An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently.


Kinases are important therapeutic targets in oncology due to their frequent deregulation in cancer. Typical ATP-competitive kinase inhibitors, however, also inhibit off-target kinases that could lead to drug toxicity. Allosteric inhibitors represent an alternative approach to achieve greater kinase selectivity, although examples of such compounds are few… (More)
DOI: 10.1158/1535-7163.MCT-09-0102


5 Figures and Tables