Rap guanine nucleotide exchange factor 1 (RAPGEF1)

Rap guanine nucleotide exchange factor 1 (RAPGEF1), also known as C3G or GRF2, is a cytoplasmic enzyme that acts as a guanine nucleotide exchange factor (GEF) for members of the Ras superfamily, particularly Rap1, and coordinates a range of signaling events downstream of adaptor proteins such as CRK[1][2][3][7]. It modulates processes including integrin-mediated cell adhesion, migration, immune cell signaling, apoptosis, cytoskeletal remodeling, and neurodevelopment[2][3]. Dysregulation of RAPGEF1 can play context-dependent roles in tumorigenesis and has been implicated in metabolic, neurodevelopmental, and immune disorders[2][3]. Various transcript variants exist, and its expression and function are tightly regulated through interactions with kinases and other adaptors[2]. No approved drugs are known to directly target RAPGEF1.

Other names

C3GGRF2Protein C3GGuanine nucleotide-releasing factor 2CRK SH3-binding GNRPRap guanine nucleotide exchange factor (GEF) 1guanine nucleotide-releasing factor 2 (specific for crk proto-oncogene)

Direct modulation of GTPase signaling (primarily Rap1 and Ras family) via guanine nucleotide exchange activity; Regulation of integrin activation and inside-out signaling; Modulation of downstream kinase cascades (including ERK, p38 MAPK)