2f7x: Difference between revisions

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[[Image:2f7x.~~gif~~|left|200px]]

[[Image:2f7x.png|left|200px]]

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~~'''~~Protein Kinase A bound to (S)-2-(1H-Indol-3-yl)-1-[5-((E)-2-pyridin-4-yl-vinyl)-pyridin-3-yloxymethyl]-ethylamine~~'''~~

===Protein Kinase A bound to (S)-2-(1H-Indol-3-yl)-1-[5-((E)-2-pyridin-4-yl-vinyl)-pyridin-3-yloxymethyl]-ethylamine===

~~==Overview==~~

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~~A novel series of Akt/PKB inhibitors derived from a screening lead (1) has been prepared.~~ The ~~novel trans-3~~,~~4'-bispyridinylethylenes described herein are potent inhibitors of Akt/PKB with IC(50) values in~~ the ~~low double-digit nanomolar range against Akt1. Compound 2q shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor~~ to ~~modest selectivity against closely related kinases in~~ the ~~AGC and CMGC families~~. ~~The cellular activities including inhibition of cell growth and phosphorylation of downstream target GSK3 are also described~~. ~~The X-ray structure of compound 2q complexed with PKA in~~ the ~~ATP binding site was determined~~.

The line below this paragraph, {{ABSTRACT_PUBMED_16403626}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16403626 is the PubMed ID number.

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==About this Structure==

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[[Category: Akt inhibitor]]

[[Category: Protein kinase some]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4 03~~:33:57 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:07:52 2008''

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@@ Line 1: / Line 1: @@
-[[Image:2f7x.gif|left|200px]]
+{{Seed}}
+[[Image:2f7x.png|left|200px]]
 <!--
@@ Line 9: / Line 10: @@
 {{STRUCTURE_2f7x|  PDB=2f7x  |  SCENE=  }}
-'''Protein Kinase A bound to (S)-2-(1H-Indol-3-yl)-1-[5-((E)-2-pyridin-4-yl-vinyl)-pyridin-3-yloxymethyl]-ethylamine'''
+===Protein Kinase A bound to (S)-2-(1H-Indol-3-yl)-1-[5-((E)-2-pyridin-4-yl-vinyl)-pyridin-3-yloxymethyl]-ethylamine===
-==Overview==
+<!--
-A novel series of Akt/PKB inhibitors derived from a screening lead (1) has been prepared. The novel trans-3,4'-bispyridinylethylenes described herein are potent inhibitors of Akt/PKB with IC(50) values in the low double-digit nanomolar range against Akt1. Compound 2q shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor to modest selectivity against closely related kinases in the AGC and CMGC families. The cellular activities including inhibition of cell growth and phosphorylation of downstream target GSK3 are also described. The X-ray structure of compound 2q complexed with PKA in the ATP binding site was determined.
+The line below this paragraph, {{ABSTRACT_PUBMED_16403626}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16403626 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16403626}}
 ==About this Structure==
@@ Line 46: / Line 50: @@
 [[Category: Akt inhibitor]]
 [[Category: Protein kinase some]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 03:33:57 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:07:52 2008''