Title of article
Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 3: Importance of the indole orientation
Author/Authors
Qing Lu، نويسنده , , Zheng Chen، نويسنده , , John Perumattam، نويسنده , , Dan-Xiong Wang، نويسنده , , Weiling Liang، نويسنده , , Yong-jin Xu، نويسنده , , Steven Do، نويسنده , , Llorente Bonaga، نويسنده , , Jeffrey Higaki، نويسنده , , Hanmin Dong، نويسنده , , Albert Liclican، نويسنده , , Steve Sideris، نويسنده , , Maureen Laney، نويسنده , , Sundeep Dugar، نويسنده , , Babu Mavunkel، نويسنده , , Daniel E. Levy، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
2399
To page
2403
Abstract
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 10 nM to >20 μM 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.
Keywords
inhibitors , calmodulin , maleimides , kinase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799367
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