1uyi: Difference between revisions

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[[Image:1uyi.~~gif~~|left|200px]]

[[Image:1uyi.png|left|200px]]

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~~'''~~HUMAN HSP90-ALPHA WITH 8-(2,5-DIMETHOXY-BENZYL)-2-FLUORO-9-PENT-9H-PURIN-6-YLAMINE~~'''~~

===HUMAN HSP90-ALPHA WITH 8-(2,5-DIMETHOXY-BENZYL)-2-FLUORO-9-PENT-9H-PURIN-6-YLAMINE===

~~==Overview==~~

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~~Inhibition of the ATPase activity of the chaperone protein HSP90 is a potential strategy for treatment of cancers. We have determined structures of the HSP90alpha N~~-~~terminal domain complexed with the purine~~-~~based inhibitor~~, ~~PU3~~, ~~and analogs with enhanced potency both in enzyme and cell-based assays. The compounds induce upregulation of HSP70 and downregulation of~~ the ~~known HSP90 client proteins Raf-1, CDK4, and ErbB2, confirming that~~ the ~~molecules inhibit cell growth by a mechanism dependent~~ on ~~HSP90 inhibition~~. ~~We have also determined~~ the ~~first structure of the N~~-terminal domain of HSP90beta, complexed with PU3. The structures allow a detailed rationale to be developed for the observed affinity of the PU3 class of compounds for HSP90 and also provide a structural framework for design of compounds with improved binding affinity and drug-~~like properties.~~

The line below this paragraph, {{ABSTRACT_PUBMED_15217611}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 15217611 is the PubMed ID number.

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==About this Structure==

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[[Category: Hsp90]]

[[Category: Puz]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sat May 3 11~~:51:51 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 08:40:19 2008''

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-[[Image:1uyi.gif|left|200px]]
+{{Seed}}
+[[Image:1uyi.png|left|200px]]
 <!--
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 {{STRUCTURE_1uyi|  PDB=1uyi  |  SCENE=  }}
-'''HUMAN HSP90-ALPHA WITH 8-(2,5-DIMETHOXY-BENZYL)-2-FLUORO-9-PENT-9H-PURIN-6-YLAMINE'''
+===HUMAN HSP90-ALPHA WITH 8-(2,5-DIMETHOXY-BENZYL)-2-FLUORO-9-PENT-9H-PURIN-6-YLAMINE===
-==Overview==
+<!--
-Inhibition of the ATPase activity of the chaperone protein HSP90 is a potential strategy for treatment of cancers. We have determined structures of the HSP90alpha N-terminal domain complexed with the purine-based inhibitor, PU3, and analogs with enhanced potency both in enzyme and cell-based assays. The compounds induce upregulation of HSP70 and downregulation of the known HSP90 client proteins Raf-1, CDK4, and ErbB2, confirming that the molecules inhibit cell growth by a mechanism dependent on HSP90 inhibition. We have also determined the first structure of the N-terminal domain of HSP90beta, complexed with PU3. The structures allow a detailed rationale to be developed for the observed affinity of the PU3 class of compounds for HSP90 and also provide a structural framework for design of compounds with improved binding affinity and drug-like properties.
+The line below this paragraph, {{ABSTRACT_PUBMED_15217611}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 15217611 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_15217611}}
 ==About this Structure==
@@ Line 45: / Line 49: @@
 [[Category: Hsp90]]
 [[Category: Puz]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 11:51:51 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 08:40:19 2008''