ITGA5

Integrin alpha-5 (ITGA5), also designated CD49e or VLA-5, forms a heterodimer with integrin beta-1 (ITGB1) to constitute the α5β1 integrin receptor. This transmembrane glycoprotein mediates cell-extracellular matrix adhesion by binding fibronectin through its RGD (Arg-Gly-Asp) recognition motif, facilitating cellular migration, proliferation, and survival. The α5β1 integrin activates downstream signaling cascades including FAK/Src, PI3K/Akt, and MAPK pathways, which regulate angiogenesis, tissue remodeling, and epithelial-mesenchymal transition (EMT). Dysregulation of ITGA5 is implicated in tumor metastasis, fibrotic disorders (e.g., pulmonary and hepatic fibrosis), and aberrant wound healing. Therapeutic strategies targeting α5β1, such as monoclonal antibodies (e.g., volociximab), small-molecule inhibitors, and RGD-mimetic peptides, are under investigation for anticancer and antifibrotic applications. Recent phase I/II trials have explored its inhibition in glioblastoma and idiopathic pulmonary fibrosis, demonstrating modulated ECM interactions without severe toxicity.