Integrin alpha-V beta-3, Integrin alpha-V beta-5, and Integrin alpha-5 beta-1 (Integrin αvβ3, Integrin αvβ5, and Integrin α5β1)

Integrins αvβ3, αvβ5, and α5β1 are heterodimeric transmembrane cell adhesion receptors that mediate interactions between cells and the extracellular matrix (ECM)[5][7]. These integrins are critical regulators of angiogenesis, cell migration, and signal transduction during normal tissue homeostasis, development, and immune responses[2][6][8]. - Integrin αvβ3 is a major receptor for vitronectin and fibronectin, supporting endothelial cell survival, migration, and new blood vessel formation during angiogenesis[6]. - Integrin αvβ5 also binds vitronectin and is involved in TGF-β activation, wound healing, and phagocytosis by macrophages[2]. - Integrin α5β1 is the primary fibronectin receptor and key mediator of cell adhesion, migration, and proliferation, especially in processes such as development, tissue repair, and immune cell function[3]. They are overexpressed in many cancers and inflamed tissues, and are well-validated therapeutic targets for anti-angiogenic, anti-inflammatory, and anti-metastatic agents[4][8]. Ligand binding leads to intracellular signaling that modulates cytoskeleton organization, gene expression, and cell fate. Importantly, redundancy and compensation among integrins and their crosstalk with growth factor receptors can limit the efficacy of integrin-targeted therapies, necessitating careful clinical application[4][6].

Other names

αvβ3 integrinαvβ5 integrinα5β1 integrinVitronectin receptor (for αvβ3 and αvβ5)Fibronectin receptor (for α5β1)CD51/CD61 (for αvβ3)CD49e/CD29 (for α5β1)

Inhibition of ligand binding (e.g., inhibition of interaction with vitronectin, fibronectin, fibrinogen) Blockade of signaling pathways which promote angiogenesis, cell survival, migration, and proliferation Promotion of apoptosis in endothelial and tumor cells by disrupting integrin-ECM interactions Modulation of immune cell recruitment and function