2iwx: Difference between revisions

Line 1:

[[Image:2iwx.~~jpg~~|left|200px]]

[[Image:2iwx.png|left|200px]]

<!--

Line 9:

Line 10:

~~'''~~ANALOGUES OF RADICICOL BOUND TO THE ATP-BINDING SITE OF HSP90.~~'''~~

===ANALOGUES OF RADICICOL BOUND TO THE ATP-BINDING SITE OF HSP90.===

~~==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.

The line below this paragraph, {{ABSTRACT_PUBMED_17114002}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 17114002 is the PubMed ID number.

-->

==About this Structure==

Line 33:

Line 37:

[[Category: Multigene family]]

[[Category: Nucleotide-binding]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4 08~~:00:43 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 05:48:45 2008''

Navigation menu

Page actions

Page actions

Personal tools

Navigation

Search

Tools

@@ Line 1: / Line 1: @@
-[[Image:2iwx.jpg|left|200px]]
+{{Seed}}
+[[Image:2iwx.png|left|200px]]
 <!--
@@ Line 9: / Line 10: @@
 {{STRUCTURE_2iwx|  PDB=2iwx  |  SCENE=  }}
-'''ANALOGUES OF RADICICOL BOUND TO THE ATP-BINDING SITE OF HSP90.'''
+===ANALOGUES OF RADICICOL BOUND TO THE ATP-BINDING SITE OF HSP90.===
-==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.
+The line below this paragraph, {{ABSTRACT_PUBMED_17114002}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 17114002 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_17114002}}
 ==About this Structure==
@@ Line 33: / Line 37: @@
 [[Category: Multigene family]]
 [[Category: Nucleotide-binding]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 08:00:43 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 05:48:45 2008''