2byh

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:2byh.gif|left|200px]]<br /><applet load="2byh" size="350" color="white" frame="true" align="right" spinBox="true"
+
[[Image:2byh.gif|left|200px]]
-
caption="2byh, resolution 1.90&Aring;" />
+
 
-
'''3-(5-CHLORO-2,4-DIHYDROXYPHENYL)-PYRAZOLE-4-CARBOXAMIDES AS INHIBITORS OF THE HSP90 MOLECULAR CHAPERONE'''<br />
+
{{Structure
 +
|PDB= 2byh |SIZE=350|CAPTION= <scene name='initialview01'>2byh</scene>, resolution 1.90&Aring;
 +
|SITE= <scene name='pdbsite=AC1:2d7+Binding+Site+For+Chain+A'>AC1</scene>
 +
|LIGAND= <scene name='pdbligand=2D7:N-(4-ACETYLPHENYL)-5-(5-CHLORO-2,4-DIHYDROXYPHENYL)-1H-PYRAZOLE-4-CARBOXAMIDE'>2D7</scene>
 +
|ACTIVITY=
 +
|GENE=
 +
}}
 +
 
 +
'''3-(5-CHLORO-2,4-DIHYDROXYPHENYL)-PYRAZOLE-4-CARBOXAMIDES AS INHIBITORS OF THE HSP90 MOLECULAR CHAPERONE'''
 +
 
==Overview==
==Overview==
Line 7: Line 16:
==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 <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].
+
2BYH is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BYH OCA].
==Reference==
==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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16213716 16213716]
+
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:[http://www.ncbi.nlm.nih.gov/pubmed/16213716 16213716]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
Line 32: Line 41:
[[Category: pyrazole]]
[[Category: pyrazole]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:42:57 2008''
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:08:22 2008''

Revision as of 14:08, 20 March 2008

Image:2byh.gif


PDB ID 2byh

Drag the structure with the mouse to rotate
, resolution 1.90Å
Sites:
Ligands:
Coordinates: save as pdb, mmCIF, xml



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. 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 Mar 20 16:08:22 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2byh"
Personal tools