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2c2z

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[[Category: zymogen]]
[[Category: zymogen]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 08:47:47 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 10:48:37 2007''

Revision as of 08:43, 30 October 2007

Image:2c2z.gif

2c2z, resolution 1.95Å

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CRYSTAL STRUCTURE OF CASPASE-8 IN COMPLEX WITH AZA-PEPTIDE MICHAEL ACCEPTOR INHIBITOR

Overview

Aza-peptide Michael acceptors are a novel class of inhibitors that are, potent and specific for caspases-2, -3, -6, -7, -8, -9, and -10. The, second-order rate constants are in the order of 10(6) M(-1) s(-1). The, aza-peptide Michael acceptor inhibitor 18t, (Cbz-Asp-Glu-Val-AAsp-trans-CH=CH-CON(CH(2)-1-Naphth)(2) is the most, potent compound and it inhibits caspase-3 with a k(2) value of 5620000, M(-1) s(-1). The inhibitor 18t is 13700, 190, 6.4, 594, 37500, and, 173-fold more selective for caspase-3 over caspases-2, -6, -7, -8, -9, and, -10, respectively. Aza-peptide Michael acceptors designed with caspase, specific sequences are selective and do not show any cross reactivity with, clan CA cysteine proteases such as papain, cathepsin B, and calpains., High-resolution crystal structures ... [(full description)]

About this Structure

2C2Z is a [Single protein] structure of sequence from [Homo sapiens] with DTD as [ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

Design, synthesis, and evaluation of aza-peptide Michael acceptors as selective and potent inhibitors of caspases-2, -3, -6, -7, -8, -9, and -10., Ekici OD, Li ZZ, Campbell AJ, James KE, Asgian JL, Mikolajczyk J, Salvesen GS, Ganesan R, Jelakovic S, Grutter MG, Powers JC, J Med Chem. 2006 Sep 21;49(19):5728-49. PMID:16970398

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