Target intelligence / Profile preview

ARF GTPase-activating protein 2 (ARFGAP2)

Target
ARFGAP2
Molecular classification
Enzyme (specifically, GTPase-activating protein), Regulatory protein, Signal transduction regulator
01

Overview

ARF GTPase-activating protein 2 (ARFGAP2) is an enzyme that regulates intracellular signal transduction by accelerating the hydrolysis of GTP bound to ARF family GTPases, thereby converting them from the active (GTP-bound) to inactive (GDP-bound) state[1][4]. ARF GTPases act as molecular switches controlling vesicle formation, membrane trafficking, and actin cytoskeleton dynamics. ARFGAP2 acts as a negative regulator, ensuring proper timing and localization of ARF activity. Dysregulation of this GTPase cycle has been linked to developmental defects, cancer cell migration, and other pathologies related to vesicle transport[1][2][4]. While the protein has not been directly targeted by drugs, its critical roles make it a potential candidate for research into cancer metastasis and other diseases involving cell migration or trafficking dysfunction.

Other names
ARFGAP2ADP-ribosylation factor GTPase-activating protein 2ArfGAP2CGAPKIAA1017
02

Mechanism of action

Drugs that would target this class of protein would typically act by: - Inhibiting GTPase-activating function, keeping ARF GTPases in an active state, potentially disrupting membrane trafficking. - Stabilizing or disrupting its interaction with GTPases, thus altering signal output.

03

Biological functions

Regulation of small GTPase signalingNegative regulation of ARF (ADP-ribosylation factor) family GTPases by acting as a GTPase-activating protein (GAP)Control of vesicular trafficking (Golgi, endosomes, plasma membrane)Regulation of actin cytoskeleton restructuringModulating focal adhesion dynamics and cell migration[1][2][4]
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Disease associations

Cancer (through effects on cell migration and cytoskeletal regulation, which can influence metastasis)[1][2]Neurodegenerative disease (implicated via vesicular trafficking dysfunction, though direct evidence specific for ARFGAP2 is limited)Other (disorders of vesicle transport and signal transduction)
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Safety considerations

Therapeutic targeting of this protein may affect fundamental cellular processes such as vesicular trafficking, membrane dynamics, and cytoskeletal organization, raising potential for toxicity involving cell viability, immune responses, and neural or cardiac function if not precisely targeted[1][2][4].Disruption of GTPase regulation is associated with broad cellular dysfunction.

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