DISCOVERY OF MUTANT SELECTIVE PLATELET DERIVED GROWTH FACTOR RECEPTOR (PDGFR) FAMILY KINASE INHIBITORS

Abstract

In the past decade there has been rapid growth in the number of FDA approved cancer drugs within the class known as kinase inhibitors. Some kinase inhibitors have become first line chemotherapy for certain tumor types. For example, imatinib (Gleevec) is used effectively to treat Ph+ chronic myelogenous leukemia. Unfortunately, resistance to kinase inhibitors can develop through upregulation of, or mutation of the target kinase resulting in decreased drug binding