Peptide Research Protocols pp 181-198 | Cite as
Characterization of a New Endothelin Receptor Ligand by In Vitro Assays
- 401 Downloads
Abstract
Following the discovery of endothelin (1), functional characterization of the three endothelin (ET) isoforms (ET-1, ET-2 and ET-3) predicted that two mammalian receptor subtypes are present: the ETA receptor that is selective for ET-1, and the ETB receptor that has equal affinity for the three isoforms (2). The existence of the two distinct high-affinity ET receptor subtypes has been confirmed by cloning. Unique cDNAs that code for ETA and ETB belonging to the G-protein linked heptahelical receptor superfamily are identified in human, bovine and rat tissues (3, 4, 5, 6). While pharmacological studies suggest that there may be more ET receptor subtypes (7), no additional homologous mammalian cDNAs have been identified.
Keywords
Binding Study Test Agent Arachidonic Acid Release Receptor Binding Study Coronary Artery Smooth Muscle CellReferences
- 1.Yanagisawa M., Kurihara H., Kimura S., Tomobe Y., Kobayashi M., Mitsui Y., et al. (1988) A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 332, 411–414.PubMedCrossRefGoogle Scholar
- 2.Opgenorth T. J. (1995) Endothelin receptor antagonism. Adv. Pharmacol. 33, 1–65.PubMedCrossRefGoogle Scholar
- 3.Arai H., Hori S., Aramori I., Ohkubo H., and Nakanishi S. (1990) Cloning and expression of a cDNA encoding an ET receptor. Nature 348, 730–732.PubMedCrossRefGoogle Scholar
- 4.Sakurai T., Yanagisawa M., Takuwa Y., Miyazaki H., Kimura S., Goto K., and Masaki T. (1990) Cloning of a cDNA encoding a nonisopeptide-selective subtype of the endothelin receptor. Nature 348, 732–735.PubMedCrossRefGoogle Scholar
- 5.Arai H., Nakao K., Takaya K., Hosoda K., Ogawa Y., Nakanishi S., and Imura H. (1993) The human endothelin-B receptor gene. J. Biol. Chem. 268, 3463–3470.PubMedGoogle Scholar
- 6.Elshourbagy N. A., Korman D. R., Wu H.-L., Sylvester D. R., Lee J. A., Nuthalaganti P., et al. (1993) Molecular characterization and regulation of the human endothelin receptors. J. Biol. Chem. 268, 3873–3879.PubMedGoogle Scholar
- 7.Bax W. and Saxena P. (1994) The current endothelin receptor classification: time for reconsideration? Trends Pharmacol. Sci. 15, 379–386.PubMedCrossRefGoogle Scholar
- 8.Simonson M. S. (1993) Endothelins: Multifunctional renal peptides. Physiol. Rev. 73, 375–411.PubMedGoogle Scholar
- 9.Wu-Wong J. R. and Opgenorth T. J. (2002) The roles of endothelins in proliferation, apoptosis, and angiogenesis. Handbook of Experimental Pharmacology, in press.Google Scholar
- 10.Wu-Wong J. R. and Opgenorth T. J. (1998) Endothelin and isoproterenol counter-regulate cAMP and mitogen-activated protein kinases. J. Cardiovasc. Pharmacol. 31, S185–S191.PubMedCrossRefGoogle Scholar
- 11.Wu-Wong J. R., Chiou W., Dickinson R. and Opgenorth T. J. (1997) Endothelin attenuates apoptosis in human smooth muscle cells. Biochem. J. 28, 733–737.Google Scholar
- 12.Shichiri M., Kato H., Marumo F., and Hirata Y. (1998) Endothelin-B receptormediated suppression of endothelial apoptosis. J. Cardiovasc. Pharmacol. 31, S138–S141.PubMedCrossRefGoogle Scholar
- 13.Webb D. J., Monge J. C., Rabelink T. J., and Yanagisawa M. (1998) Endothelin: new discoveries and rapid progress in the clinic. Trends Pharmacol. Sci. 19, 5–8.PubMedCrossRefGoogle Scholar
- 14.Ihara M., Noguchi K., Saeki T., Fukuroda T., Tsuchida S., Kimura S., et al. (1991) Biological profile of highly potent novel endothelin antagonists selective for the ETA receptor. Life Sci. 50, 247–255.CrossRefGoogle Scholar
- 15.Sogabe K., Nirei H., Shoubo M., Nomoto A., Ao S., Notsu T., and Ono T. (1993) Pharmacological profile of FR139317, a novel, potent, endothelin ETA receptor antagonist. J. Pharmacol. Exp. Ther. 264, 1040–1046.PubMedGoogle Scholar
- 16.Opgenorth T. J., Adler A. L., Calzadilla S., Chiou W. J., Dayton B. D., Dixon D. B., et al. (1996) Pharmacological Characterization of A-127722: An orally active and highly potent ETA-selective receptor antagonist. J. Pharmacol. Exp. Ther. 276, 473–481.PubMedGoogle Scholar
- 17.Wu-Wong J. R., Dixon D. B., Chiou W. J., Dayton B. D., Novosad E. I., Adler A. L., et al. (1999) Pharmacology of A-216546: A Highly Selective Antagonist for The Type-A Endothelin Receptor. Eur. J. Pharmacol. 366, 189–201.PubMedCrossRefGoogle Scholar
- 18.Chiou W., Magnuson S. R., Dixon D. B., Sundy S., Opgenorth T. J., and Wu-Wong J. R. (1997) Dissociation characteristics of endothelin receptor agonists and antagonists in cloned human type-B endothelin receptor. Endothelium: J. Endothelial Cell Res. 5, 179–189.Google Scholar
- 19.Wu-Wong J. R., Chiu W., Magnuson J. R., Bianchi B. R., and Lin C. W. (1996) Human astrocytoma U138MG cells express predominantly type-A endothelin receptors. Biochem. Biophys. Acta 1311, 155–163.PubMedCrossRefGoogle Scholar
- 20.Wu-Wong J. R., Chiou W., Magnuson S. R., and Opgenorth T. J. (1995) Endothelin Receptor in Human Astrocytoma U373MG Cells: Binding, Dissociation, Receptor Internalization. J. Pharmacol. Exp. Ther. 274, 499–507.PubMedGoogle Scholar
- 21.Wu-Wong J. R., Chiou W., Magnuson S. R., and Opgenorth T. J. (1994) Endothelin receptor agonists and antagonists exhibit different dissociation characteristics. Biochem. Biophys. Acta 1224, 288–294.PubMedCrossRefGoogle Scholar
- 22.Chiou W. J., Wang J., Berg C. E., and Wu-Wong J. R. (1999) SV40 virus transformation down-regulates endothelin receptor. Biochem. Biophys. Acta 1450, 35–44.PubMedCrossRefGoogle Scholar
- 23.Wu-Wong J. R., Berg C. E., Wang J., Chiou W. J., and Fissel B. (1999) Endothelin Stimulates Glucose Uptake and GLUT4 Translocation Via Activation of Endothelin ETA Receptor in 3T3-L1 Adipocytes. J. Biol. Chem. 274, 8103–8110.PubMedCrossRefGoogle Scholar
- 24.Wu-Wong J. R., Chiou W., and Opgenorth T. J. (1993) Phosphoramidon modulates the number of endothelin receptors in cultured Swiss 3T3 fibroblasts. Mol. Pharmacol. 44, 422–429.PubMedGoogle Scholar
- 25.Wu-Wong J. R., Chiou W., Magnuson S. R., Witte D. G., and Lin C. W. (1993) Identification and characterization of type A endothelin receptor in MMQ cells. Mol. Pharmacol. 44, 285–291.PubMedGoogle Scholar
- 26.Nelson J. B., Hedican S. P., George D. J., Reddi A. H., Piantadosi S., Eisenberger M. A., and Simons J. W. (1995) Identification of endothelin-1 in the pathophysiology of metastatic adenocarcinoma of the prostate. Nature Med. 1, 944–949.PubMedCrossRefGoogle Scholar
- 27.Tsukahara H., Ende H., Magazine H. I., Bahou W. F., and Goligorsky M. S. (1994) Molecular and functional characterization of the nonisopeptide-selective ETB receptor in endothelial cells. Receptor coupling to nitric oxide synthase. J. Biol. Chem. 269, 21,778–21,785.PubMedGoogle Scholar
- 28.Morbidelli L., Orlando C., Maggi C. A., Ledda F., and Ziche M. (1995) Proliferation and migration of endothelial cells is promoted by endothelins via activation of ETB receptors. Am. J. Physiol. 269, H686–H695.PubMedGoogle Scholar
- 29.Lahav R., Heffner G., and Patterson P. H. (1999) An endothelin receptor B antagonist inhibits growth and induces cell death in human melanoma cells in vitro and in vivo. Proc. Natl. Acad. Sci. 96, 11496–11500.PubMedCrossRefGoogle Scholar
- 30.Bagnato A., Tecce R., Di Castro V., and Catt K. J. (1997) Activation of mitogenic signaling by endothelin 1 in ovarian carcinoma cells. Cancer Res. 57, 1306–1311.PubMedGoogle Scholar
- 31.Wu-Wong J. R., Chiou W., Huang Z.-J., Vidal M. J., and Opgenorth T. J. (1994) Endothelin receptor in human pericardium smooth muscle cells: antagonist potency differs on agonist-evoked responses. Amer. J. Physiol. 267, C1185–C1195.PubMedGoogle Scholar
- 32.Oriji G. K. (1999) Endothelin-induced prostacyclin production in rat aortic endothelial cells is mediated by protein kinase C. Prostaglandins Leukot. Essent. Fatty Acids 60, 263–268.CrossRefGoogle Scholar
- 33.Cioffi C. L. and Garay M. (1993) Short-term regulation of endothelin receptormediated phosphoinositide hydrolysis and arachidonic acid release in A7r5 smooth-muscle cells. J. Cardiovasc. Pharmacol. 22, S168–S170.PubMedCrossRefGoogle Scholar
- 34.Vigne P. and Frelin C. (1994) Endothelins activate phospholipase A2 in brain capillary endothelial cells. Brain Res. 651, 342–344.PubMedCrossRefGoogle Scholar
- 35.Yousufzai S. Y. and Abdel-latif A. A. (1997) Endothelin-1 stimulates the release of arachidonic acid and prostaglandins in cultured human ciliary muscle cells: activation of phospholipase A2. Exp. Eye Res. 65, 73–81.PubMedCrossRefGoogle Scholar
- 36.Abdel-Latif A. A., Husain S., and Yousufzai S. Y. (2000) Role of protein kinase C alpha and mitogen-activated protein kinases in endothelin-1-stimulation of cytosolic phospholipase A2 in iris sphincter smooth muscle. J. Cardiovasc. Pharmacol. 36, S117–S119.PubMedGoogle Scholar
- 37.Suzuki A., Shinoda J., Watanabe-Tomita Y., Ozaki N., Oiso Y., and Kozawa O. (1997) ETA receptor mediates the signaling of endothelin-1 in osteoblast-like cells. Bone 21, 143–146.PubMedCrossRefGoogle Scholar
- 38.Wu-Wong J. R., Dayton B. D., and Opgenorth T. J. (1996) Endothelin-1-evoked arachidonic acid release: a Ca(2+)-dependent pathway. Am. J. Physiol. 271, C869–C877.PubMedGoogle Scholar
- 39.Ishikawa K., Ihara M., Noguchi K., Mase T., Mino N., Saeki T., et al. (1994) Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc. Natl. Acad. Sci. 91, 4892–4896.PubMedCrossRefGoogle Scholar