Target intelligence / Profile preview

Rho guanine nucleotide exchange factor 16 (ARHGEF16)

Target
ARHGEF16
Molecular classification
Guanine nucleotide exchange factor (GEF), Enzyme, Regulatory/signaling protein, Other
01

Overview

Rho guanine nucleotide exchange factor 16 (ARHGEF16) is a member of the RhoGEF family and acts as an activator of Rho-family small GTPases, including RhoG, Rac1, and CDC42. It functions by stimulating these GTPases to exchange GDP for GTP, thus regulating signal transduction pathways involved in cytoskeletal remodeling, cell proliferation, migration, and invasive behavior. In cancer, ARHGEF16 is upregulated in several tumor types—most notably colon cancer, where it promotes cell proliferation, migration, and invasion, and is associated with increased metastatic potential. The protein is also called Ephexin-4 and plays roles in pathways downstream of Eph family receptor tyrosine kinases, with implications for both physiological and pathological conditions, including cancer cell metastasis and potentially apoptotic cell clearance. Its structure includes Dbl homology (DH), pleckstrin homology (PH), and Src homology-3 (SH3) domains, typical of Rho GEF proteins. There are currently no approved drugs specifically targeting ARHGEF16, and its value as a therapeutic target remains experimental.

Other names
Ephexin-4EPHEXIN4GEF16neuroblastoma breakpoint protein (NBR)putative neuroblastoma proteinrho guanine exchange factor (GEF) 16ARHGG
02

Biological functions

Signal transduction (specifically, activation of Rho-family GTPases)Cell proliferationCell migrationCell invasionRegulation of cytoskeletonPossibly apoptotic cell clearance
03

Disease associations

Cancer (notably colon cancer, with supporting evidence also for roles in breast cancer, melanoma, and possibly other tumors)Other (genetic associations reported for osteogenesis imperfecta type I and chromosome 1p36 deletion syndrome, but relevance less clear)

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