Skip to main content

Memapsin 2

  • Chapter
Class 3 Hydrolases

Part of the book series: Springer Handbook of Enzymes ((HDBKENZYMES,volume S6))

  • 649 Accesses

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 259.00
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 329.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 329.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Ghosh, A.K.; Bilcer, G.; Harwood, C.; Kawahama, R.; Shin, D.; Hussain, K.A.; Hong, L.; Loy, J.A.; Nguyen, C.; Koelsch, G.; Ermolieff, J.; Tang, J.: Structure-based design: potent inhibitors of human brain memapsin 2 (β-secretase). J. Med. Chem., 44, 2865–2868 (2001)

    Article  PubMed  CAS  Google Scholar 

  2. Turner, R.T.; III; Loy, J.A.; Nguyen, C.; Devasamudram, T.; Ghosh, A.K.; Koelsch, G.; Tang, J.: Specificity of memapsin 1 and its implications on the design of memapsin 2 (β-secretase) inhibitor selectivity. Biochemistry, 41, 8742–8746 (2002)

    Article  PubMed  CAS  Google Scholar 

  3. Turner, R.T.; Koelsch, G.; Hong, L.; Castenheira, P.; Ghosh, A.; Tang, J.: Subsite specificity of memapsin 2 (b-secretase): implications for inhibitor design. Biochemistry, 40, 10001–10006 (2001)

    Article  PubMed  CAS  Google Scholar 

  4. Hong, L.; Turner, R.T.; Koelsch, G.; Shin, D.; Ghosh, A.K.; Tang, J.: Crystal structure of memapsin 2 (b-secretase) in complex with an inhibitor 0M00-3. Biochemistry, 41, 10963–10967 (2002)

    Article  PubMed  CAS  Google Scholar 

  5. Kennedy, M.E.; Wang, W.; Song, L.; Lee, J.; Zhang, L.; Wong, G.; Wang, L.; Parker, E.: Measuring human β-secretase (BACE1) activity using homogeneous time-resolved fluorescence. Anal. Biochem., 319, 49–55 (2003)

    Article  PubMed  CAS  Google Scholar 

  6. Hong, L.; Koelsch, G.; Lin, X.; Wu, S.; Terzyan, S.; Ghosh, A.K.; Zhang, X.C.; Tang, J.: Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor. Science, 290, 150–153 (2000)

    Article  PubMed  CAS  Google Scholar 

  7. Roggo, S.: Inhibition of BACE, a promising approach to Alzheimer’s disease therapy. Curr. Top. Med. Chem., 2, 359–370 (2002)

    Article  PubMed  CAS  Google Scholar 

  8. Ghosh, A.K.; Hong, L.; Tang, J.: β-Secretase as a therapeutic target for inhibitor drugs. Curr. Med. Chem., 9, 1135–1144 (2002)

    PubMed  CAS  Google Scholar 

  9. Ermolieff, J.; Loy, J.A.; Koelsch, G.; Tang, J.: Proteolytic activation of recombinant pro-memapsin 2 (pro-β-secretase) studied with new fluorogenic substrates. Biochemistry, 39, 12450–12456 (2000)

    Article  PubMed  CAS  Google Scholar 

  10. Ehehalt, R.; Michel, B.; De Pietri Tonelli, D.; Zacchetti, D.; Simons, K.; Keller, P.: Splice variants of the β-site APP-cleaving enzyme BACE1 in human brain and pancreas. Biochem. Biophys. Res. Commun., 293, 30–37 (2002)

    Article  PubMed  CAS  Google Scholar 

  11. Luo, Y.; Bolon, B.; Damore, M.A.; Fitzpatrick, D.; Liu, H.; Zhang, J.; Yan, Q.; Vassar, R.; Citron, M.: BACE1 (β-secretase) knockout mice do not acquire compensatory gene expression changes or develop neural lesions over time. Neurobiol. Dis., 14, 81–88 (2003)

    Article  PubMed  CAS  Google Scholar 

  12. Yan, R.; Han, P.; Miao, H.; Greengard, P.; Xu, H.: The transmembrane domain of the Alzheimer’s β-secretase (BACE1) determines its late Golgi localization and access to β-amyloid precursor protein (APP) substrate. J. Biol. Chem., 276, 36788–36796 (2001)

    Article  PubMed  CAS  Google Scholar 

  13. Puglielli, L.; Ellis, B.C.; Saunders, A.J.; Kovacs, D.M.: Ceramide stabilizes β-site amyloid precursor protein-cleaving enzyme 1 and promotes amyloid β-peptide biogenesis. J. Biol. Chem., 278, 19777–19783 (2003)

    Article  PubMed  CAS  Google Scholar 

  14. Kitazume, S.; Tachida, Y.; Oka, R.; Kotani, N.; Ogawa, K.; Suzuki, M.; Dohmae, N.; Takio, K.; Saido, T.C.; Hashimoto, Y.: Characterization of α 2,6-sialyltransferase cleavage by Alzheimer’s β-secretase (BACE1). J. Biol. Chem., 278, 14865–14871 (2003)

    Article  PubMed  CAS  Google Scholar 

  15. Tomasselli, A.G.; Qahwash, I.; Emmons, T.L.; Lu, Y.; Leone, J.W.; Lull, J.M.; Fok, K.F.; Bannow, C.A.; Smith, C.W.; Bienkowski, M.J.; Heinrikson, R.L.; Yan, R.: Employing a superior BACE1 cleavage sequence to probe cellular APP processing. J. Neurochem., 84, 1006–1017 (2003)

    Article  PubMed  CAS  Google Scholar 

  16. Bruinzeel, W.; Yon, J.; Giovannelli, S.; Masure, S.: Recombinant insect cell expression and purification of human β-secretase (BACE-1) for X-ray crystallography. Protein Expr. Purif., 26, 139–148 (2002)

    Article  PubMed  CAS  Google Scholar 

  17. Beckman, M.; Holsinger, R.M.; Small, D.H.: Heparin activates β-secretase (BACE1) of Alzheimers disease and increases autocatalysis of the enzyme. Biochemistry, 45, 6703–6714 (2006)

    Article  PubMed  CAS  Google Scholar 

  18. Kimura, T.; Hamada, Y.; Stochaj, M.; Ikari, H.; Nagamine, A.; Abdel-Rahman, H.; Igawa, N.; Hidaka, K.; Nguyen, J.T.; Saito, K.; Hayashi, Y.; Kiso, Y.: Design and synthesis of potent β-secretase (BACE1) inhibitors with P1 carboxylic acid bioisosteres. Bioorg. Med. Chem. Lett., 16, 2380–2386 (2006)

    Article  PubMed  CAS  Google Scholar 

  19. von Arnim, C.A.; Kinoshita, A.; Peltan, I.D.; Tangredi, M.M.; Herl, L.; Lee, B.M.; Spoelgen, R.; Hshieh, T.T.; Ranganathan, S.; Battey, F.D.; Liu, C.X.; Bacskai, B.J.; Sever, S.; Irizarry, M.C.; Strickland, D.K.; Hyman, B.T.: The low density lipoprotein receptor-related protein (LRP) is a novel β-secretase (BACE1) substrate. J. Biol. Chem., 280, 17777–17785 (2005)

    Article  Google Scholar 

  20. Angeletti, B.; Waldron, K.J.; Freeman, K.B.; Bawagan, H.; Hussain, I.; Miller, C.C.; Lau, K.F.; Tennant, M.E.; Dennison, C.; Robinson, N.J.; Dingwall, C.: BACE1 cytoplasmic domain interacts with the copper chaperone for superoxide dismutase-1 and binds copper. J. Biol. Chem., 280, 17930–17937 (2005)

    Article  PubMed  CAS  Google Scholar 

  21. Wong, H.K.; Sakurai, T.; Oyama, F.; Kaneko, K.; Wada, K.; Miyazaki, H.; Kurosawa, M.; De Strooper, B.; Saftig, P.; Nukina, N.: β Subunits of voltage-gated sodium channels are novel substrates of β-site amyloid precursor protein-cleaving enzyme (BACE1) and γ-secretase. J. Biol. Chem., 280, 23009–23017 (2005)

    Article  PubMed  CAS  Google Scholar 

  22. Yang, H.C.; Chai, X.; Mosior, M.; Kohn, W.; Boggs, L.N.; Erickson, J.A.; McClure, D.B.; Yeh, W.K.; Zhang, L.; Gonzalez-DeWhitt, P.; Mayer, J.P.; Martin, J.A.; Hu, J.; Chen, S.H.; Bueno, A.B.; Little, S.P.; McCarthy, J.R.; May, P.C.: Biochemical and kinetic characterization of BACE1: investigation into the putative species-specificity for β-and β-cleavage sites by human and murine BACE1. J. Neurochem., 91, 1249–1259 (2004)

    Article  PubMed  CAS  Google Scholar 

  23. Rossner, S.; Lange-Dohna, C.; Zeitschel, U.; Perez-Polo, J.R.: Alzheimers disease β-secretase BACE1 is not a neuron-specific enzyme. J. Neurochem., 92, 226–234 (2005)

    Article  PubMed  CAS  Google Scholar 

  24. Laird, F.M.; Cai, H.; Savonenko, A.V.; Farah, M.H.; He, K.; Melnikova, T.; Wen, H.; Chiang, H.C.; Xu, G.; Koliatsos, V.E.; Borchelt, D.R.; Price, D.L.; Lee, H.K.; Wong, P.C.: BACE1, a major determinant of selective vulnerability of the brain to amyloid-β amyloidogenesis, is essential for cognitive, emotional, and synaptic functions. J. Neurosci., 25, 11693–11709 (2005)

    Article  PubMed  CAS  Google Scholar 

  25. Zuechner, T.; Perez-Polo, J.R.; Schliebs, R.: β-Secretase BACE1 is differentially controlled through muscarinic acetylcholine receptor signaling. J. Neurosci. Res., 77, 250–257 (2004)

    Article  CAS  Google Scholar 

  26. Hattori, C.; Asai, M.; Onishi, H.; Sasagawa, N.; Hashimoto, Y.; Saido, T.C.; Maruyama, K.; Mizutani, S.; Ishiura, S.: BACE1 interacts with lipid raft proteins. J. Neurosci. Res., 84, 912–917 (2006)

    Article  PubMed  CAS  Google Scholar 

  27. Harada, H.; Tamaoka, A.; Ishii, K.; Shoji, S.; Kametaka, S.; Kametani, F.; Saito, Y.; Murayama, S.: β-site APP cleaving enzyme 1 (BACE1) is increased in remaing neurons in Alzheimers disease brains. Neurosci. Res., 54, 24–29 (2006)

    Article  PubMed  CAS  Google Scholar 

  28. Sardana, V.; Xu, B.; Zugay-Murphy, J.; Chen, Z.; Sardana, M.; Darke, P.L.; Munshi, S.; Kuo, L.C.: A general procedure for the purification of human β-secretase expressed in Escherichia coli. Protein Expr. Purif., 34, 190–196 (2004)

    Article  PubMed  CAS  Google Scholar 

  29. Willem, M.; Garratt, A.N.; Novak, B.; Citron, M.; Kaufmann, S.; Rittger, A.; Destrooper, B.; Saftig, P.; Birchmeier, C.; Haass, C.: Control of peripheral nerve myelination by the β-secretase BACE1. Science, 314, 664–666 (2006)

    Article  PubMed  CAS  Google Scholar 

Download references

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2009 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

(2009). Memapsin 2. In: Chang, A. (eds) Class 3 Hydrolases. Springer Handbook of Enzymes, vol S6. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-85705-1_24

Download citation

Publish with us

Policies and ethics