2c1b: Difference between revisions

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[[Image:2c1b.~~gif~~|left|200px]]

[[Image:2c1b.png|left|200px]]

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~~'''~~STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE~~'''~~

===STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE===

~~==Overview==~~

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~~Structure~~-~~based drug design of novel isoquinoline~~-~~5-sulfonamide inhibitors of PKB as potential antitumour agents was investigated. Constrained pyrrolidine analogues that mimicked~~ the ~~bound conformation of linear prototypes were identified and investigated by co-crystal structure determinations with~~ the ~~related protein PKA~~. ~~Detailed variation in the binding modes between inhibitors with similar overall conformations was observed~~. ~~Potent PKB inhibitors from this series inhibited GSK3beta phosphorylation in cellular assays~~, ~~consistent with inhibition of PKB kinase activity in cells~~.

The line below this paragraph, {{ABSTRACT_PUBMED_16249095}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16249095 is the PubMed ID number.

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==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 ~~Sat May 3 21~~:05:38 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:46:55 2008''

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-[[Image:2c1b.gif|left|200px]]
+{{Seed}}
+[[Image:2c1b.png|left|200px]]
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 {{STRUCTURE_2c1b|  PDB=2c1b  |  SCENE=  }}
-'''STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE'''
+===STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE===
-==Overview==
+<!--
-Structure-based drug design of novel isoquinoline-5-sulfonamide inhibitors of PKB as potential antitumour agents was investigated. Constrained pyrrolidine analogues that mimicked the bound conformation of linear prototypes were identified and investigated by co-crystal structure determinations with the related protein PKA. Detailed variation in the binding modes between inhibitors with similar overall conformations was observed. Potent PKB inhibitors from this series inhibited GSK3beta phosphorylation in cellular assays, consistent with inhibition of PKB kinase activity in cells.
+The line below this paragraph, {{ABSTRACT_PUBMED_16249095}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16249095 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16249095}}
 ==About this Structure==
@@ Line 46: / Line 50: @@
 [[Category: Serine/threonine-protein kinase]]
 [[Category: Transferase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 21:05:38 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:46:55 2008''