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Target intelligence / Profile preview
ADP-ribosylation factor guanine nucleotide exchange factors (ARF-GEFs)
- Target
- ARF-GEFs
- Molecular classification
- Enzyme, Guanine nucleotide exchange factor
01
Overview
ADP-ribosylation factor guanine nucleotide exchange factors (ARF-GEFs) are a family of proteins that catalyze the exchange of GDP for GTP on ADP-ribosylation factors (ARFs), which are small GTP-binding proteins involved in membrane trafficking, vesicle formation, and cytoskeletal dynamics. ARF-GEFs play a central role in regulating the activity of ARFs by promoting their active, GTP-bound state. They contain a conserved Sec7 domain responsible for nucleotide exchange activity and are divided into subfamilies like Gea/GBF/GNOM, Sec7/BIG, Cytohesin/ARNO, and EFA6, each with distinct localization and function. Their activity is often sensitive to brefeldin A (BFA). Dysregulation has been linked to diseases involving secretion disorders or neurodegeneration.
02
Mechanism of action
Catalyzes GDP-to-GTP exchange on ARFs, activating them for downstream signaling in vesicle formation and protein trafficking.
03
Biological functions
Vesicle formationProtein traffickingRegulation of ARF activityMembrane traffickingCytoskeletal dynamics
04
Disease associations
Secretion disordersNeurodegenerationIntracellular trafficking defects
05
Safety considerations
Dysregulation can lead to intracellular trafficking defects.Inhibition can disrupt Golgi structure.
06
Interacting drugs
Brefeldin A (BFA)
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