of protein phosphatases as a mechanism of the muscarinic-receptor-mediated inhibition of cardiac L-type Ca2+ channels. Pflugers Arch. 429, 531–538.
Hidaka, H. and Kobayashi, R. (1992) Pharmacology of protein kinase inhibitors Ann. Rev Pharmacol Toxicol. 32, 377–397
Hingtgen, C. M. and Vasko, M. R. (1994) The phosphatase inhibitor, okadaic acid, increases peptide release from rat sensory neurons in culture. Neurosci Lett. 178, 135–138.
Hoffmann, F., Bechtel, P. J., and Krebs, E. G. (1977) Concentrations of cyclic AMP-dependent protein kinase subunits in various tissues. J. Biol. Chem. 252, 1441–1447.
Honkanen, R. E. (1993) Cantharidin, another natural toxin that inhibits the activity of serine/threonine protein phosphatases types 1 and 2A. FEBS Lett 330, 283–286.
Honkanen, R. E., Zwillers, J., Moore, R. E., Daily, S. L., Khatra, B. S., Dukelow, M., and Boynton, A. L. (1990) Characterization of microcystin-LR, a potent inhibitor of type 1 and type 2A protein phosphatases. J. Biol. Chem 265, 19,401–19,404.
Hsu, C.-Y. J., Persons, P. E., Spada, A. P., Bednar, R. A., Levitzki, A., and Zilberstein, A. (1991) Kinetic analysis of the inhibition of the epi-dermal growth factor receptor tyrosine kinase by Lavendustin-A and its analogue. J. Biol. Chem 266, 21,105–21,112.
Hu, B. R., Yang, Y and Wieloch, T. (1993) Depression of neuronal protein synthesis initiation by protein tyrosine kinase inhibitors. J Neurochem 61, 1789–1794.
Hug, H. and Sarre, T. F. (1993) Protein kinase isoforms: divergence in signal transduction? Biochem J. 291, 329–343.
Huggenvik, J. I., Collard, M. W., Stofko, R. S., Seasholtz, A. F., and Uhler, M. D (1991) Regulation of the human enkephalin promotor by two isoforms of the catalytic subunit of cyclic adenosine 3′,5′-monophosphate-dependent protein kinase. Mol. Endocnnol. 5, 921–930.
Hvalby, ∅., Hemmings, H. C., Jr., Paulsen, O., Czernik, A. J, Nairn, A C., Godframd, J.-M., Jensen, V., Raastad, M., Strom, J. F., Andersen, P., and Greengard, P (1994) Specificity of protein kinase inhibitor peptides and induction of long-term potentiation Proc Natl Acad Sci USA 91, 4761–4765
Ichinose, M., Endo, S., Critz, S. D, Shenolikar, S, and Byrne, J. H. (1990) Microcystin-LR, a potent phosphatase inhibitor, prolongs the serotonin-and cAMP-mduced currents in sensory neurons of Aplysia californica. Brain Res 533, 137–140
Ishida, A., Kameshita, I., Okuno, S., Kitani, T., and Fujisawa, H. (1995) A novel highly specific and potent inhibitor of calmodulin-dependent protein kinase II Biochem. Biophys. Res Commun 212, 806–812.
Ishihara, H., Martin, B. L., Brautigan, D. L., Karaki, H., Ozaki, H., Kato, Y., Fusetani, N., Watabe, S., Hashimoto, K., Uemura, D, and Hartshorne, D. J. (1989) Calyculin A and okadaic acid: inhibitors of protein phosphatase activity Biochem Biophys Res Commun 159, 871–877
Ishii, H., Jirousek, M. R., Koya, D., Takagi, C, Xia, P., Clermont, A., Bursell, S.-E., Kern, T S., Ballas, L. M., Heath, W. F., Stramm, L. E., Feener, E. P., and King, G. L. (1996) Amelioration of vascular dysfunctions in diabetic rats by an oral PKCp inhibitor Science 272, 728–731
Ishii, A., Kiuchi, K., Kobayashi, R., Sumi, M., Hidaka, H., and Nagatsu, T. (1991) A selective Ca2+/calmodulm-dependent protein kinase II inhibitor, KN-62, inhibits the enhanced phosphorylation and the activation of tyrosine hydroxylase by 56 mM K+ in rat pheochromocytoma PC12h cells Biochem Biophys Res Commun 156, 1051–1056.
Ishikawa, T., Chijiwa, T., Hagiwara, M., Mamiya, S., Saitoh, M., and Hidaka, H. (1988) ML-9 inhibits the vascular contraction via the inhibition of myosin light chain phosphorylation. Mol Pharmacol 33, 598–603.
Ito, I., Hidaka, H., and Sugiyama, H. (1991) Effects of KN-62, a specific inhibitor of calcium /calmodulin-dependent protein kinase II, on long-term potentiation in the rat hippocampus. Neurosci. Lett 121, 119–121.
Itoh, T., Ikebe, M., Kargacin, G J., Hartshorne, D. J., Kemp, B.E., and Fay, F. S. (1989) Effect of modulators of myosin light-chain kinase activity in single smooth muscle cells. Nature 338, 164–168.
Izquierdo, M., Leevers, S.J., Williams, D. H., Marshall, J., Weiss, A, and Cantrell, D. (1994) The role of protein kinase in the regulation of extracellular signal-regulated kinase by the T cell antigen receptor. Eur J Immunol 24, 2462–2468.
Jian, X., Hidaka, H., and Schmidt, J. T. (1994) Kinase requirement for retinal growth cone motility J. Neurobiol 25, 1310–1328.
Kase, H., Iwahashi, K., Nakanishi, S., Matsuda, Y., Yamada, K., Takahashi, M., Murakata, C, Sato, A., and Kaneko, M. (1987) K-252 compounds, novel and potent inhibitors of protein kinase and cyclic nucleotide-dependent protein kmases. Biochem. Biophys Res. Commun 142, 436–440.
Kedzierski, W., Aguila-Mansilla, N., Kozlowski, G. P., and Porter, J.C., (1994) Expression of tyrosine hydroxylase gene in cultured hypothalamic cells: roles of protein kinase A and C. J. Neurochem. 62, 431–437.
Keller, H. U. and Niggli, V. (1993) The PKC-inhibitor Ro 31-8220 selec-tively suppresses PMA-and diacylglycerol-mduced fluid pinocytosis and actin polymerization in PMNS. Biochem Biophys Res Commun 194, 1111–1116
Kemp, B. E. and Pearson, R B. (1991) Design and use of peptide sub-strates for protein kinases. Methods Enzymol. 200, 121–134.
Kemp, B. E, Pearson, R., and House, M. (1991) Pseudosubstrate-based peptide inhibitors Methods Enzymol 201, 287–304
Keyser, D. O. and Alger, B. E. (1990) Arachidonic acid modulates hippocampal calcium current via protein kinase and oxygen radicals Neuron 5, 545–553.
Kim, K.-S., Tinti, C, Song, B., Cubells, J. F., and Joh, T. H. (1994) Cyclic AMP-dependent protein kinase regulates basal and cyclic AMP-stimulated but not phorbol ester-stimulated transcription of the tyrosine hydroxylase gene J. Neurochem. 63, 834–842.
Kindy, M. S. (1993) Inhibition of tyrosine phosphorylation prevents delayed neuronal death following cerebral ischemia. J Cereb. Blood Flow Metab. 13, 372–377.
Kitagawa, M., Okabe, T., Ogino, H., Matsumoto, H., Suzuki-Takahashi, I., Kokubo, T, Higashi, H, Saitoh, S., Taya, Y., Yasuda, H., Ohba, Y., Nishimura, S., Tanaka, N., and Okuyama, A. (1993) Butyrolactone I, a selective inhibitor of cdk2 and cdc2 kinase. Oncogene 8, 2425–2432.
Klann, E, Chen, S. J., and Sweatt, J. D. (1991) Persistent protein kinase activation in the maintenance phase of long-term potentiation. J. Biol Chem. 266, 24,253–24,256.
Klann, E., Chen, S. J., and Sweatt, J. D. (1992) Increased phosphoryla-tion of a 17-kDa protein kinase substrate (P-17) in long-term potentiation. J. Neurochem 58, 1576–1579.
Klee, C.B., Draetta, G. F., and Hubbard, M. J. (1988) Calcineurin Adv. Enzymol. 61, 149–200.
Knusel, B. and Hefti, F. (1992) K-252 compounds: modulators of neurotrophin signal transduction. J. Neurochem 59, 1987–1996.
Kobayashi, E., Nakano, H., Morimoto, M, and Tamaoki, T. (1989) Calphostin (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C. Biochem. Biophys. Res Commun. 159, 548–553
Kolaj, M., Cerne, R., Cheng, G., Brickley, D. A., and Randic, M. (1994) Alpha subunit of calcium/calmodulin-dependent protein kinase enhances excitatory amino acid and synaptic responses of rat spinal dorsal horn neurons. J. Neurophysiol 72, 2525–2531
Kovalenko, M., Gazit, A., Bóhmer, A., Rorsman, C., Ronnstrand, L., Heldin, C-H., Waltenberger, J., Bohmer, F.-D., and Levitzki, A (1995) Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation Cancer Res. 54, 6106–6114.
Kumakura, K., Sasaki, K, Sakurai, T, Ohara-Imaizumi, M, Misonou, H., Nakamura, S., Matsuda, Y., and Nonomura, Y (1994) Essential role of myosin light chain kinase in the mechanism for MgATP-dependent priming of exocytosis in adrenal chromaffin cells. J Neurosa. 14, 7695–7703.
Kurino, M., Fukunage, K., Ushio, Y., and Miyamoto, E. (1995) Activation of mitogen-activated protein kinase in cultured rat hippocampal neurons by stimulation of glutamte receptors. J. Neurochem 65, 1282–1289.
Le Cabec, V. and Maridonneau-Parini, I. (1995) Complete and revers-ible inhibition of NADPH oxidase in human neutrophils by phenylarsine oxide at a step distal to membrane translocation of the enzyme subunits. J. Biol Chem 270, 2067–2073.
Levitzki, A. and Gazit, A. (1995) Tyrosine kinase inhibition, an approach to drug development. Science 267, 1782–1788
Lew, J. and Wang, J. H. (1995) Neuronal cdc2-like kinase. Trends Biochem. Sci. 20, 33–37.
Li, G., Hidaka, H., and Wollheim, C.B., (1992) Inhibition of voltage-gated Ca2+ channels and insulin secretion in HIT cells by the Ca2+/calmodulin-dependent protein kinase II inhibitor KN-62: comparison with antagonists of calmodulin and L-type Ca2+ channels. Mol. Pharmacol. 42, 489–498.
Li, Y.-M., MacKintosh, C, and Casida, J. E. (1993) Protein phosphatase 2A and its [3H]cantharidin/[3H]endothall thioanhydride binding site: inhibitor specificity of cantharidin and ATP analogues. Biochem. Pharmacol. 46, 1435–1443.
Liao, K., Hoffman, R. D., and Lane, M. D. (1991) Phosphotyrosyl turn-over in insulin signaling. Characterization of two membane-bound ppl5 protein tyrosine phosphatases from 3T3-L1 adipocytes. J. Biol Chem 266, 6544–6553.
Lieberman, D N. and Mody, I. (1994) Regulation of NMDA channel function by endogenous Ca2+-dependent phosphatase. Nature 369, 235–239.
Linden, D. J. and Conner, J. A. (1991) Participation of postsynaptic PKC in cerebellar long-term depression in culture. Science 254, 1656–1659.
Liu, J., Farmer, J. D., Jr., Lane, W. S., Friedman, J., Weissman, I., and Schreiber, S. L. (1991) Calcineurin is a common target of cyclophilincyclosporin A and FKBP-FK506 complexes. Cell 66, 807–815.
Liu, J.-P., Sim, A. T. R., and Robinson, P J. (1994) Calcineurin inhibition of dynamin I GTPase activity coupled to nerve terminal depolarization. Science 265, 970–973.
Lopez-Molina, L., Boddeke, H, and Muller, D (1993) Blockade of long-term potentiation and of NMDA receptors by the protein kinase antagonist calphostin C. Naunyn Schmiedebergs Arch Pharmacol 348, 1–6.
Losiewicz, M. D., Carlson, B. A., Kaur, G., Sausville, E. A., and Worland, P. J. (1994) Potent inhibition of cdc2 kinase activity by the flavonoid L86-8275. Biochem. Biophys. Res Commun. 201, 589–595.
MacKintosh, C., and Klumpp, S (1990) Tautomycin from the bacterium Streptomyces verticillatus, another potent and specific inhibitor or protein phosphatases 1 and 2A. FEBS Lett 277, 137–140.
MacKintosh, C. and MacKintosh, R. W. (1994) Inhibitors of protein kin-ases and phosphatases. Trends Biochem. Sci 19, 444–448.
MacKintosh, C, Beattie, K. A, Klumpp, S., Cohen, P., and Codd, G. A. (1990) Cyanobacterial microcystin-LR is a potent and specific inhibitor of protein phosphatases 1 and 2A from both manmmals and higher plants. FEBS Lett 264, 187–192.
Mahon, T. M. and O’Neill, L A. J. (1995) Studies into the effect of the tyrosine kinase inhibitor herbimycin A on NF-κactivation in T lymphocytes. J Biol Chem. 270, 28,557–28,564.
Majumdar, S., Kane, L. H., Rossi, M. W, Volpp, D., Nauseef, W M, and Korchak, H. M. (1993) Protein kinase isotypes and signaltransduction in human neutrophils: selective substrate specificity of calcium-dependent beta-PKC and novel calcium-independent nPKC. Biochim. Biophys. Acta 1176, 276–286.
Malenka, R. C, Kauer, J. A., Perkel, D. J., Mauk, M. D., and Kelly, P. T. (1989) An essential role for postsynaptic calmodulin and protein kinase activity in long-term potentiation. Nature 340, 554–557.
Malinow, R., Schulman, H., and Tsien, R. W. (1989) Inhibition of postsyn-aptic PKC or CaMKII blocks induction but not expression of LTP. Science 245, 862–866.
Mamiya, N., Goldenring, J. R., Tsunoda, Y., Modlin, I. M., Yasui, K., Usuda, N., Ishikawa, T., Natsume, A., and Haidaka, H. (1993) Inhibition of acid secretion in gastric parietal cells by the Ca2+/ calmodulin-dependent protein kinase II inhibitor KN-93. Biochem. Biophys Res Commun 195, 608–615.
Margolis, B., Rhee, S G., Felder, S., Mervic, M., Lyall, R., Levitzki, A., Ullrich, A., Zilberstein, A., and Schlessmger, J. (1989) EGF induces tyrosine phosphorylation of phospholipase C-II: a potential mechanism for EGF receptor signaling. Cell 57, 1101–1107
Markovits, J., Larsen, A K., Segal-Bendirdjian, E., Fosse, P., Saucier, J. M., Gazit, A., Levitzki, A., Umezawa, K., and Jacquemin-Sablon, A(1994) Inhibition of DNA topoisomerases I and II and induction of apoptosis by erbstatin and tyrphostin derivatives. Biochem. Pharmacol 48, 549–560.
Martiny-Baron, G., Kazanietz, M. G., Mischak, H., Blumberg, P M, Kochs, G., Hug, H., Marmé, D., and Schachtele, C., (1993) Selective inhibition of protein kinase isozymes by the indolocarbazole Gò 6976 J. Biol Chem 268, 9194–9197
Mathis, C, Lehmann, J., and Ungerer, A. (1992) The selective protein kinase inhibitor, NPC 15437, induces specific deficits in memory retention in mice Eur J Pharmacol 220, 1101–1107.
Matsushima, R., Yoshizawa, S, Watanabe, M. F, Harada, K., Furusawa, M., Carmichael, W. W, and Fujiki, H. (1990) In vitro and in vivo effects of protein phosphatase inhibitors, microcystins and nodularin, on mouse skin and fibroblasts Biochem Biophys Res Commun. 171, 867–874.
Mattiazzi, A., Hove-Madsen, L., and Bers, D. M. (1994) Protein kinase inhibitors reduce SR Ca2+ transport in permeabihzed myocytes. Am J. Physiol 267, H812–H820.
McCarron, J G., McGeown, J G., Reardon, S., Ikebe, M., Fay, F. S, and Walsh, J. V., Jr. (1992) Calcium-dependent enhancement of calcium current in smooth muscle by calmodulin-dependent protein kinase II. Nature 357, 74–77
Meydan, N., Grunberger, T., Dadi, H., Shahar, M, Arpaia, E., Lapidot, Z, Leeder, J. S., Freedman, M., Cohen, A., Gazit, A., Levitzki, A., and Roifman, C. M., (1996) Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor. Nature 379, 645–648.
Miller, D. R., Lee, G. M., and Maness, P. F. (1993) Increased neurite out-growth induced by inhibition of protein tyrosine kinase activity in PC12 pheochromocytoma cells. J Neurochem 60, 2134–2144.
Mizuno, K., Noda, K., Udea, Y., Hanaki, H., Saido, T. C, Ikuta, T., Kuroki, T., Tamaoki, T., Hirai, S.-I., Osada, S., and Ohno, S (1995) UCN-01, an anti-tumor drug, is a selective inhibitor of the conventional PKC family. FEBS Lett. 359, 259–261.
Mochida, S., Nonomura, Y., and Kobayashi, H. (1994) Analysis of the mechanism for acetylcholine release at the synapse formed between rat sympathetic neurons in culture. Microsc Res. Tech. 29, 94–102.
Monteiro, H. P., Ivaschenko, Y., Fischer, R., and Stern, A. (1991) Inhibi-tion of protein tyrosine phosphatase activity by diamide is reversed by epidermal growth factor in fibroblasts. FEBS Lett 295, 146–148.
Morgan, D. (1995) Principles of CDK regulation. Nature 374, 131–134.
Muid, R. E, Dale, M M., Davis, P. D., Elliott, L H., Hill, C.H., Kumar, H., Lawton, G., Twomey, M., Wadsworth, J., Wilkinson, S. E., and Nixon, J. S (1991) A novel conformationally restricted protein kinase inhibitor, Ro 31-8425, inhibits human neutrophil superoxide generation by soluble, particulate and post-receptor stimuli. FEBS Lett 293, 169–172.
Mulkey, R. M., Herron, C.E.,, and Malenka, R.C., (1993) An essential role for protein phosphatases in hippocampal long-term depression. Science 261, 1051–1055.
Mulkey, R. M., Endo, S, Shenolikar, S., and Malenka, R. C. (1994) Involve-ment of a calcineurin/inhibitor-1 phosphatase cascade in hippocampal long-term depression. Nature 369, 486–488.
Muller, W., Petrozzmo, J. J, Griffith, L. C, Danho, W., and Conner, J. A (1992) Specific involvement of Ca2+-calmodulin kinase II in cholinergic modulation of neuronal responsiveness. J. Neurophysiol. 68, 2264–2269.
Murata, K., Sakon, M., Kambayashi, J., Yukawa, M., Yano, Y., Fujitani, K., Kawasaki, T, Shiba, E., and Mori, T. (1993) The possible involvement of protein phosphatase 1 in thrombm-induced Ca2+ influx of human platelets. J. Cell Biochem. 51, 442–445.
Nagatsu, T., Suzuki, H., Kiuchi, K., Saitoh, M., and Hidaka, H. (1987) Effects of myosin light-chain kinase inhibitor on catecholamine secretion from rat pheochromocytoma PC12h cells. Biochem. Biophys Res. Commun 143, 1045–1048
Nairn, A. C. and Picciotto, M. R. (1994) Calcium/calmodulin-dependent protein kinases Cancer Biol 5, 295–303
Nairn, A. C. and Shenolikar, S. (1992) The role of protein phosphatases in synaptic transmission, plasticity and neuronal development. Curr. Opinion Neurobiol. 2, 296–301.
Nakanishi, S., Kakita, S., Takahashi, I., Kawahara, K., Tsukuda, E., Sano, T., Yamada, K., Yoshida, M., Kase, H., and Matsuda, Y. (1992) Wortmannm, a microbial product inhibitor of myosin light chain kinase. J. Biol Chem. 267, 2157–2163.
Nakazawa, K., Mikawa, S., Hashikawa, T., and Ito, M. (1995) Transient and persistent phosphorylation of AMP A-type glutamate receptor subunits in cerebellar Purkinje cells Neuron 15, 697–709.
Neumann, J., Herzig, S., Boknik, P., Apel, M., Kaspareit, G., Schmitz, W., Scholz, H., Tepel, M, and Zimmermann, N. (1995) On the cardiac contractile, biochemical and electrophysiological effects of cantharidin, a phosphatase inhibitor. J. Pharmacol. Exp. Ther. 274, 530–539.
Nichols, R. A., Sihra, T. S., Czernik, A. J., Nairn, A. C, and Greengard, P. (1990) Calcium/calmodulin-dependent protein kinase II increases glutamate and noradrenaline release from synaptosomes. Nature 343, 647–651.
Nichols, R. A., Suplick, G. R., and Brown, J. M. (1994) Calcineurin-medi-ated protein dephosphorylation in brain nerve terminals regulates the release of glutamate. J. Biol Chem. 269, 23,817–23,823
Nichols, R. A., Suplick, G. R., and Golemme, S. S. (1996) Inhibition of phosphatases 1 and 2A reduces stimulation-induced glutamate release from synaptosomes by inhibiting Ca2+ influx. J Neurochem, in press.
Niki, L., Okazaki, K., Saitoh, M., Niki, A., Niki, H., Tamagawa, T., Iguchi, A., and Hidaka, H. (1993) Presence and possible involvement of Ca2+/ calmodulin dependent protein kinases in insulin release from the rat pancreatic β cell Biochem. Biophys Res. Commun 191, 255–261.
Nixon, J S, Bishop, J., Bradshaw, D., Davis, P. D., Hill, H., Elliott, L H., Kumar, H., Lawton, G., Lewis, E. J, Mulqueen, M., Westmacott, D., Wadsworth, J., and Wilkinson, S. E. (1992) The design and biological properties of potent and selective inhibitors of protein kinase C. Biochem. Soc. Trans. 20, 419–425.
Noronha, K. F. and Mercier, A. J (1995) A role for calcium/calmodulin-dependent protein kinase in mediating synaptic modulation by a neuropeptide. Brain Res. 673, 70–74
Nye, S H, Squinto, S. P., Glass, D. J, Stitt, T. N., Hantzopoulos, P., Macchi, M. J., Lindsay, N. S., Ip, N. Y., and Yancopoulos, G. D. (1992) K-252a and staurosporine selectively block autophosphory-lation of neurotrophin receptors and neurotrophin-mediated responses. Mol. Biol Cell 3, 677–686.
O’Dell, T. J., Kandel, E. R., and Grant, S. G. N. (1991) Long-term poten-tiation in the hippocampus is blocked by tyrosine kinase inhibitors. Nature 353, 558–560.
Ogiwara, T., Murdoch, G., Chik, C. L., and Ho, A. K. (1995) Tyrosine kinase inhibitors enhance cGMP production in rat pinealocytes. Biochem Biophys. Res. Commun. 207, 994–1002.
∅greid, D., Dostmann, W., Genieser, H.-G., Niemann, P., Doskeland, S. O., and Jastorff, B., (1994) (Rp)-and (Sp)-8-piperidino-adenosme 3′,5′-(cyclic)thiophosphatases discriminate completely between site A and of the regulatory subunits of cAMP-dependent protein kinase type I and II. Eur J. Biochem 221, 1089–1094.
Ohara-Imaizumi, M., Sakurai, T., Nakamura, S., Nakanishi, S., Matsuda, Y., Muramatsu, S., Nonmura, Y., and Kumakura, K. (1992) Inhibition of Ca2+-dependent catecholamine release by myosin light chain kinase inhibitor, wortmannm, in adrenal chromaffin cells. Biochem. Biophys. Res, Commun 185, 1016–1021.
Ohmichi, M, Pang, L., Ribon, V., Gazit, A., Levitzki, A., and Saltiel, A. R. (1993) The tyrosine kinase inhibitor tyrphostin blocks the cellular actions of nerve growth factor Biochemistry 32, 4650–4658
Okada, D. (1995) Protein kinase modulates calcium sensitivity of nitric oxide synthase in cerebellar slices. J Neurochem 64, 1298–1304.
Okazaki, K., Ishikawa, T., Inui, M., Tada, M., Goshima, K., Okamoto, T., and Hidaka, H. (1994) KN-62, a specific Ca2+Jcalmoduhn-dependent protein kinase inhibitor, reversibly depresses the rate of beating of cultured fetal mouse cardiac myocytes J Pharmacol Exp. Ther. 270, 1319–1324
Olsen, S. R and Uhler, M. D (1991) Inhibition of protein kinase-A by overexpression of the cloned human protein kinase inhibitor. Mol Endocrinol 5, 1246–1247
Onoda, T., Linuma, H., Sasaki, Y., Hamada, M., Isshiki, K., Naganawa, H., Takeuchi, T., Tatsuta, K., and Umezawa, K. (1989) Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus. J Nat. Prod 52, 1252–1257
Onozuka, M., Watanabe, K., Nagata, K.-Y., and Imai, S. (1994) Involve-ment of a Ca++/calmodulin-dependent protein kinase II-associated mechanism in the induction of an outward potassium current by quisqualate. Brain Res 650, 336–340.
Osborne, P. B. and Williams, J. T. (1995) Characterization of acute homol-ogous desensitization of μ-opioid receptor-induced currents in locus coeruleus neurons. Br J Pharmacol 115, 925–932.
Osherov, N. and Levitzki, A (1994) Epidermal-growth-factor-dependent activation of the Src-family kmases. Eur J Biochem. 225, 1047–1053.
Otero, A D. S. and Sweitzer, N. M. (1993) Benzoquinoid tyrosine kinase inhibitors are potent blockers of cardiac muscarinic receptor function Mol Pharmacol 44, 595–604.
Pang, L, Sawada, T., Decker, S. J., and Saltiel, A. R. (1995) Inhibition of MAP kinase kinase blocks the differentiation of PC-12 cells induced by nerve growth factor J Biol Chem 270, 13,585–13,588.
Park, D. S., Farinelli, S. E., and Greene, L. A. (1996) Inhibitors of cyclin-dependent kinases promote survival of post-mitotic neuronally differentiated PC12 cells and sympathetic neurons. J Biol. Chem 271, 8161–8169.
Parsons, J. N., Wiederrecht, G. J., Salowe, S., Burbaum, J. J., Rokosz, L L., Kincaid, R. L., and O’Keefe, S. J. (1994) Regulation of calcineurin phosphatase activity and interaction with the FK-506●FK-506 binding protein complex. J Biol. Chem. 269, 19,610–19,616.
Pavlakovic, G., Eyer, C. L., and Isom, G. E (1995) Neuroprotective effects of PKC inhibition against chemical hypoxia. Brain Res. 676, 205–211.
Pawson, T. (1995) Protein modules and signalling networks. Nature 373, 573–579.
Payne, M. E., Fong, Y L., Ono, R. J., Colbran, R. J., and Kemp, B.E., (1988) Calcium/calmodulin-dependent protein kinase II. Characterization of distinct calmodulin binding and inhibitory domains. J Biol. Chem. 263, 7190–7195.
Peng, H. Baker, L. P., and Dai, Z. (1993) A role of tyrosine phosphoryla-tion in the formation of acetylcholine receptor clusters induced by electric fields in cultured Xenopus muscle cells. J. Cell Biol. 120, 197–204.
Posner, I., Engel, M., Gazit, A., and Levitzki, A. (1993) Kinetics of inhi-bition by tyrphostins of the tyrosine kinase activity of the epidermal growth factor receptor and analysis by a new computer program Mol. Pharmacol. 45, 673–683.
Powis, G. (1991) Signalling targets for anticancer drug development TIPS 12, 188–194.
Powis, G, Bonjouklian, R., Berggren, M. M, Gallego, A, Abraham, R., Ashendel, C, Zalkow, L, Matter, W. F., Dodge, J., Grindey, G., and Vlahos, C. J., (1994) Wortmannm, a potent and selective inhibitor of phosphatidylinositol-3-kinase Cancer Res 54, 2419–2423.
Quick, J, Ware, J. A, and Driedger, P. E (1992) The structure and bio-logical activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source Biochem Biophys Res Commun 187, 657–663
Reber, B. F. and Bouron, A (1995) Calyculin-A-induced fast neurite retraction in nerve growth factor-diferentiated rat pheochromocytoma (PC12) cells. Neurosa Lett 183, 198–201.
Reeve, H. L., Vaughan, P. F., and Peers, C., (1995) Enhancement of Ca2+ channel currents in human neuroblastoma (SH-SY5Y) cells by phorbol esters with and without activation of protein kinase C. Pflugers Arch 429, 729–737
Reinhart, P. H. and Levitan, I. B. (1995) Kinase and phosphatase activi-ties intimately associated with a reconstituted calcium-dependent potassium channel. J Neurosa. 15, 4572–4579.
Reisine, T., Rougon, G., and Barbet, J. (1986) Liposome delivery of cyclic AMP-dependent protein kinase inhibitor into intact cells, specific blockade of cyclic AMP-mediated adrenocorticotropm release from mouse anterior pituitary tumor cells. J Cell Biol 102, 1630–1637.
Reisine, T., Rougon, G, Barbet, J, and Affolter, H U. (1985) Corticotropin-releasmg factor-induced adrenocorticotropin hormone release and synthesis is blocked by incorporation of the inhibitor of cyclic AMP-dependent protein kinase into anterior pituitary tumor cells by liposomes. Proc. Natl. Acad. Sci USA 82, 8261–8265
Robinson, P J. (1992) Potencies of protein kinase inhibitors are depen-dent on the activators used to stimulate the enzyme. Biochem. Pharmacol. 44, 1325–1334
Rodriguez, J, Quignard, J.-F., Fagni, L., Lafon-Cazal, M., and Bockaert, J. (1994) Blockade of nitric oxide synthesis by tyrosine kinase inhib-itors in neurones. Neuropharmacology 33, 1267–1274.
Rüegg, U. T. and Burgess, G. M. (1989) Staurosporine, K-252 and UCN-01 · potent but nonspecific inhibitors of protein kmases. TIPS 10, 218–220.
Saitoh, M., Naka, M., and Hidaka, H. (1986) The modulatory role of myosin light chain phosphorylation in human platelet activation Biochem Biophys. Res Commun. 140, 280–287.
Saitoh, M, Ishikawa, T., Matsushima, S., Naka, M., and Hidaka, H. (1987) Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase. J Biol Chem 262, 7796–7801.
Sargeant, P., Farndale, R. W., and Sage, S. O. (1993) ADP-and thapsigargin-evoked Ca2+ entry and protein-tyrosine phosphorylation are inhibited by the tyrosine kinase inhibitors genistein and methyl-2,5-dihydroxycinnamate in fura-2-loaded human platelets. J Biol Chem 268, 18,151–18,156.
Sato, K.-L, Miki, S., Tachibana, H., Hayashi, F., Akiyama, T., and Fukami, Y. (1990) A synthetic peptide corresponding to residues 137 to 157 of pp60v-src inhibits tyrosine-specific protein kinases Biochem Biophys. Res. Commun. 171, 1152–1159
Shigeri, Y. and Fujimoto, M. (1994) Y2 receptors for neuropeptide Y are coupled to three intracellular signal transduction pathways in a human neuroblastoma cell line. J Biol. Chem 269, 8842–8848
Shimokado, K., Yokota, T., Umezawa, K., Sasaguri, T., and Ogata, J. (1994) Protein tyrosine kinase inhibitors inhibit chemotaxis of vascular smooth muscle cells. Arteriosclerosis Thromb 14, 973–981.
Sihra, T. S. and Pearson, H. A. (1995) Ca/Calmodulin-dependent kinase II inhibitor KN62 attenuates glutamate release by inhibiting voltage-dependent Ca2+-channels. Neuropharmacology 34, 731–741
Sihra, T. S., Bogonez, E., and Nicholls, D. G(1992) Localized Ca2+entry preferentially effects protein dephosphorylation, phosphorylation, and glutamate release J Biol Chem 267, 1983–1989
Sim, A. T. R., Lloyd, H. G. E., Jarvie, P. E., Morrison, M., Rostas, J. A. P, and Dunkley, P. R. (1993) Synaptosomal amino acid release-effect of inhibiting protein phosphatases with okadaic acid Neuroscience Lett. 160, 181–184.
Sim, A. T. R., Ratcliffe, E., Mumby, M. C, Villa-Moruzzi, E., and Rostas, J. A. P. (1994) Differential activities of protein phosphatase types 1 and 2A in cytosolic and particulate fractions from rat forebrain J Neurochem. 62, 1552–1559.
Simpson, C. S., and Morris, B. J. (1995) Induction of c-fos and zif/268 gene expression in rat striatal neurons, following stimulation of D1-like dopamine receptors, involves protein kinase A and protein kinase Neuroscience 68, 97–106.
Sitges, M., Dunkley, P. R., and Chiu, L. M. (1995) A role for calcium/ calmodulin kinase(s) in the regulation of GABA exocytosis. Neurochem. Res 20, 245–252.
Smith, M. K., Colbran, R. J., and Soderling, T. R. (1990) Specificities of autoinhibitory domain peptides for four protein kinases: implications for intact cell studies of protein kinase function. J Biol Chem 265, 1837–1840.
Smith, M. K., Colbran, R. J., Brickey, D. A., and Soderling, T. R (1992) Functional determinants in the autoinhibitory domain of calcium/ calmodulin-dependent protein kinase II-role of His282 and multiple basic residues. J Biol Chem. 267, 1761–1768.
Snell, L D. Iorio, K. R., Tabakoff, B, and Hoffman, P. L. (1994) Protein kinase activation attenuates N-methyl-D-aspartate-induced increases in intracellular calcium in cerebellar granule cells J Neurochem. 62, 1783–1789
Soderling, T R. (1990) Protein kinases: regulation by autoinhibitory domains. J Biol. Chem 265, 1823–1826
Stone, R. L. and Dixon, J. E. (1994) Protein-tyrosine phosphatases. J Biol Chem. 269, 31,323–31,326.
Sullivan, J. A., Merritt, J. E., Budd, J. M., Booth, R. F., and Hallam, T J. (1994) Effect of a selective protein kinase inhibitor, Ro 31-8425, on Mac-1 expression and adhesion of human neutrophils. Eur J Immunol 24, 621–626
Sullivan, J. P., Connor, J. R., Tiffany, C, Shearer, B. G., and Burch, R. M. (1991) NPC 15437 interacts with the C1 domain of protein kinase An analysis using mutant PKC constructs. FEBS Lett 285, 120–123
Sullivan, J. P., Connor, J R, Shearer, B. G., and Burch, R. M. (1992) 2,6-Diamino-N-([1-(1-oxotndecyl)-2-pipendinyl] methyDhexanamide (NPC 15437): a novel inhibitor of protein kinase interacting at the regulatory domain. Mol Pharmacol 41, 38–44.
Sumi, M., Kiuchi, K., Ishikawa, T, Ishii, A, Hagiwara, M, Nagatsu, T, and Hidaka, H. (1991) The newly synthesized selective Ca2+/calmodulin-dependent protein kinase II inhibitor KN-93 reduces dopamine contents in PC12h cells. Biochem Biophys Res Commun 181, 968–975.
Surmeier, D. J., Bargas, J., Hemmings, H. C., Jr, Nairn, A.C., and Greengard, P. (1995) Modulation of calcium currents by a D1 dopaminergic protein kinase/phosphatase cascade in ratneostriatal neurons. Neuron 14, 385–397.
Takano, K., Stanfield, P. R, Nakajima, S, and Nakajima, Y. (1995) Protein kmase C-mediated inhibition of an inward rectifier potassium channel by substance P in nucleus basalis neurons. Neuron 14, 999–1008.
Tamaoki, T. (1991) Use and specificity of staurosporine, UCN-01, and calphostin as protein kinase inhibitors. Methods Enzymol 201, 340–347.
Tan, S.-E., Wenthold, R. J., and Soderling, T R (1994) Phsophorylation of AMPA-type glutamate receptors by calcium / calmodulin-dependent protein kinase II and protein kinase in cultured hippocampal neurons. J. Neurosci 14, 1123–1129
Tanaka, C., and Nishizuka, Y. (1994) The protein kinase family for neuronal signaling. Ann. Rev Neurosci. 17, 551–567.
Tanaka, H., Katagiri, M., Arima, S, Matsuzaki, K., Inokoshi, J., and Omura, S. (1995) Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid. Biochem Biophys Res. Commun 216, 291–297.
Tansey, M. G., Luby-Phelps, K., Kamm, K. E., and Stull, J. T. (1994) Ca2+-dependent phosphorylation of myosin light chain kinase decreases the Ca2+ sensitivity of light chain phosphorylation within smooth muscle cells. J. iol Chem 269, 9912–9920.
Teng, K. K. and Greene, L. A (1994) KT5926 selectively inhibits nerve growth factor-dependent neurite elongation. J. Neurosa. 14, 2624–2635.
Terbush, D. R. and Holz, R. W. (1990) Activation of protein kinase is not required for exocytosis from bovine adrenal chromaffin cells. The effects of protein kinase–31), Ca/CaM kinase II(291-317), and staurosporine. J Biol Chem. 265, 21,179–21,184.
Tokimasa, T., Ito, M., Simmons, M. A., Schneider, C. R., Tanaka, T., Nakano, T., and Akasu, T. (1995) Inhibition by wortmannin of M-current in bullfrog sympathetic neurones. Br J. Pharmacol. 114, 489–495
Tokumitsu, H., Chijiwa, T., Hagiwara, M., Mizutani, A., and Terasawa, M. (1990) KN-62, 1-(N,O-Bis[5-isoquinolinesulfonyl]-N-methyl-L-tyrosyl]-4-phenylpiperazine, a specific inhibitor of Ca2+/ calmodulin-dependent protein kinase II.J Biol Chem 265, 4315–4320
Tong, G. and Jahr, C.E., (1994) Regulation of glycine-insensitive desen-sitization of the NMDA receptor in outside-out patches. J Neurophysiol. 72, 754–761.
Torii, N., Kamishita, T, Otsu, Y, and Tsumoto, T. (1995) An inhibitor for calcineurin, FK506, blocks induction of long-term depression in rat visual cortex. Neurosci. Lett. 185, 1–4.
Toullec, D., Pianetti, P., Coste, H., Bellevergue, P., Grand-Perret, T, Ajakane, M., Baudet, V., Boissin, P., Boursier, E, Loriolle, F, Duhamel, L., Charon, D., and Kirilovsky, J. (1991) The bis-indolylmaleimide GF 109203X is a potent and selective inhibitor of pro-tein kinase J. Biol Chem. 266, 15,771–15,781.
Ueda, H., Miyamae, T., Hayashi, C., Watanabe, S., Fukushima, N., Sasaki, Y., Iwamura, T., and Misu, Y. (1995) Protein kinase involvement in homologous desensitization of 5-opioid receptor coupled to G11-phospholipase activation in Xenopus oocytes. J. Neurosa. 15, 7485–7499.
Uehara, Y. and Fukazawa, H. (1991) Use and selectivity of herbimycin A as inhibitor of protein-tyrosine kinases. Methods Enzymol 201, 370–379.
Uehara, Y., Fukazawa, H., Murakami, Y., and Mizuno, S. (1989) Irreversible inhibition of v-src tyrosine kinase activity by herbimycin A and its abrogation by sulfhydryl compounds. Biochem Biophys Res. Commun. 163, 803–809.
Umezawa, K. and Imoto, M. (1991) Use of erbstatin as protein-tyrosine kinase inhibitor. Methods Enzymol. 201, 379–385.
Umezawa, K., Hori, T., Tajima, H., Imoto, M, Isshiki, K., and Takeuchi, T. (1990) Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors. FEBS Lett. 260, 198–200.
Umezawa, K, Sugata, D., Yamashita, K., Johtoh, N., and Shibuya, M. (1992) Inhibition of epidermal growth factor receptor functions by tyrosine kinase inhibitors in NIH3T23 cells FEBS Lett 314, 289–292.
Valenzuela, F., Machu, K., McKernan, R. M., Whiting, P., Van Renterghem, B.B., McManaman, J. L, Brozowski, S. J, Smith, G Olsen, R. W., and Harris, R. A. (1995) Tyrosine kinase phosphorylation of GABA a receptors Mol Brain Res 31, 165–172.
Vera, J. C, Reyes, A. M., Cádrcamo, J. G., Velásquez, F V., Rivas, I, Zhang, R. H., Strobel, P, Iribarren, R., Scher, H. I., Slebe, J C, and Golde, D. W. (1996) Genistin is a natural inhibitor of hexose and dehydroascorbic acid transport through the glucose transporter, GLUT1. J Biol Chem. 271, 8719–8724.
Veselý, J., Havlicek, L, Strnad, M., Blow, J J., Donella-Deana, A., Pinna, L, Letham, D S, Kato, J-Y, Detivaud, L, Leclerc, S., and Meijer, L (1994) Inhibition of cyclin-dependent kmases by purine analogues. Eur J. Biochem 224, 771–786
Vickroy, T W., Malphurs, W. L., and Carriger, M L (1995) Regulation of stimulus-dependent hippocampal acetylcholine release by okadaic acid-sensitive phosphoprotein phosphatases Neurosci Lett 191, 200–204.
Victor, R. G, Thomas, G. D., Marban, E, and O’Rourke, B., (1995) Pre-synaptic modulation of cortical synaptic activity by calcmeurin. Proc Natl Acad. Sci USA 92, 6269–6273
Walaas, S. I. and Greengard, P. (1991) Protein phosphorylation and neu-ronal function Pharmacol. Rev 43, 299–349
Walker, D. L. and Gold, P. E. (1994) Intra-amygdala kinase inhibitors disrupt retention of a learned avoidance response in rats. Neurosci Lett 176, 255–258.
Walsh, D. A. and Glass, D. B. (1991) Utilization of the inhibitor protein of adenosine cyclic monophosphate-dependent protein kinase, and peptides derived from it, as tools to study adenosine cyclic monophosphate-mediated cellular processes. Methods Enzymol 201, 304–316.
Walterova, D., Ulrichova, Preininger, V, Simanek, V., Lenfeld, J, and Lasovsky, J. (1981) Inhibition of liver alanine aminotransferase activity by some benzophenanthridine alkaloids. J. Med Chem 24, 1100–1103.
Wang, J-H. and Feng, D P. (1992) Postsynaptic protein kinase essential to induction and maintenance of long-term potentiation in the hippocampal CA1 region. Proc Natl. Acad. Sci. USA 89, 2576–2580.
Wang, J.-H. and Kelly, P. T. (1995) Postsynaptic injection of Ca2+JCaM induces synaptic potentiation requiring CaMKII and PKC activity Neuron 15, 443–452.
Wang, L.-Y., Dudek, E. M., Browning, M.D., and MacDonald, J F (1994a) Modulation of AMPAJkainate receptors in cultured murine hippocampal neurones by protein kinase C. J Physiol. 475, 431–437.
Wang, L.-Y., Orser, A., Brautigan, D. L., and MacDonald, J. F. (1994b) Regulation of NMDA receptors in cultured hippocampal neurons by protein phosphatases 1 and 2A. Nature 369, 230–232.
Wang, L.-Y, Salter, M. W., and MacDonald, J. F. (1991) Regulation of kainate receptors by cAMP-dependent protein kinase and phosphatases. Science 253, 1132–1135.
Wang, S. S, Mathes, C, and Thompson, S. H. (1993) Membrane toxicity of the protein kinase inhibitor calpohostin A by a free-radical mechanism. Neurosci Lett 157, 25–28.
Wang, Y.-T. and Salter, M. W. (1994) Regulation of NMDA receptors by tyrosine kinases and phosphatases. Nature 369, 233–235.
Wenham, R. M., Landt, M., Walters, S. M., Hidaka, H., and Easom, R. A. (1992) Inhibition of insulin secretion by KN-62, a specific inhibitor of the multifunctional Ca2+Jcalmodulin-dependent protein kinase II. Biochem. Biophys Res. Commun. 189, 128–133.
Wenzel-Seifert, K., Scháchtele, C., and Seifert, R. (1994) N-Protein kinase isoenzymes may be involved in the regulation of various neutrophil functions. Biochem Biophys Res Commun. 200, 1536–1543
Wera, S and Hemmings, B.A., (1995) Serine / threonine protein phos-phatases. Biochem J. 311, 17–29.
Wetsel, W. C, Eraly, S. A., Whyte, D. and Mellon, P. L. (1993) Regula-tion of gonadotropin-releasing hormone by protein kinase-A and-C in immortalized hypothalamic neurons. Endocrinology 132, 2360–2370
Wiechen, K., Yue, D. T., and Herzig, S. (1995) Two distinct functional effects of protein phosphatase inhibitors on guinea-pig cardiac L-type Ca2+channels. J. Physiol. 484, 583–592.
Wijetunge, S, Aalkjaer, C., Schachter, M., and Hughes, A. D. (1992) Tyro-sine kinase inhibitors block calcium channel currents in vascular smooth muscle cells. Biochem Biophys. Res. Commun. 189, 1620–1623.
Wilkinson, S. E., Parker, P. J., and Nixon, J. S. (1993) Isoenzyme specific-ity of bismdolylmaleimides, selective inhibitors of protein kinase Biochem J. 294, 335–337.
Williams, E. J., Walsh, F. S., and Doherty, P. (1994) Tyrosine kinase inhibi-tors can differentially inhibit integrin-dependent and CAM-stimulated neurite outgrowth. J Cell Biol. 124, 1029–1037.
Wolbring, G., Hollenberg, M D., and Schnetkamp, P. P M. (1994) Inhi-bition of GTP-utilizing enzymes by tyrphostins. J Biol Chem. 269, 22,470–22,472
Worland, P. J., Stetler-Stevenson, M, Sebers, S., Sartor, O., and Sausville, E. A. (1993) Alteration of the phosphorylation state of p34edc2 kinase by the flavone L86-8275 in breast carcinoma cells. Correlation with decreased H1 kinase activity. Biochem. Pharmacol 46, 1831–1840.
Wu, Y. N. and Wagner, P. D. (1991) Effects of phosphatase inhibitors and a protein phosphatase on norepinephrine secretion by permeabilized bovine chromaffin cells. Biochim Biophys. Acta 1092, 384–390.
Wyllie, D. J A and Nicoll, R. A (1994) A role for protein kinases and phosphatases in the Ca2+-induced enhancement of hippocampal AMPA receptor-mediated synaptic responses. Neuron 13, 635–643
Yan, X., Corbin, J. D., Francis, S. H, and Lawrence, D. S (1996) Preci-sion trageting of protein kinases: an affinity label that inactivates the cGMP-but not the cAMP-dependent protein kinase. J Biol Chem 271, 1845–1848.
Yang, J. and Tsien, R W. (1993) Enhancement of N-and L-type calcium channel currents by protein kinase in frog sympathetic neurons Neuron 10, 127–136
Yashpal, K., Pitcher, G. M., Parent, A., Quirion, R., and Coderre, T. J (1995) Noxious thermal and chemical stimulation induce increases in 3H-phorbol 12,13-dibutyrate binding in spinal cord dorsal horn as well as persistent pain and hyperalgesia, which is reduced by inhibition of protein kinase J Neurosci 15, 3263–3272.
Zirrgiebel, U, Ohga, Y., Carter, B., Berninger, B., Inagaki, N, Thoenen, H., and Lindholm, D (1995) Characterization of TrkB receptormediated signaling pathways in rat cerebellar granule neurons · involvement of protein kinase in neuronal survival. J Neurochem 65, 2241–2250.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1997 Humana Press Inc.
About this protocol
Cite this protocol
Hemmings, H.C. (1997). Protein Kinase and Phosphatase Inhibitors. In: Hemmings, H.C. (eds) Regulatory Protein Modification. Neuromethods, vol 30. Humana Press. https://doi.org/10.1385/0-89603-415-1:121
Download citation
DOI: https://doi.org/10.1385/0-89603-415-1:121
Publisher Name: Humana Press
Print ISBN: 978-0-89603-415-0
Online ISBN: 978-1-59259-635-5
eBook Packages: Springer Protocols