2byh
From Proteopedia
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==Overview== | ==Overview== | ||
| - | Information from X-ray crystal structures of Hsp90 inhibitors bound to the | + | Information from X-ray crystal structures of Hsp90 inhibitors bound to the human Hsp90 molecular chaperone was used to assist in the design of 3-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as novel inhibitors of Hsp90. Accessing an extra interaction with the protein via Phe138 gave a significant increase in binding potency compared to similar analogues that do not make this interaction. |
==About this Structure== | ==About this Structure== | ||
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[[Category: Barril, X.]] | [[Category: Barril, X.]] | ||
[[Category: Beswick, M.]] | [[Category: Beswick, M.]] | ||
| - | [[Category: Brough, P | + | [[Category: Brough, P A.]] |
| - | [[Category: Drysdale, M | + | [[Category: Drysdale, M J.]] |
| - | [[Category: Dymock, B | + | [[Category: Dymock, B W.]] |
[[Category: Grant, K.]] | [[Category: Grant, K.]] | ||
[[Category: Massey, A.]] | [[Category: Massey, A.]] | ||
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[[Category: pyrazole]] | [[Category: pyrazole]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:42:57 2008'' |
Revision as of 14:42, 21 February 2008
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3-(5-CHLORO-2,4-DIHYDROXYPHENYL)-PYRAZOLE-4-CARBOXAMIDES AS INHIBITORS OF THE HSP90 MOLECULAR CHAPERONE
Overview
Information from X-ray crystal structures of Hsp90 inhibitors bound to the human Hsp90 molecular chaperone was used to assist in the design of 3-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as novel inhibitors of Hsp90. Accessing an extra interaction with the protein via Phe138 gave a significant increase in binding potency compared to similar analogues that do not make this interaction.
About this Structure
2BYH is a Single protein structure of sequence from Homo sapiens with as ligand. Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone., Brough PA, Barril X, Beswick M, Dymock BW, Drysdale MJ, Wright L, Grant K, Massey A, Surgenor A, Workman P, Bioorg Med Chem Lett. 2005 Dec 1;15(23):5197-201. Epub 2005 Oct 5. PMID:16213716
Page seeded by OCA on Thu Feb 21 16:42:57 2008
Categories: Homo sapiens | Single protein | Barril, X. | Beswick, M. | Brough, P A. | Drysdale, M J. | Dymock, B W. | Grant, K. | Massey, A. | Surgenor, A. | Workman, P. | Wright, L. | 2D7 | Atp-binding | Chaperone | Heat shock | Hsp90 | Nucleotide-binding | Phosphorylation | Pyrazole
