Structure-based subsite specificity mapping of human cathepsin D using statine-based inhibitors

Protein Science

Volumn 6, Issue 7, 1997, Pages 1458-1466

  Majer, Pavel ^a   Collins, Jack R ^a   Gulnik, Sergei V ^a   Erickson, John W ^a  

^a NATIONAL CANCER INSTITUTE   (United States)

Author keywords

Human cathepsin D; Inhibitors; Statine; Structure based design

Indexed keywords

ASPARTIC PROTEINASE; CATHEPSIN D; ENZYME INHIBITOR; LYSOSOME ENZYME; PEPSTATIN; STATINE DERIVATIVE;

ARTICLE; ENZYME INHIBITION; ENZYME STRUCTURE; HUMAN; MOLECULAR MODEL; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

EID: 0030855215     PISSN: 09618368     EISSN: None     Source Type: Journal    
DOI: 10.1002/pro.5560060710     Document Type: Article

References (20)

1. Agarwal NS, Rich DH. 1986. Inhibition of cathepsin D by substrate analogues containing staline and by analogues of pepstatin. J Med Chem 29:2519-2524.
2. Baldwin ET, Bhat TN, Gulnik S, Hosur MV, Sowder RC II, Cachau RE, Collins J, Silva AM, Erickson J. 1993. Crystal structures of native and inhibited forms of human cathepsin D: Implications for lysosomal targeting and drug design. Proc Natl Acad Sci USA 90:6796-6800.
3. Barrett AJ. 1977. Cathepsin D and other carboxyl proteinases. In: Barrett AJ, ed. Proteinases in mammalian cells and tissues. New York: Elsevier/North Holland Biomedical Press. pp 209-248.
4. Castaldo AM, Nixon RA. 1990. Enzymatically active lysosomal proteases are associated with amyloid deposits in Alzheimer brain. Proc Natl Acad Sci USA 87:3861-3865.
5. Dreyer RN, Bausch KM, Fracasso P, Hammond LJ, Wunderlich D, Wirak DO, Davis G, Brini CM, Buckholz TM, König G, Kamarck ME, Tamburini PP. 1994. Processing of the pre-β-amyloid protein by cathepsin D is enhanced by a familial Alzheimer's disease mutation. Eur J Biochem 224:265-271.
6. Greenlee W. 1990. Renin inhibitors. Med Res Rev 2:173-236.
7. Jouin P, Castro B, Nisato D. 1987. Stereospecific synthesis of N-protected staline and its analogues via chiral tetramic acids. J Chem Soc Perkin Trans I 1987:1177.
8. Jupp RA, Dunn BM, Jacobs JW, Vlasuk G, Arcuri KE, Veber DF, Perlow DS, Payne LS, Boger J, de Laszlo S, Chakravarty PK, tenBroeke J, Hangauer DG, Ondeyka D, Greenlee WJ, Kay J. 1990. The selectivity of statine-based inhibitors against various human aspartic proteinases. Biochem J 265:871-878.
9. Kenessey A, Banay-Schwartz M, deGuzman T, Lajtha A. 1989. Increase in cathepsin D activity in rat brain in aging. J Neurosci Res 23:454-456.
10. Ladror US, Snyder SW, Wang GT, Holzman TF, Krafft GA. 1994. Cleavage at the amino and carboxyl termini of Alzheimer's amyloid-β by cathepsin D. J Biol Chem 269:18422-18428.
11. Nicholls A, Sharp K, Honig B. 1991. Protein folding and association: Insights from the interfacial and thermodynamic properties of hydrocarbons. Proteins Struct Fund Genet 11:281.
12. Novotny J, Brucoleri R, Saul F. 1989. On the attribution of binding energy in antigen-antibody complexes MCPC 603, D1.3 and HyHEL-S. Biochemistry 28:4735-4749.
13. 2 variation. J Med Chem 36:2614-2620.
14. Saftig P, Hetman M, Schmahl W, Weber K, Heine L, Mossmann H, Koster A, Hess B, Evers M, von FK, Christoph P. 1995. Mice deficient for the lysosomal proteinase cathepsin D exhibit progressive atrophy of the intestinal mucosa and profound destruction of lymphoid cells. EMBO J 14(15):3599-3608.
15. Scarborough PE, Guruprasad K, Topham C, Richo GR, Conner GE, Blundell TL, Dunn BM. 1993. Exploration of subsite binding specificity of human cathepsin D through kinetics and rule-based molecular modeling. Protein Sci 2:264-276.
16. van Lierop N, van Noort J, Wagenaar J, Rutten V, Langeveld J, Meloen R, Hensen E. 1994. T cell-stimulatory fragment of foot-and-mouth disease virus released by mild treatment with cathepsin D. J Gen Virol 75:2937-2946.
17. Westley B, May F. 1996. Cathepsin D and breast cancer. Eur J Cancer 32A:15-24.
18. William JW, Morrison JF. 1979. The kinetic of reversible tight-binding inhibition. Methods Enzymol 63:437-467.
19. Xie D, Gulnik S, Gustchina E, Bhat TN, Erickson JW. 1997. Thermodynamic and proton uptake for pepstatin binding to retroviral and eukaryotic aspartic proteases. In: James M, ed. Aspartic proteinases, structure and function: Retroviral and cellular enzymes. New York: Plenum Press. Forthcoming.
20. Yanker BA, Duffy LK, Kirschner DA. 1990. Neurotrophic and neurotoxic effects of amyloid β-protein: Reversal by tachykinin neuropeptides. Science 250:279-282.