Target intelligence / Profile preview

Integrin alpha-8 beta-1 (ITGA8B1)

Target
ITGA8B1
Molecular classification
Integrin, Cell adhesion molecule, Heterodimeric transmembrane receptor, RGD-binding receptor
01

Overview

Integrin alpha-8 beta-1 is a heterodimeric cell surface receptor composed of the alpha-8 (ITGA8) and beta-1 (ITGB1) subunits. It belongs to the RGD-binding integrin family, which recognizes the arginine-glycine-aspartic acid motif in ligands such as nephronectin, osteopontin, and fibronectin (UniProt P53708). Biologically, this integrin is essential for kidney morphogenesis, mediating critical interactions between the ureteric bud and the metanephric mesenchyme during development (PMID: 9023306). In adult tissues, it is primarily expressed in contractile cells, including vascular smooth muscle cells and renal mesangial cells, where it helps maintain tissue architecture. Pathologically, Integrin alpha-8 beta-1 is significantly upregulated in activated myofibroblasts during the progression of fibrosis in the liver, lungs, and kidneys (PMID: 28611158). Its role in promoting myofibroblast activation and TGF-beta signaling makes it a prominent therapeutic target for chronic fibrotic diseases. Experimental treatments, including small molecule inhibitors like CWHM-12 and specific monoclonal antibodies, aim to block its ligand-binding domain to attenuate pathological tissue remodeling (PMID: 24631444). Targeting this receptor offers a potential pathway to arrest the progression of idiopathic pulmonary fibrosis and chronic kidney disease.

Other names
ITGA8:ITGB1Integrin alpha 8 beta 1Alpha8beta1 integrinITGA8/ITGB1 complex
02

Mechanism of action

Competitive antagonism of the RGD-binding site to prevent interaction with extracellular matrix ligands, thereby inhibiting myofibroblast activation and TGF-beta signaling pathways.

03

Biological functions

Cell adhesionCell migrationKidney morphogenesisSmooth muscle cell differentiationSignal transductionMyofibroblast activationExtracellular matrix organization
04

Disease associations

FibrosisChronic kidney diseaseIdiopathic pulmonary fibrosisLiver fibrosisRenal agenesisCancer metastasis
05

Safety considerations

Potential renal toxicityVascular stability concernsImpaired wound healingDevelopmental toxicity (teratogenicity)
06

Interacting drugs

CWHM-12

1 more in the full profile.

07

Biomarkers

ITGA8 expression in myofibroblastsNephronectin (NPNT) levelsOsteopontin (SPP1) levels

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