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 ,
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
