Title of article
Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 2: SAR of the amine tether
Author/Authors
Daniel E. Levy، نويسنده , , Dan-Xiong Wang، نويسنده , , Qing Lu، نويسنده , , Zheng Chen، نويسنده , , John Perumattam، نويسنده , , Yong-jin Xu، نويسنده , , Jeffrey Higaki، نويسنده , , Hanmin Dong، نويسنده , , Albert Liclican، نويسنده , , Maureen Laney، نويسنده , , Babu Mavunkel، نويسنده , , Sundeep Dugar، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
2395
To page
2398
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 34 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. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.
Keywords
calmodulin , maleimides , kinase , inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799366
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