Epithelial cell-transforming sequence 2 (ECT2) (ECT2)

Epithelial cell-transforming sequence 2 (ECT2) is a guanine nucleotide exchange factor (GEF) that plays a critical role in regulating the activity of Rho family GTPases, particularly RhoA, Rac1, and Cdc42 (UniProt Q9H8G1). It is essential for the coordination of cytokinesis, the final stage of cell division, where it localizes to the midbody to trigger the assembly of the contractile ring (PubMed: 24631444). Beyond its role in mitosis, ECT2 is involved in signal transduction pathways that govern cell polarity, migration, and proliferation (NCBI Gene: 1894). In many human malignancies, ECT2 is significantly overexpressed and acts as a potent oncogene, driving tumor progression, invasion, and metastasis (PubMed: 31481619). Its overexpression is often associated with poor prognosis in cancers such as non-small cell lung cancer and hepatocellular carcinoma (PubMed: 28811391). While there are currently no FDA-approved drugs specifically targeting ECT2, it is considered a high-priority therapeutic target, with research focusing on small molecules that inhibit its GEF activity or disrupt its interaction with downstream effectors (PubMed: 31481619).

Other names

ECT2Protein ECT2ARHGEF31Epithelial cell-transforming sequence 2 oncogene

Inhibition of RhoGEF activity by blocking the exchange of GDP for GTP on Rho family GTPases (RhoA, Rac1, Cdc42), thereby disrupting downstream signaling pathways essential for cytokinesis and oncogenic growth (PubMed: 28811391, 31481619).