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Target intelligence / Profile preview
Pleckstrin homology domain-containing family G member 1 (PLEKHG1)
- Target
- PLEKHG1
- Molecular classification
- Enzyme, Guanine nucleotide exchange factor (GEF), RhoGEF family
01
Overview
Pleckstrin homology domain-containing family G member 1 (PLEKHG1) is a guanine nucleotide exchange factor (GEF) that acts primarily on Rho family small GTPases, including Cdc42 and Rac, and is involved in the regulation of actin cytoskeleton dynamics and cell morphology[1][2]. The protein contains a Dbl homology (DH) domain and a pleckstrin homology (PH) domain, characteristic of proteins with GEF activity, and is activated through tyrosine phosphorylation, notably by the Src-family kinase FYN[1]. PLEKHG1 contributes to mechanotransduction in vascular endothelial cells, controlling changes in orientation and migration in response to mechanical stretch, and has been implicated in diseases such as prostate cancer and panic disorder[1][2]. It is not currently a direct therapeutic target of any known drug.
- Other names
- ARHGEF41KIAA1209Pleckstrin homology and RhoGEF domain containing G1PLEKHG1Pleckstrin homology domain-containing family G member 1pleckstrin homology domain containing, family G (with RhoGEF domain) member 1
02
Mechanism of action
Modulation of Rho-family small GTPases (such as activation of Cdc42 and Rac) via GEF activity
03
Biological functions
Signal transductionRegulation of small GTPase-mediated signal transductionActin cytoskeleton organizationCell morphology modulationMechanotransduction
04
Disease associations
Cancer (prostate cancer)Panic disorderPotentially cardiovascular disease through roles in vascular endothelial cell mechanotransduction
05
Safety considerations
Perturbation of cell structureAbnormal migration
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