2byh
From Proteopedia
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| - | [[Image:2byh.gif|left|200px]]<br /><applet load="2byh" size=" | + | [[Image:2byh.gif|left|200px]]<br /><applet load="2byh" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2byh, resolution 1.90Å" /> | caption="2byh, resolution 1.90Å" /> | ||
'''3-(5-CHLORO-2,4-DIHYDROXYPHENYL)-PYRAZOLE-4-CARBOXAMIDES AS INHIBITORS OF THE HSP90 MOLECULAR CHAPERONE'''<br /> | '''3-(5-CHLORO-2,4-DIHYDROXYPHENYL)-PYRAZOLE-4-CARBOXAMIDES AS INHIBITORS OF THE HSP90 MOLECULAR CHAPERONE'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2BYH is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 2D7 as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:2d7 Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | + | 2BYH is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=2D7:'>2D7</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:2d7+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BYH OCA]. |
==Reference== | ==Reference== | ||
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[[Category: pyrazole]] | [[Category: pyrazole]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:29:20 2008'' |
Revision as of 08:29, 3 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 Sun Feb 3 10:29:20 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
