Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

ARF1 (P84077) - Overview - Molecular Target Synopsis

Protein


ARF1, ADP-ribosylation factor 1
UniProt P84077

Also Known as ARF1_HUMAN, ARF1

GTP-binding protein involved in protein trafficking among different compartments. Modulates vesicle budding and uncoating within the Golgi complex. Deactivation induces the redistribution of the entire Golgi complex to the endoplasmic reticulum, suggesting a crucial role in protein trafficking. In its GTP-bound form, its triggers the association with coat proteins with the Golgi membrane. The hydrolysis of ARF1-bound GTP, which is mediated by ARFGAPs proteins, is required for dissociation of coat proteins from Golgi membranes and vesicles. The GTP-bound form interacts with PICK1 to limit PICK1-mediated inhibition of Arp2/3 complex activity; the function is linked to AMPA receptor (AMPAR) trafficking, regulation of synaptic plasicity of excitatory synapses and spine shrinkage during long-term depression (LTD)., (Microbial infection) Functions as an allosteric activator of the cholera toxin catalytic subunit, an ADP-ribosyltransferase. Interacts (when activated) with GGA1, GGA2 and GGA3; the interaction is required for proper subcellular location of GGA1, GGA2 and GGA3 (PubMed:11950392, PubMed:28868155). Interacts with ARHGAP21, ASAP2, HERC1, PRKCABP, PIP5K1B, TMED2, PSCD2, TMED10 and GRIA2 (PubMed:10022920, PubMed:17347647, PubMed:23889934, PubMed:8861955). Interacts with ARFGAP1, which hydrolyzes GTP and thus, regulates its function (PubMed:10102276). Interacts with PI4KB in the Golgi complex (PubMed:17555535). Interacts with NCS1/FREQ in the Golgi and at the plasma membrane (PubMed:17555535). Interacts with PLEKHA3 (PubMed:21454700). Interacts with PLEKHA8; the interaction, together with phosphatidylinositol 4-phosphate binding, is required for FAPP2-mediated glucosylceramide transfer activity (PubMed:15107860). Interacts (activated) with PICK1 (via PDZ domain); the interaction blocks Arp2/3 complex inhibition (PubMed:23889934). Interacts with IQSEC1 (PubMed:24058294). Interacts with C9orf72 (By similarity) (PubMed:24058294).

6DFF
STRUCTURE OF THE CARGO BOUND AP-1:ARF1:TETHERIN-NEF MONOMER
RCSB/PDB
Inspect Structure
See all 3D Structures for ARF1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform

Sub-cellular localization


UniProt: ARF1 is active in the following subcellular-locations: cell junction, cytoplasm, golgi apparatus, membrane, perinuclear region, postsynaptic cell membrane, postsynaptic density, synapse, synaptosome, trans-golgi network membrane.
GO terms: ARF1 is active in the following subcellular-locations: cell leading edge, COPI-coated vesicle, cytoplasm, cytosol, extracellular exosome, focal adhesion, glutamatergic synapse, Golgi apparatus, Golgi membrane, late endosome, neuron projection, perinuclear region of cytoplasm, peroxisomal membrane, plasma membrane, postsynaptic density, postsynaptic membrane, protein-containing complex, sarcomere, trans-Golgi network.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ARF1 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: CAKI_1, PC_3, RPMI_8226

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC2911, HCC38, NCI-H1781

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, IMR-90

(see details)

3D Structures


For ARF1 there are:
17 structures (35 chains) solved
16 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ARF1 has been screened with 2 compounds (3 bioactivities). (see details)