Target intelligence / Profile preview

Pleckstrin homology and RhoGEF domain-containing protein G6 (PLEKHG6)

Target
PLEKHG6
Molecular classification
Enzyme, Guanine nucleotide exchange factor (GEF), RhoGEF family protein
01

Overview

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.

Other names
Pleckstrin homology domain-containing family G member 6PH domain-containing family G member 6MyoGEFFLJ10665MYOGEFARHGEF46Myosin-interacting guanine nucleotide exchange factormyosin II interacting GEFmyosin interacting guanine nucleotide exchange factor
02

Mechanism of action

Activation of small GTPase RhoG by catalyzing exchange of GDP for GTP; Indirect modulation of actin cytoskeleton and cell morphology

03

Biological functions

Signal transductionRegulation of small GTPase activityActivation of RhoGInduction of myosin filament formationCytoskeletal remodelingFormation of microvilli and membrane rufflesMacropinocytosis
04

Disease associations

Cancer (potential role via cytoskeletal and signaling regulation, though not directly established)Joubert syndrome 21Periventricular nodular heterotopia

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