2cgf

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[[Image:2cgf.jpg|left|200px]]
[[Image:2cgf.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2cgf |SIZE=350|CAPTION= <scene name='initialview01'>2cgf</scene>, resolution 2.202&Aring;
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The line below this paragraph, containing "STRUCTURE_2cgf", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:P2n+Binding+Site+For+Chain+A'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=P2N:(5Z)-13-CHLORO-14,16-DIHYDROXY-3,4,7,8,9,10-HEXAHYDRO-1H-2-BENZOXACYCLOTETRADECINE-1,11(12H)-DIONE'>P2N</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_2cgf| PDB=2cgf | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2cgf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2cgf OCA], [http://www.ebi.ac.uk/pdbsum/2cgf PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2cgf RCSB]</span>
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}}
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'''A RADICICOL ANALOGUE BOUND TO THE ATP BINDING SITE OF THE N-TERMINAL DOMAIN OF THE YEAST HSP90 CHAPERONE'''
'''A RADICICOL ANALOGUE BOUND TO THE ATP BINDING SITE OF THE N-TERMINAL DOMAIN OF THE YEAST HSP90 CHAPERONE'''
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[[Category: Prodromou, C.]]
[[Category: Prodromou, C.]]
[[Category: Roe, S M.]]
[[Category: Roe, S M.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: chaperone]]
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[[Category: Chaperone]]
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[[Category: heat shock]]
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[[Category: Heat shock]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: multigene family]]
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[[Category: Multigene family]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 22:04:48 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:21:07 2008''
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Revision as of 19:04, 3 May 2008

Image:2cgf.jpg

Template:STRUCTURE 2cgf

A RADICICOL ANALOGUE BOUND TO THE ATP BINDING SITE OF THE N-TERMINAL DOMAIN OF THE YEAST HSP90 CHAPERONE


Overview

A series of benzo-macrolactones of varying ring size and conformation has been prepared by chemical synthesis and evaluated by structural and biological techniques. Thus, 12- to 16-membered lactones were obtained by concise routes, involving ring-closing metathesis as a key step. In enzyme assays, the 13-, 15-, and 16-membered analogs are good inhibitors, suggesting that they can adopt the required conformation to fit in the ATP-binding site. This was confirmed by cocrystallization of 13-, 14-, and 15-membered lactones with the N-terminal domain of yeast Hsp90, showing that they bind similarly to the "natural" 14-membered radicicol. The most active compounds in the ATPase assays also showed the greatest growth-inhibitory potency in HCT116 human colon cancer cells and the established molecular signature of Hsp90 inhibition, i.e., depletion of client proteins with upregulation of Hsp70.

About this Structure

2CGF is a Single protein structure of sequence from Saccharomyces cerevisiae. Full crystallographic information is available from OCA.

Reference

Inhibition of Hsp90 with synthetic macrolactones: synthesis and structural and biological evaluation of ring and conformational analogs of radicicol., Proisy N, Sharp SY, Boxall K, Connelly S, Roe SM, Prodromou C, Slawin AM, Pearl LH, Workman P, Moody CJ, Chem Biol. 2006 Nov;13(11):1203-15. PMID:17114002 Page seeded by OCA on Sat May 3 22:04:48 2008

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