Rac GTPase-activating protein 1 (RACGAP1) (RACGAP1)

Rac GTPase-activating protein 1 (RACGAP1) is a critical regulator of cytokinesis and the cell cycle, primarily functioning as a component of the centralspindlin complex (UniProt: P51270). It acts as a GTPase-activating protein for Rho family members such as Rac1 and Cdc42, facilitating the transition from mitosis to cytokinesis by coordinating the formation of the contractile ring (PubMed: 11564802). In many malignancies, including hepatocellular carcinoma and breast cancer, RACGAP1 is significantly overexpressed and serves as a driver of tumor progression, metastasis, and poor clinical outcomes (PubMed: 28656234, 31435355). Targeting RACGAP1 mRNA via RNA interference (siRNA) or antisense oligonucleotides has shown promise in preclinical studies by inducing cell cycle arrest and apoptosis in cancer cells (PubMed: 25110371). However, because of its fundamental role in normal cell division, therapeutic strategies must carefully manage potential toxicities in healthy, rapidly proliferating tissues (PubMed: 23873478). As a target, RACGAP1 mRNA represents a vulnerability in high-proliferation tumors where its depletion leads to mitotic catastrophe.

Other names

MgcRacGAPHsCYK4ID-GAPRac GTPase-activating protein 1Male germ cell RacGAP

RNA interference (RNAi) or antisense-mediated degradation of RACGAP1 mRNA, leading to reduced protein levels and subsequent inhibition of cytokinesis and induction of apoptosis.