1d8f

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[[Image:1d8f.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_1d8f| PDB=1d8f | SCENE= }}
{{STRUCTURE_1d8f| PDB=1d8f | SCENE= }}
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'''CRYSTAL STRUCTURE OF MMP3 COMPLEXED WITH A PIPERAZINE BASED INHIBITOR.'''
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===CRYSTAL STRUCTURE OF MMP3 COMPLEXED WITH A PIPERAZINE BASED INHIBITOR.===
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==Overview==
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A new generation of cyclic matrix metalloproteinase (MMP) inhibitors derived from dl-piperazinecarboxylic acid has been described. The design involves: incorporation of hydroxamic acid as the bidentate chelating agent for catalytic Zn(2+), placement of a sulfonamide group at the 1N-position of the piperazine ring to fill the S1' pocket of the enzyme, and finally attachment of diverse functional groups at the 4N-position to optimize potency and peroral absorption. A unique combination of all three elements produced inhibitor 20 with high affinity for MMPs 1, 3, 9, and 13 (24, 18, 1.9, and 1.3 nM, respectively). X-ray crystallography data obtained for MMP-3 cocrystallized with 20 gave detailed information on key binding interactions defining an overall scaffold geometry for piperazine-based MMP inhibitors.
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The line below this paragraph, {{ABSTRACT_PUBMED_10669564}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 10669564 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10669564}}
==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 13:34:02 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 22:40:13 2008''

Revision as of 19:40, 30 June 2008

Image:1d8f.png

Template:STRUCTURE 1d8f

CRYSTAL STRUCTURE OF MMP3 COMPLEXED WITH A PIPERAZINE BASED INHIBITOR.

Template:ABSTRACT PUBMED 10669564

About this Structure

1D8F is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of piperazine-based matrix metalloproteinase inhibitors., Cheng M, De B, Pikul S, Almstead NG, Natchus MG, Anastasio MV, McPhail SJ, Snider CE, Taiwo YO, Chen L, Dunaway CM, Gu F, Dowty ME, Mieling GE, Janusz MJ, Wang-Weigand S, J Med Chem. 2000 Feb 10;43(3):369-80. PMID:10669564

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