AI Article Synopsis
- A family of aryl-substituted maleimides was created and tested for how effectively they inhibit calmodulin-dependent kinase.
- The inhibitory effects varied significantly, from 34nM to over 20µM, influenced by the type of aryl group and the tether connecting the basic amine to the indolyl maleimide core.
- Key interactions between these compounds and the kinase's ATP site and hinge region were predicted through homology modeling and later confirmed.
Article 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 34nM to >20microM 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.
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| http://dx.doi.org/10.1016/j.bmcl.2008.02.058 | DOI Listing |
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Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.
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Scios, Inc., 6500 Paseo Padre Parkway, Fremont, CA 94555, USA.
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 10nM to >20microM 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.
View Article and Find Full Text PDFAryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 2: SAR of the amine tether.
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Article Synopsis
- A family of aryl-substituted maleimides was created and tested for how effectively they inhibit calmodulin-dependent kinase.
- The inhibitory effects varied significantly, from 34nM to over 20µM, influenced by the type of aryl group and the tether connecting the basic amine to the indolyl maleimide core.
- Key interactions between these compounds and the kinase's ATP site and hinge region were predicted through homology modeling and later confirmed.
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 1: SAR of the aryl region.
Bioorg Med Chem Lett
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Scios, Inc., 6500 Paseo Padre Parkway, Fremont, CA 94555, USA.
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 34nM to >20microM 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.
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