KIT receptor tyrosine kinase (KIT)

KIT receptor tyrosine kinase (also known as c-KIT or CD117) is a transmembrane protein that serves as a growth factor receptor for stem cell factor (SCF or KITLG) and plays an essential role in signal transduction pathways controlling cell proliferation, survival, and differentiation. Aberrant activation or mutation of KIT is a well-established driver of several malignancies, most notably gastrointestinal stromal tumors. Sunitinib is a small-molecule inhibitor that binds to the ATP-binding pocket of KIT, stabilizing its autoinhibited conformation and blocking kinase activity. Sunitinib is used clinically as a second-line therapy in GIST patients with imatinib-resistant KIT mutations, but certain activation loop mutations conferring drug resistance remain a therapeutic challenge.

Other names

c-KITCD117Mast/stem cell growth factor receptor Kit

ATP-competitive inhibition of the KIT kinase domain, blocking phosphorylation and downstream signaling\nInduction of autoinhibited kinase conformation