Integrin beta-1 subunit-containing receptors (ITGB1 integrins)

Integrins are heterodimeric transmembrane receptors composed of alpha and beta subunits that mediate cell-extracellular matrix (ECM) and cell-cell interactions. The β1-containing integrin family is the largest subgroup, involving the β1 subunit (CD29) paired with various alpha subunits. Integrins α2β1 and α3β1 primarily serve as receptors for collagen and laminin, respectively, playing vital roles in platelet function, wound healing, and epithelial stability (UniProt P05556, P17301). In contrast, other β1 integrins like α5β1, α8β1, and αvβ1 recognize the Arginine-Glycine-Aspartic acid (RGD) motif found in proteins like fibronectin and vitronectin (PubMed: 28219922). These receptors are frequently upregulated in various cancers, where they promote tumor cell survival, migration, and angiogenesis, making them significant therapeutic targets (Nature Reviews Drug Discovery, 2017). Drugs targeting these integrins, such as the monoclonal antibody Volociximab or the pan-β1 inhibitor OS2966, aim to disrupt pathological adhesion and signaling pathways involved in oncology and fibrotic diseases (ClinicalTrials.gov).

Other names

CD29VLA proteinsVery Late Antigen familyGPIa-IIa (for α2β1)VLA-2VLA-3VLA-5VLA-8

Antagonism of ligand binding to the extracellular domain, preventing interaction with ECM components like collagen, laminin, and fibronectin, thereby inhibiting downstream FAK/Src signaling pathways.