Composite: BCR-ABL1, SRC family kinase, c-KIT, EPHA2, PDGFRβ (BCR-ABL1, SRC, KIT, EPHA2, PDGFRB)

These proteins are tyrosine kinases involved in signal transduction cascades that regulate cell growth, proliferation, survival, and mobility. BCR-ABL1 is a fusion protein created by chromosomal translocation in leukemia, leading to constitutive kinase activity and uncontrolled cell division. c-KIT, EPHA2, and PDGFRβ are receptor tyrosine kinases activated by their respective ligands, involved in development, cancer progression, angiogenesis, and more. SRC family kinases are non-receptor tyrosine kinases that act as signaling mediators downstream of various receptors, integrating signals from growth factors, cell adhesion molecules, and immune receptors. In oncology, all are critical as drug targets due to their roles in driving malignancy upon dysregulation.

Other names

Philadelphia chromosome proteinBCR::ABLPH+ proteinSRCFYNLYNYESBLKHCKnon-receptor tyrosine kinasesCD117stem cell factor receptorKIT proto-oncogeneEphA2Ephrin receptor A2PDGFRBPDGF receptor beta

Inhibition of tyrosine kinase activity: competitive inhibition at the ATP-binding site or allosteric inhibition (asciminib for BCR-ABL1); Blockade of downstream signaling: preventing cell proliferation and survival; Induction of apoptosis in target cells