Target intelligence / Profile preview

ADP-ribosylation factor 1 (ARF1)

Target
ARF1
Molecular classification
Small GTPase, Enzyme, Regulatory protein, Ras superfamily
01

Overview

ADP-ribosylation factor 1 is a small GTP-binding protein belonging to the Ras superfamily, functioning as a key regulator of vesicular trafficking, primarily at the Golgi apparatus. ARF1 cycles between an active GTP-bound state and an inactive GDP-bound state, with conformational changes critical for its ability to recruit coat proteins (such as COPI) and adaptors that drive vesicle formation, cargo sorting, and membrane curvature. It also interacts with and activates enzymes including phospholipase D. Dysfunction of ARF1 can disrupt membrane traffic and contribute to diseases such as cancer and neurodegenerative disorders. The prototypical ARF inhibitor, Brefeldin A, disrupts ARF1’s function by preventing GDP-GTP exchange, highlighting its role as a drug target.

Other names
ARF1ADP-ribosylation factor 1 (human)ADP-ribosylation factor 1 GTPase
02

Mechanism of action

Inhibition of ARF1 GTPase (by Brefeldin A, leading to disruption of vesicular transport)

03

Biological functions

Vesicular traffickingProtein transportGolgi apparatus maintenanceSignal transduction
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Disease associations

CancerNeurodegenerative diseaseInflammationOther (general roles in various diseases via membrane trafficking dysfunction)
05

Safety considerations

Targeting ARF1 may disrupt essential cellular trafficking and Golgi function, with high risk for cellular toxicity and global cellular dysfunction.
06

Interacting drugs

Brefeldin A
07

Biomarkers

Golgi integrity markers (used to observe ARF1 activity/dysfunction in research)

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