Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.

Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation. Research Abstract Details 

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Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation. Abstract Text:

Qing Lu,Zheng Chen,John Perumattam,Dan-Xiong Wang,Weiling Liang,Yong-Jin Xu,Steven Do,Llorente Bonaga,Jeffrey Higaki,Hanmin Dong,Albert Liclican,Steve Sideris,Maureen Laney,Sundeep Dugar,Babu Mavunkel,Daniel E Levy,Qing Lu,Zheng Chen,John Perumattam,Dan-Xiong Wang,Weiling Liang,Yong-Jin Xu,Steven Do,Llorente Bonaga,Jeffrey Higaki,Hanmin Dong,Albert Liclican,Steve Sideris,Maureen Laney,Sundeep Dugar,Babu Mavunkel,Daniel E Levy,

A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 10nM to >20microM and were dependant upon both the nature of the aryl group and the tether joining the basic amine to the indolyl maleimide core of the inhibitors. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.

Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation. Publishing Authors By Initials

Q Lu,Z Chen,J Perumattam,DX Wang,W Liang,YJ Xu,S Do,L Bonaga,J Higaki,H Dong,A Liclican,S Sideris,M Laney,S Dugar,B Mavunkel,DE Levy,Q Lu,Z Chen,J Perumattam,DX Wang,W Liang,YJ Xu,S Do,L Bonaga,J Higaki,H Dong,A Liclican,S Sideris,M Laney,S Dugar,B Mavunkel,DE Levy,

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Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 2399-403

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ISSN: 1464-3405

DAY: 4

MONTH: 03

YEAR: 2008

Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.

AFFILIATION: Scios, Inc., 6500 Paseo Padre Parkway, Fremont, CA 94555, USA.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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