BCR-ABL, PDGFR, c-Kit

The term "BCR-ABL, PDGFR, c-Kit" refers to a group of distinct but related therapeutic targets that are frequently co-targeted by tyrosine kinase inhibitors like imatinib. BCR-ABL is a fusion tyrosine kinase generated by a chromosomal translocation, primarily implicated in chronic myeloid leukemia. PDGFR and c-Kit are type III receptor tyrosine kinases involved in cell growth, survival, and proliferation. Dysregulation or activating mutations in these targets contribute to various cancers, including gastrointestinal stromal tumors, leukemias, and other solid tumors. Their structural similarities in the ATP-binding domain allow certain small molecule inhibitors to effectively target multiple members of this group.

Other names

Philadelphia chromosome fusion proteinBCR-ABL1p210p190 (size isoforms)PDGF receptorPDGFR-alphaPDGFR-betaKITCD117stem cell factor receptorSCFR

The common mechanism involves inhibition of the ATP-binding site of the tyrosine kinase domains of these related targets, blocking downstream signaling pathways that drive cell proliferation and survival.