This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


2bsm

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:2bsm.gif|left|200px]]
[[Image:2bsm.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 2bsm |SIZE=350|CAPTION= <scene name='initialview01'>2bsm</scene>, resolution 2.05&Aring;
+
The line below this paragraph, containing "STRUCTURE_2bsm", creates the "Structure Box" on the page.
-
|SITE= <scene name='pdbsite=AC1:Bsm+Binding+Site+For+Chain+A'>AC1</scene>
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=BSM:5-(5-CHLORO-2,4-DIHYDROXYPHENYL)-N-ETHYL-4-(4-METHOXYPHENYL)-1H-PYRAZOLE-3-CARBOXAMIDE'>BSM</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY=
+
or leave the SCENE parameter empty for the default display.
-
|GENE=
+
-->
-
|DOMAIN=
+
{{STRUCTURE_2bsm| PDB=2bsm | SCENE= }}
-
|RELATEDENTRY=
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bsm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bsm OCA], [http://www.ebi.ac.uk/pdbsum/2bsm PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bsm RCSB]</span>
+
-
}}
+
'''NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN'''
'''NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN'''
Line 38: Line 35:
[[Category: Workman, P.]]
[[Category: Workman, P.]]
[[Category: Wright, L.]]
[[Category: Wright, L.]]
-
[[Category: atp-binding]]
+
[[Category: Atp-binding]]
-
[[Category: atpase]]
+
[[Category: Atpase]]
-
[[Category: chaperone]]
+
[[Category: Chaperone]]
-
[[Category: heat shock]]
+
[[Category: Heat shock]]
-
[[Category: hsp90]]
+
[[Category: Hsp90]]
-
[[Category: pu3]]
+
[[Category: Pu3]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:44:43 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:11:11 2008''
+

Revision as of 17:44, 3 May 2008

Image:2bsm.gif

Template:STRUCTURE 2bsm

NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN


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.

About this Structure

2BSM is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design., Dymock BW, Barril X, Brough PA, Cansfield JE, Massey A, McDonald E, Hubbard RE, Surgenor A, Roughley SD, Webb P, Workman P, Wright L, Drysdale MJ, J Med Chem. 2005 Jun 30;48(13):4212-5. PMID:15974572 Page seeded by OCA on Sat May 3 20:44:43 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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