2hvx

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{{STRUCTURE_2hvx| PDB=2hvx | SCENE= }}
{{STRUCTURE_2hvx| PDB=2hvx | SCENE= }}
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'''Discovery of Potent, Orally Active, Nonpeptide Inhibitors of Human Mast Cell Chymase by Using Structure-Based Drug Design'''
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===Discovery of Potent, Orally Active, Nonpeptide Inhibitors of Human Mast Cell Chymase by Using Structure-Based Drug Design===
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==Overview==
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A series of beta-carboxamido-phosphon(in)ic acids (2) was identified as a new structural motif for obtaining potent inhibitors of human mast cell chymase. For example, 1-naphthyl derivative 5f had an IC50 value of 29 nM and (E)-styryl derivative 6g had an IC50 value of 3.5 nM. An X-ray structure for 5f.chymase revealed key interactions within the enzyme active site. Compound 5f was selective for inhibiting chymase versus eight serine proteases. Compound 6h was orally bioavailable in rats (F=39%), and orally efficacious in a hamster model of inflammation.
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(as it appears on PubMed at http://www.pubmed.gov), where 17361995 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17361995}}
==About this Structure==
==About this Structure==
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[[Category: Wells, G I.]]
[[Category: Wells, G I.]]
[[Category: Serine protease]]
[[Category: Serine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:46:39 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:41:35 2008''

Revision as of 12:41, 28 July 2008

Image:2hvx.png

Template:STRUCTURE 2hvx

Discovery of Potent, Orally Active, Nonpeptide Inhibitors of Human Mast Cell Chymase by Using Structure-Based Drug Design

Template:ABSTRACT PUBMED 17361995

About this Structure

2HVX is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase., Greco MN, Hawkins MJ, Powell ET, Almond HR Jr, de Garavilla L, Hall J, Minor LK, Wang Y, Corcoran TW, Di Cera E, Cantwell AM, Savvides SN, Damiano BP, Maryanoff BE, J Med Chem. 2007 Apr 19;50(8):1727-30. Epub 2007 Mar 16. PMID:17361995

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