RIT1 allosteric inhibitor

RIT1 allosteric inhibitor is a small molecule, non-covalent, non-competitive inhibitor of Ras-like without CAAX protein 1 (RIT1) GTPase. It binds to a druggable pocket in the switch II domain of RIT1, independent of the GTP-binding active site. By binding to this pocket, the molecule promotes RIT1 dimerization, locking the protein in an inactive state. This allosteric inhibition retains binding capability across both wild-type (amplified) and mutant forms of RIT1 (such as M90I and A77G). In non-small cell lung cancer (NSCLC) cell lines, treatment with this inhibitor leads to downregulation of the G2/M checkpoint, dampened p38 signaling, and upregulation of necroptosis, demonstrating potent anti-tumor activity in RIT1-high and RIT1-aberrant tumors.

Other names

RIT1 allosteric non-competitive inhibitorRIT-1 allosteric non-competitive inhibitorRIT 1 allosteric non-competitive inhibitor