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FYVE, RhoGEF and PH domain-containing protein 5 (FGD5)
- Target
- FGD5
- Molecular classification
- Enzyme (specifically, Rho guanine-nucleotide exchange factor, or Rho GEF), Other: Zinc finger protein (contains FYVE domain, typically associated with membrane recruitment)
01
Overview
FYVE, RhoGEF and PH domain-containing protein 5 (FGD5) is a multidomain enzyme that acts as a guanine-nucleotide exchange factor (GEF), primarily activating the Rho GTPase Rac1, and in some contexts Cdc42[1][4]. It contains FYVE, Dbl homology (DH), and pleckstrin homology (PH) domains required for membrane recruitment, GTPase interaction, and catalytic activity[1]. FGD5 is expressed in endothelial cells, where it regulates angiogenesis downstream of factors such as VEGF[1][4]. It also marks hematopoietic stem cells in bone marrow[5]. Amplification and increased expression of FGD5 have been linked to breast cancer proliferation, with variable impact on prognosis[2]. It is considered a therapeutic target in oncology and cardiovascular biology, with experimental drug inhibition studied in vitro[1].
- Other names
- FGD5ZFYVE23FLJ39957FLJ00274Zinc finger FYVE domain-containing protein 23FYVE, RhoGEF and PH domain containing 5
02
Mechanism of action
Direct inhibition of the GEF enzymatic activity (block GDP-GTP exchange on Rac1/Cdc42)
03
Biological functions
Guanyl-nucleotide exchange factor activity (activates Rac1 or CDC42 by GDP-GTP exchange)Actin cytoskeleton organizationRegulation of cell shapeAngiogenesis (promotes angiogenic sprouting in endothelial cells)Filopodium assembly (protrusions required for cell migration)Hematopoietic stem cell marker
04
Disease associations
Cancer (notably, amplification and expression in breast cancer tumor cells; linked to cell proliferation and possible involvement in prognosis)Cardiovascular disease (role in VEGF-induced angiogenesis, endothelial function)Aarskog Syndrome (disease association by genetics)Gastroduodenitis (listed as disease association)
05
Safety considerations
Experimental compounds used to target FGD5 (aurintricarboxylic acid, mitoxantrone) are not yet validated for clinical applicationPotential therapeutic targeting risks due to FGD5's role in basic vascular and hematopoietic biology
06
Interacting drugs
Aurintricarboxylic acid
1 more in the full profile.
07
Biomarkers
FGD5 amplification or protein expression in tumor samples (used in breast cancer studies as both cytoplasmic and nuclear biomarker)FGD5 expression as a marker of hematopoietic stem cells in mice
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