1g05

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{{STRUCTURE_1g05| PDB=1g05 | SCENE= }}
{{STRUCTURE_1g05| PDB=1g05 | SCENE= }}
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'''HETEROCYCLE-BASED MMP INHIBITOR WITH P2'SUBSTITUENTS'''
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===HETEROCYCLE-BASED MMP INHIBITOR WITH P2'SUBSTITUENTS===
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==Overview==
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Potent and selective inhibition of matrix metalloproteinases was demonstrated for a series of sulfonamide-based hydroxamic acids. The design of the heterocyclic sulfonamides incorporates a six- or seven-member central ring with a P2' substituent that can be modified. Binding interactions of this substituent at the S2' site are believed to contribute to high inhibitory potency against stromelysin, collagenase-3 and gelatinases A and B, and to provide selectivity against collagenase-1 and matrilysin. An X-ray structure of a stromelysin inhibitor complex was obtained to provide insights into the SAR and selectivity trends observed for the series.
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(as it appears on PubMed at http://www.pubmed.gov), where 11327577 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11327577}}
==About this Structure==
==About this Structure==
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[[Category: Mixed alpha beta structure]]
[[Category: Mixed alpha beta structure]]
[[Category: Zinc protease]]
[[Category: Zinc protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 16:57:49 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 04:12:04 2008''

Revision as of 01:12, 1 July 2008

Image:1g05.png

Template:STRUCTURE 1g05

HETEROCYCLE-BASED MMP INHIBITOR WITH P2'SUBSTITUENTS

Template:ABSTRACT PUBMED 11327577

About this Structure

1G05 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Heterocycle-based MMP inhibitors with P2' substituents., Pikul S, Dunham KM, Almstead NG, De B, Natchus MG, Taiwo YO, Williams LE, Hynd BA, Hsieh LC, Janusz MJ, Gu F, Mieling GE, Bioorg Med Chem Lett. 2001 Apr 23;11(8):1009-13. PMID:11327577

Page seeded by OCA on Tue Jul 1 04:12:04 2008

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