Integrin subunit alpha 2 (ITGA2)

Integrin subunit alpha 2 (ITGA2), also known as CD49b, is a transmembrane protein that dimerizes with the beta-1 subunit to form the α2β1 integrin complex, a major receptor for collagen and laminin [1, 10]. This receptor is expressed on various cell types, including platelets, endothelial cells, and epithelial cells, where it mediates critical interactions between the cell and the extracellular matrix [1, 5]. In the cardiovascular system, α2β1 is essential for platelet adhesion to collagen at sites of vascular injury, facilitating thrombus formation [6]. In oncology, ITGA2 is frequently upregulated and plays a pivotal role in tumor cell migration, invasion, and the development of chemoresistance in cancers such as pancreatic ductal adenocarcinoma and glioma [4, 13, 14]. Therapeutic targeting of ITGA2 involves small molecules like E7820, which reduces its expression, and allosteric inhibitors like E-6482 that block ligand binding [1, 6]. While targeting this integrin offers potential for treating thrombosis and metastatic cancer, safety considerations include its impact on normal wound healing and the potential for increased bleeding risk [1, 6].

Other names

CD49bVLA-2 alphaPlatelet membrane glycoprotein IaGPIaHPA-5BRVLAA2Very late antigen 2

Inhibition of collagen binding through allosteric modulation of the I-domain or downregulation of subunit expression