2a8h: Difference between revisions

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[[Image:2a8h.gif|left|200px]]
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{{STRUCTURE_2a8h|  PDB=2a8h  |  SCENE=  }}  
{{STRUCTURE_2a8h|  PDB=2a8h  |  SCENE=  }}  


'''Crystal structure of catalytic domain of TACE with Thiomorpholine Sulfonamide Hydroxamate inhibitor'''
===Crystal structure of catalytic domain of TACE with Thiomorpholine Sulfonamide Hydroxamate inhibitor===




==Overview==
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A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing propargylic ether P1' groups, was explored. In particular, compound 5h has excellent in vitro potency against isolated TACE enzyme and in cells, oral activity in a model of TNF-alpha production and a collagen-induced arthritis model, was selected as a clinical candidate for the treatment of RA.
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{{ABSTRACT_PUBMED_16426848}}


==About this Structure==
==About this Structure==
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[[Category: Tace/adam-17]]
[[Category: Tace/adam-17]]
[[Category: Zn-endopeptidase]]
[[Category: Zn-endopeptidase]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 18:44:38 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 06:56:01 2008''

Revision as of 06:56, 28 July 2008

File:2a8h.png

Template:STRUCTURE 2a8h

Crystal structure of catalytic domain of TACE with Thiomorpholine Sulfonamide Hydroxamate inhibitorCrystal structure of catalytic domain of TACE with Thiomorpholine Sulfonamide Hydroxamate inhibitor

Template:ABSTRACT PUBMED 16426848

About this StructureAbout this Structure

2A8H is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates., Levin JI, Chen JM, Laakso LM, Du M, Schmid J, Xu W, Cummons T, Xu J, Jin G, Barone D, Skotnicki JS, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. Epub 2006 Jan 19. PMID:16426848

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