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 ,
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
