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1nms

From Proteopedia

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[[Image:1nms.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_1nms| PDB=1nms | SCENE= }}
{{STRUCTURE_1nms| PDB=1nms | SCENE= }}
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'''Caspase-3 tethered to irreversible inhibitor'''
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===Caspase-3 tethered to irreversible inhibitor===
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==Overview==
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Cysteine aspartyl protease-3 (caspase-3) is a mediator of apoptosis and a therapeutic target for a wide range of diseases. Using a dynamic combinatorial technology, 'extended tethering', we identified unique nonpeptidic inhibitors for this enzyme. Extended tethering allowed the identification of ligands that bind to discrete regions of caspase-3 and also helped direct the assembly of these ligands into small-molecule inhibitors. We first designed a small-molecule 'extender' that irreversibly alkylates the cysteine residue of caspase-3 and also contains a thiol group. The modified protein was then screened against a library of disulfide-containing small-molecule fragments. Mass-spectrometry was used to identify ligands that bind noncovalently to the protein and that also form a disulfide linkage with the extender. Linking the selected fragments with binding elements from the extenders generates reversible, tight-binding molecules that are druglike and distinct from known inhibitors. One molecule derived from this approach inhibited apoptosis in cells.
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(as it appears on PubMed at http://www.pubmed.gov), where 12563278 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12563278}}
==About this Structure==
==About this Structure==
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[[Category: Irreversible]]
[[Category: Irreversible]]
[[Category: Tether]]
[[Category: Tether]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:43:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 00:07:42 2008''

Revision as of 21:07, 28 July 2008

Image:1nms.png

Template:STRUCTURE 1nms

Caspase-3 tethered to irreversible inhibitor

Template:ABSTRACT PUBMED 12563278

About this Structure

1NMS is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

In situ assembly of enzyme inhibitors using extended tethering., Erlanson DA, Lam JW, Wiesmann C, Luong TN, Simmons RL, DeLano WL, Choong IC, Burdett MT, Flanagan WM, Lee D, Gordon EM, O'Brien T, Nat Biotechnol. 2003 Mar;21(3):308-14. Epub 2003 Feb 3. PMID:12563278

Page seeded by OCA on Tue Jul 29 00:07:42 2008

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