Author/Authors :
Daniel E. Levy، نويسنده , , Dan-Xiong Wang، نويسنده , , Qing Lu، نويسنده , , Zheng Chen، نويسنده , , John Perumattam، نويسنده , , Yong-jin Xu، نويسنده , , Albert Liclican، نويسنده , , Jeffrey Higaki، نويسنده , , Hanmin Dong، نويسنده , , Maureen Laney، نويسنده , , Babu Mavunkel، نويسنده , , Sundeep Dugar، نويسنده ,
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 hydrogen bond donating potential of the maleimide ring. Key interactions with the kinase ATP site and hinge region were found to be consistent with homology modeling predictions.
Keywords :
inhibitors , kinase , maleimides , calmodulin
