2az5: Difference between revisions

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[[Image:2az5.gif|left|200px]]
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[[Image:2az5.png|left|200px]]


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{{STRUCTURE_2az5|  PDB=2az5  |  SCENE=  }}  
{{STRUCTURE_2az5|  PDB=2az5  |  SCENE=  }}  


'''Crystal Structure of TNF-alpha with a small molecule inhibitor'''
===Crystal Structure of TNF-alpha with a small molecule inhibitor===




==Overview==
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We have identified a small-molecule inhibitor of tumor necrosis factor alpha (TNF-alpha) that promotes subunit disassembly of this trimeric cytokine family member. The compound inhibits TNF-alpha activity in biochemical and cell-based assays with median inhibitory concentrations of 22 and 4.6 micromolar, respectively. Formation of an intermediate complex between the compound and the intact trimer results in a 600-fold accelerated subunit dissociation rate that leads to trimer dissociation. A structure solved by x-ray crystallography reveals that a single compound molecule displaces a subunit of the trimer to form a complex with a dimer of TNF-alpha subunits.
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{{ABSTRACT_PUBMED_16284179}}


==About this Structure==
==About this Structure==
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[[Category: He, M M.]]
[[Category: He, M M.]]
[[Category: Tnf-alpha trimer disruption by binding of a small molecule inhibitor]]
[[Category: Tnf-alpha trimer disruption by binding of a small molecule inhibitor]]
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Revision as of 14:03, 27 July 2008

File:2az5.png

Template:STRUCTURE 2az5

Crystal Structure of TNF-alpha with a small molecule inhibitorCrystal Structure of TNF-alpha with a small molecule inhibitor

Template:ABSTRACT PUBMED 16284179

About this StructureAbout this Structure

2AZ5 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Small-molecule inhibition of TNF-alpha., He MM, Smith AS, Oslob JD, Flanagan WM, Braisted AC, Whitty A, Cancilla MT, Wang J, Lugovskoy AA, Yoburn JC, Fung AD, Farrington G, Eldredge JK, Day ES, Cruz LA, Cachero TG, Miller SK, Friedman JE, Choong IC, Cunningham BC, Science. 2005 Nov 11;310(5750):1022-5. PMID:16284179

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