2vo7: Difference between revisions

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-[[Image:2vo7.jpg|left|200px]]
+{{Seed}}
+[[Image:2vo7.png|left|200px]]
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 {{STRUCTURE_2vo7|  PDB=2vo7  |  SCENE=  }}
-'''STRUCTURE OF PKA COMPLEXED WITH 4-(4-CHLOROBENZYL)-1-(7H-PYRROLO(2,3-D)PYRIMIDIN-4-YL)PIPERIDIN-4-YLAMINE'''
+===STRUCTURE OF PKA COMPLEXED WITH 4-(4-CHLOROBENZYL)-1-(7H-PYRROLO(2,3-D)PYRIMIDIN-4-YL)PIPERIDIN-4-YLAMINE===
-==Overview==
+<!--
-Fragment-based screening identified 7-azaindole as a protein kinase B inhibitor scaffold. Fragment elaboration using iterative crystallography of inhibitor-PKA-PKB chimera complexes efficiently guided improvements in the potency and selectivity of the compounds, resulting in the identification of nanomolar 6-(piperidin-1-yl)purine, 4-(piperidin-1-yl)-7-azaindole, and 4-(piperidin-1-yl)pyrrolo[2,3- d]pyrimidine inhibitors of PKBbeta with antiproliferative activity and showing pathway inhibition in cells. A divergence in the binding mode was seen between 4-aminomethylpiperidine and 4-aminopiperidine containing molecules. Selectivity for PKB vs PKA was observed with 4-aminopiperidine derivatives, and the most PKB-selective inhibitor (30-fold) showed significantly different bound conformations between PKA and PKA-PKB chimera.
+The line below this paragraph, {{ABSTRACT_PUBMED_18345609}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 18345609 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_18345609}}
 ==About this Structure==
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 [[Category: Serine/threonine-protein kinase]]
 [[Category: Transferase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 30 13:35:01 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:44:59 2008''