Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 8, Pages 2582-2588Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.03.017
Keywords
JNK; JIP1; Kinase inhibitor
Funding
- NIH [DK080263]
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We report comprehensive structure-activity relationship studies on a novel series of c-Jun N-terminal kinase (JNK) inhibitors. Intriguingly, the compounds have a dual inhibitory activity by functioning as both ATP and JIP mimetics, possibly by binding to both the ATP binding site and to the docking site of the kinase. Several of such novel compounds display potent JNK inhibitory profiles both in vitro and in cell. (C) 2011 Elsevier Ltd. All rights reserved.
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