2bt0: Difference between revisions

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==Overview==
==Overview==
The crystal structure of a previously reported screening hit 1 (CCT018159), bound to the N terminal domain of molecular chaperone Hsp90 has been used, to design 5-amide analogues. These exhibit enhanced potency against the, target in binding and functional assays with accompanying appropriate, cellular pharmacodynamic changes. Compound 11 (VER-49009) compares, favorably with the clinically evaluated 17-AAG.
The crystal structure of a previously reported screening hit 1 (CCT018159) bound to the N terminal domain of molecular chaperone Hsp90 has been used to design 5-amide analogues. These exhibit enhanced potency against the target in binding and functional assays with accompanying appropriate cellular pharmacodynamic changes. Compound 11 (VER-49009) compares favorably with the clinically evaluated 17-AAG.


==About this Structure==
==About this Structure==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Barril, X.]]
[[Category: Barril, X.]]
[[Category: Brough, P.A.]]
[[Category: Brough, P A.]]
[[Category: Cansfield, J.E.]]
[[Category: Cansfield, J E.]]
[[Category: Drysdale, M.J.]]
[[Category: Drysdale, M J.]]
[[Category: Dymock, B.W.]]
[[Category: Dymock, B W.]]
[[Category: Hubbard, R.E.]]
[[Category: Hubbard, R E.]]
[[Category: Massey, A.]]
[[Category: Massey, A.]]
[[Category: Mcdonald, E.]]
[[Category: Mcdonald, E.]]
[[Category: Roughley, S.D.]]
[[Category: Roughley, S D.]]
[[Category: Surgenor, A.]]
[[Category: Surgenor, A.]]
[[Category: Webb, P.]]
[[Category: Webb, P.]]
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[[Category: phosphorylation]]
[[Category: phosphorylation]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:27:31 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:41:19 2008''