ARFGAP1

ARFGAP1 encodes ADP-ribosylation factor GTPase-activating protein 1, often called ARF GAP 1. As a GTPase-activating protein, it catalyzes GTP hydrolysis of ARF1 and ARF3, inactivating these small GTPases. This regulation is critical for COP I-mediated retrograde vesicle transport between the Golgi apparatus and endoplasmic reticulum, maintaining organelle structure and protein trafficking homeostasis.
Dysregulated ARFGAP1 is linked to breast and lung cancers, where its overexpression may enhance cell migration and invasion by altering vesicle-mediated secretion of metastatic factors. Preclinical studies are exploring small molecules targeting its GAP activity to disrupt aberrant trafficking, though no therapeutic agents have entered clinical trials yet.