The majority of marketed and late stage development kinase inhibitors are reported to be ATPcompetitive. As a result, many promising drug candidates display non-specific activity that results in undesired physiological effects. There is growing interest towards non-ATP competitive kinase inhibitors, as they are expected to yield highly specific and efficacious molecules devoid of non-mechanistic toxicity. Recent developments in this area are summarized in our review.
Keywords: Protein kinases, Tyrosine kinases, Serine/threonine kinases, Non-ATP competitive inhibitor, Allosteric binding, Library design
Rights & PermissionsPrintExport