1yc1: Difference between revisions

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[[Image:1yc1.gif|left|200px]]
{{Seed}}
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{{STRUCTURE_1yc1|  PDB=1yc1  |  SCENE=  }}  
{{STRUCTURE_1yc1|  PDB=1yc1  |  SCENE=  }}  


'''Crystal Structures of human HSP90alpha complexed with dihydroxyphenylpyrazoles'''
===Crystal Structures of human HSP90alpha complexed with dihydroxyphenylpyrazoles===




==Overview==
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A series of dihydroxyphenylpyrazole compounds were identified as a unique class of reversible Hsp90 inhibitors. The crystal structures for two of the identified compounds complexed with the N-terminal ATP binding domain of human Hsp90alpha were determined. The dihydroxyphenyl ring of the compounds fits deeply into the adenine binding pocket with the C2 hydroxyl group forming a direct hydrogen bond with the side chain of Asp93. The pyrazole ring forms hydrogen bonds to the backbone carbonyl of Gly97, the hydroxyl group of Thr184 and to a water molecule, which is present in all of the published HSP90 structures. One of the identified compounds (G3130) demonstrated cellular activities (in Her-2 degradation and activation of Hsp70 promoter) consistent with the inhibition of cellular Hsp90 functions.
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{{ABSTRACT_PUBMED_15713410}}


==About this Structure==
==About this Structure==
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[[Category: Cell-cycle]]
[[Category: Cell-cycle]]
[[Category: Drug design]]
[[Category: Drug design]]
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