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Pleckstrin homology and RhoGEF domain-containing protein G6 (PLEKHG6) is a guanine nucleotide exchange factor (GEF) selectively activating the small GTPases RhoG and, to a lesser extent, Rac1, thereby regulating signal transduction and cytoskeletal dynamics, including the induction of myosin filament formation, microvilli, and membrane ruffles. PLEKHG6 is recruited by ezrin to the apical membrane of epithelial cells and is essential for macropinocytosis and morphological changes arising from cytoskeletal remodeling. Loss of PLEKHG6 function inhibits these processes, and the protein has been associated with genetic diseases including Joubert syndrome 21 and periventricular nodular heterotopia. It belongs to the enzyme class of RhoGEF family proteins responsible for exchanging GDP for GTP on small GTPases, modulating cell signaling and structure. Although linked to signaling pathways common in cancer, specific drug interactions or safety concerns have not been documented in the current literature.
Activation of small GTPase RhoG by catalyzing exchange of GDP for GTP; Indirect modulation of actin cytoskeleton and cell morphology
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