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Protein / target

Integrin alpha-V

Encoded byITGAVP06756Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
1
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Structure with Ligand

Protein at a glance

Biological role

Transforming growth factor beta binding

Strongest disease association

Inflammatory Bowel Diseases

Via encoding gene ITGAV · Genetic evidence · score 0.51

Therapeutic position

Established drug target

Antibodies

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

The alpha-V (ITGAV) integrins are receptors for vitronectin, cytotactin, fibronectin, fibrinogen, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin and vWF.

View complete UniProt function annotation

The alpha-V (ITGAV) integrins are receptors for vitronectin, cytotactin, fibronectin, fibrinogen, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin and vWF. They recognize the sequence R-G-D in a wide array of ligands. ITGAV:ITGB3 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 and ITGAV:ITGB6 act as receptors for fibrillin-1 (FBN1) and mediate R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887, PubMed:17158881). Integrin alpha-V/beta-6 or alpha-V/beta-8 (ITGAV:ITGB6 or ITGAV:ITGB8) mediates R-G-D-dependent release of transforming growth factor beta-1 (TGF-beta-1) from regulatory Latency-associated peptide (LAP), thereby playing a key role in TGF-beta-1 activation (PubMed:15184403, PubMed:22278742, PubMed:28117447). ITGAV:ITGB3 acts as a receptor for CD40LG (PubMed:31331973). ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP (PubMed:10640428)

Subcellular location

Cell membraneCell junction, focal adhesion
Domains and Gene Ontology detail (70)

Gene Ontology

  • Calphav-beta3 integrin-HMGB1 complex
  • Calphav-beta3 integrin-IGF-1-IGF1R complex
  • Calphav-beta3 integrin-PKCalpha complex
  • Ccell surface
  • Cexternal side of plasma membrane
  • Cextracellular exosome
  • Cfilopodium membrane
  • Cfocal adhesion
  • Cintegrin alphav-beta1 complex
  • Cintegrin alphav-beta3 complex
  • Cintegrin alphav-beta5 complex
  • Cintegrin alphav-beta6 complex

1048 aa · 116 kDa · 3 isoforms

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Lipid & lipoprotein metabolismGOCell migrationGOIon channel gatingGOReceptor tyrosine kinase signallingUniProtCell proliferation & survivalGOCell adhesionUniProt · GO
View supporting evidence

Lipid & lipoprotein metabolism

  • ·apolipoprotein A-I-mediated signaling pathway
  • ·negative regulation of lipid transport
  • ·negative regulation of lipoprotein metabolic process
  • ·negative regulation of low-density lipoprotein particle clearance

Cell migration

  • ·cell migration
  • ·negative chemotaxis
  • ·positive regulation of cell migration

Ion channel gating

  • ·calcium ion transmembrane transport

Receptor tyrosine kinase signalling

  • ·The alpha-V (ITGAV) integrins are receptors for vitronectin, cytotactin, fibronectin, fi…

Cell proliferation & survival

  • ·positive regulation of cell population proliferation

Cell adhesion

  • ·The alpha-V (ITGAV) integrins are receptors for vitronectin, cytotactin, fibronectin, fi…
  • ·Cell junction, focal adhesion
  • ·extracellular matrix binding
  • ·extracellular matrix protein binding

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Approved medicines with mapped indications

1 medicine · 2 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Angina, Unstable1 medicine
Thrombosis1 medicine

Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

abciximab
Narrow target profileApprovedInhibitor

Integrin alpha-V/beta-3 inhibitor

Indicated for Angina, Unstable, Thrombosis

Direct interaction with this protein · 1 of 3 recorded protein targets — narrow recorded profile

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene ITGAV

Gene-level evidence surfaced through the gene ITGAV that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Ischemic Stroke
0.53Moderately supported

Clinical evidence dominant · Open Targets 0.30

Inflammatory Bowel Diseases
0.52Moderately supported

Genetic evidence dominant · Open Targets 0.31

Myocardial Infarction
0.50Moderately supported

Clinical evidence dominant · Open Targets 0.40

Angina Pectoris
0.46Limited support

Clinical evidence dominant · Open Targets 0.37

Glioblastoma
0.39Limited support

Clinical evidence dominant · Open Targets 0.31

View evidence synthesis (5)
Ischemic StrokeModerately supported
0.53
agreement 0.400.66
Clinical56%Animal model43%Literature1%

Open Targets aggregate 0.30 · 3 independent evidence families

Inflammatory Bowel DiseasesModerately supported
0.52
agreement 0.380.66
Genetic95%Literature5%

Open Targets aggregate 0.31 · 2 independent evidence families

Myocardial InfarctionModerately supported
0.50
agreement 0.350.66
Clinical91%Literature9%

Open Targets aggregate 0.40 · 2 independent evidence families

Angina PectorisLimited support
0.46
agreement 0.300.61
Clinical99%Literature1%

Open Targets aggregate 0.37 · 2 independent evidence families

GlioblastomaLimited support
0.39
agreement 0.240.55
Clinical90%Literature10%

Open Targets aggregate 0.31 · 2 independent evidence families

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Neurodegenerative Diseases0.42
Myocardial Infarction0.40
Angina Pectoris0.37
Inflammatory Bowel Diseases0.31
Glioblastoma0.31
Ischemic Stroke0.30

Drug development

9 compounds recorded · 1 approved · 8 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (9)
CILENGITIDEPhase 3
STX-100Phase 2
RG-7594Phase 1
ABCIXIMABApproval
INTETUMUMABPhase 2
ABITUZUMABPhase 2
ATN-161Phase 2
ETARACIZUMABPhase 2
IMGN-388Phase 1

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesEmerging

Feasibility evidence (structure with ligand and high-quality ligand) — no clinical-stage drug of this modality recorded.

AntibodiesStrong

Approved Drug and GO CC high conf support this modality.

Protein degradersEmerging

Feasibility evidence (database ubiquitination and half-life data) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Advanced Clinical support this modality.

View underlying tractability evidence (12)
SM · Structure with LigandSM · High-Quality LigandSM · High-Quality PocketSM · Druggable FamilyAB · Approved DrugAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule BinderOC · Advanced Clinical

Raw Open Targets tractability assessment buckets, by modality.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

WITHDRAWN · via abciximab · NCT00178451

ClinicalTrials.gov via the drug-target graph.

What's happening now

2

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.