2cgf: Difference between revisions
New page: left|200px<br /> <applet load="2cgf" size="450" color="white" frame="true" align="right" spinBox="true" caption="2cgf, resolution 2.202Å" /> '''A RADICICOL ANALOG... |
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==About this Structure== | ==About this Structure== | ||
2CGF is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]] with P2N as [[http://en.wikipedia.org/wiki/ligand ligand]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2CGF OCA]]. | 2CGF is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]] with P2N as [[http://en.wikipedia.org/wiki/ligand ligand]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2CGF OCA]]. | ||
==Reference== | ==Reference== | ||
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[[Category: multigene family]] | [[Category: multigene family]] | ||
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Revision as of 15:13, 30 October 2007
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A RADICICOL ANALOGUE BOUND TO THE ATP BINDING SITE OF THE N-TERMINAL DOMAIN OF THE YEAST HSP90 CHAPERONE
OverviewOverview
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, ... [(full description)]
About this StructureAbout this Structure
2CGF is a [Single protein] structure of sequence from [Saccharomyces cerevisiae] with P2N as [ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
ReferenceReference
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
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