2c1e

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{{STRUCTURE_2c1e| PDB=2c1e | SCENE= }}
{{STRUCTURE_2c1e| PDB=2c1e | SCENE= }}
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'''CRYSTAL STRUCTURES OF CASPASE-3 IN COMPLEX WITH AZA-PEPTIDE MICHAEL ACCEPTOR INHIBITORS.'''
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===CRYSTAL STRUCTURES OF CASPASE-3 IN COMPLEX WITH AZA-PEPTIDE MICHAEL ACCEPTOR INHIBITORS.===
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==Overview==
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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 of caspase-3 and caspase-8 in complex with aza-peptide Michael acceptor inhibitors demonstrate the nucleophilic attack on C2 and provide insight into the selectivity and potency of the inhibitors with respect to the P1' moiety.
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(as it appears on PubMed at http://www.pubmed.gov), where 16970398 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16970398}}
==About this Structure==
==About this Structure==
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[[Category: Thiol protease,zymogen]]
[[Category: Thiol protease,zymogen]]
[[Category: Yama]]
[[Category: Yama]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:05:59 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 09:35:41 2008''

Revision as of 06:35, 28 July 2008

Image:2c1e.png

Template:STRUCTURE 2c1e

CRYSTAL STRUCTURES OF CASPASE-3 IN COMPLEX WITH AZA-PEPTIDE MICHAEL ACCEPTOR INHIBITORS.

Template:ABSTRACT PUBMED 16970398

About this Structure

2C1E is a Protein complex structure of sequences from Homo sapiens. 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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