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Protein / target

Integrin beta-1

Encoded byITGB1P05556Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
1
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Advanced Clinical

Protein at a glance

Biological role

Collagen binding involved in cell-matrix adhesion

Strongest disease association

Placental abruption

Via encoding gene ITGB1 · Genetic evidence · score 0.46

Therapeutic position

Established drug target

Small molecules and 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

Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are receptors for collagen.

View complete UniProt function annotation

Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are receptors for collagen. Integrins alpha-1/beta-1 and alpha-2/beta-2 recognize the proline-hydroxylated sequence G-F-P-G-E-R in collagen. Integrins alpha-2/beta-1, alpha-3/beta-1, alpha-4/beta-1, alpha-5/beta-1, alpha-8/beta-1, alpha-10/beta-1, alpha-11/beta-1 and alpha-V/beta-1 are receptors for fibronectin. Alpha-4/beta-1 recognizes one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. Integrin alpha-5/beta-1 is a receptor for fibrinogen. Integrin alpha-1/beta-1, alpha-2/beta-1, alpha-6/beta-1 and alpha-7/beta-1 are receptors for lamimin. Integrin alpha-6/beta-1 (ITGA6:ITGB1) is present in oocytes and is involved in sperm-egg fusion (By similarity). Integrin alpha-4/beta-1 is a receptor for VCAM1. It recognizes the sequence Q-I-D-S in VCAM1. Integrin alpha-9/beta-1 is a receptor for VCAM1, cytotactin and osteopontin. It recognizes the sequence A-E-I-D-G-I-E-L in cytotactin. Integrin alpha-3/beta-1 is a receptor for epiligrin, thrombospondin and CSPG4. Alpha-3/beta-1 may mediate with LGALS3 the stimulation by CSPG4 of endothelial cells migration. Integrin alpha-V/beta-1 is a receptor for vitronectin. Beta-1 integrins recognize the sequence R-G-D in a wide array of ligands. When associated with alpha-7 integrin, regulates cell adhesion and laminin matrix deposition. Involved in promoting endothelial cell motility and angiogenesis. Involved in osteoblast compaction through the fibronectin fibrillogenesis cell-mediated matrix assembly process and the formation of mineralized bone nodules. May be involved in up-regulation of the activity of kinases such as PKC via binding to KRT1. Together with KRT1 and RACK1, serves as a platform for SRC activation or inactivation. Plays a mechanistic adhesive role during telophase, required for the successful completion of cytokinesis. Integrin alpha-3/beta-1 provides a docking site for FAP (seprase) at invadopodia plasma membranes in a collagen-dependent manner and hence may participate in the adhesion, formation of invadopodia and matrix degradation processes, promoting cell invasion. ITGA4:ITGB1 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415, PubMed:24789099). ITGA4:ITGB1 and ITGA5:ITGB1 bind 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). ITGA5:ITGB1 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887, PubMed:17158881). ITGA5:ITGB1 acts as a receptor for fibronectin FN1 and mediates R-G-D-dependent cell adhesion to FN1 (PubMed:33962943). ITGA5:ITGB1 is a receptor for IL1B and binding is essential for IL1B signaling (PubMed:29030430). ITGA5:ITGB3 is a receptor for soluble CD40LG and is required for CD40/CD40LG signaling (PubMed:31331973). Plays an important role in myoblast differentiation and fusion during skeletal myogenesis (By similarity). ITGA9:ITGB1 may play a crucial role in SVEP1/polydom-mediated myoblast cell adhesion (By similarity). Integrins ITGA9:ITGB1 and ITGA4:ITGB1 repress PRKCA-mediated L-type voltage-gated channel Ca(2+) influx and ROCK-mediated calcium sensitivity in vascular smooth muscle cells via their interaction with SVEP1, thereby inhibit vasocontraction (PubMed:35802072)

Subcellular location

Cell membraneCell projection, invadopodium membraneCell projection, ruffle membraneRecycling endosomeMelanosomeCleavage furrowCell projection, lamellipodiumCell junction, focal adhesionCell membrane, sarcolemmaCell junction
Domains and Gene Ontology detail (112)

Domains & features

PSIVWFAI-EGF 1I-EGF 2I-EGF 3I-EGF 4

Gene Ontology

  • Ccell surface
  • Ccerebellar climbing fiber to Purkinje cell synapse
  • Ccleavage furrow
  • Ccytoplasm
  • Cdendritic spine
  • Cendosome membrane
  • Cexternal side of plasma membrane
  • Cextracellular exosome
  • Cfilopodium
  • Cfocal adhesion
  • Cglial cell projection
  • Cintegrin alpha1-beta1 complex

798 aa · 88 kDa · 5 isoforms

Biological roles

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

Cell migrationUniProt · GOSynaptic signallingGOIon channel gatingUniProtGrowth-factor signallingGOLipid & lipoprotein metabolismGOCell adhesionUniProt · GO
View supporting evidence

Cell migration

  • ·Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are recept…
  • ·cell migration
  • ·positive regulation of cell migration

Synaptic signalling

  • ·cerebellar climbing fiber to Purkinje cell synapse
  • ·Schaffer collateral - CA1 synapse
  • ·synapse
  • ·regulation of spontaneous synaptic transmission

Ion channel gating

  • ·Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are recept…

Growth-factor signalling

  • ·positive regulation of fibroblast growth factor receptor signaling pathway

Lipid & lipoprotein metabolism

  • ·cellular response to low-density lipoprotein particle stimulus

Cell adhesion

  • ·Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are recept…
  • ·Cell junction, focal adhesion
  • ·Cell junction
  • ·cell adhesion molecule binding

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

Approved medicines with mapped indications

1 medicine · 4 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.

Crohn's Disease1 medicine
Inflammation1 medicine
Multiple Sclerosis1 medicine
Multiple Sclerosis, Relapsing-Remitting1 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.

natalizumab
Narrow target profileApprovedInhibitor

Integrin alpha-4/beta-1 inhibitor

Indicated for Crohn's Disease, Inflammation, Multiple Sclerosis, Multiple Sclerosis, Relapsing-Remitting

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 ITGB1

Gene-level evidence surfaced through the gene ITGB1that 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.

Multiple Sclerosis
0.74Moderately supported

Clinical evidence dominant · Open Targets 0.60

Crohn's Disease
0.69Moderately supported

Clinical evidence dominant · Open Targets 0.56

Multiple Sclerosis, Relapsing-Remitting
0.46Limited support

Clinical evidence dominant · Open Targets 0.37

Placental abruption
0.46Limited support

Genetic evidence dominant · Open Targets 0.28

COVID-19
0.41Limited support

Genetic evidence dominant · Open Targets 0.24

View evidence synthesis (5)
Multiple SclerosisModerately supported
0.74
agreement 0.580.89
Clinical98%Literature2%

Open Targets aggregate 0.60 · 2 independent evidence families

Crohn's DiseaseModerately supported
0.69
agreement 0.540.85
Clinical99%Literature1%

Open Targets aggregate 0.56 · 2 independent evidence families

Multiple Sclerosis, Relapsing-RemittingLimited support
0.46
agreement 0.310.62
Clinical99%Literature1%

Open Targets aggregate 0.37 · 2 independent evidence families

Placental abruptionLimited support
0.46
agreement 0.340.58
Genetic100%

Open Targets aggregate 0.28 · 1 independent evidence family

COVID-19Limited support
0.41
agreement 0.270.55
Genetic94%Literature6%

Open Targets aggregate 0.24 · 2 independent evidence families

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
Multiple Sclerosis0.60
Crohn's Disease0.56
Virus Diseases0.53
Multiple Sclerosis, Relapsing-Remitting0.37
Placental abruption0.28
COVID-190.24
Diabetes Mellitus, Type 10.23
Musculoskeletal Diseases0.23

Drug development

6 compounds recorded · 1 approved · 5 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 (6)
VOLOCIXIMABPhase 2
NATALIZUMABApproval
ABITUZUMABPhase 2
FIRATEGRASTPhase 2
RG-7594Phase 1
ATN-161Phase 2

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 moleculesStrong

Advanced Clinical and Structure with Ligand support this modality.

AntibodiesStrong

Advanced Clinical and UniProt loc high conf support this modality.

Protein degradersEmerging

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

Other modalitiesStrong

Advanced Clinical support this modality.

View underlying tractability evidence (15)
SM · Advanced ClinicalSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · Advanced ClinicalAB · UniProt loc high confAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMAB · Human Protein Atlas locPR · UniProt UbiquitinationPR · 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)

ClinicalTrials.gov via the drug-target graph.

What's happening now

9

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.

  1. Supplemental approval2026-07-23

    Supplemental approval: NATALIZUMAB-SZTN (BLA761322)

    fda · regulatory · fda · via natalizumab

  2. Supplemental approval2026-02-02

    Supplemental approval: NATALIZUMAB-SZTN (BLA761322)

    fda · regulatory · fda · via natalizumab

  3. Label change2025-10-30

    Label change: NATALIZUMAB-SZTN (BLA761322)

    fda · regulatory · fda · via natalizumab

  4. Regulatory approval2023-09-22

    Approval: Tyruko (EMA)

    ema · regulatory · ema · via natalizumab

  5. Regulatory approval2023-08-24

    Approval: NATALIZUMAB-SZTN (BLA761322)

    fda · regulatory · fda · via natalizumab

  6. Safety communication2016-04-18

    Drug Safety Update: Natalizumab (Tysabri▼): progressive multifocal leukoencephalopathy—updated advice to support early detection

    mhra · safety · mhra · via natalizumab

  7. Safety communication2014-12-11

    Drug Safety Update: Natalizumab (Tysabri▼): risk of progressive multifocal leukoencephalopathy increases after 2 years of therapy

    mhra · safety · mhra · via natalizumab

  8. Safety communication2014-12-11

    Drug Safety Update: Natalizumab (Tysabri▼): risk of progressive multifocal leukoencephalopathy is increased in patients who have had previous immunosuppressant treatment

    mhra · safety · mhra · via natalizumab

  9. Regulatory approval2006-06-27

    Approval: Tysabri (EMA)

    ema · regulatory · ema · via natalizumab

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.