Endothelial cell integrins and angiogenesis-related receptors

Endothelial cell integrins and angiogenesis-related receptors comprise a functional class of cell surface proteins that mediate the complex process of blood vessel formation. This group includes integrin heterodimers, such as alpha-V beta-3, alpha-V beta-5, and alpha-5 beta-1, which facilitate endothelial cell attachment to the extracellular matrix and provide essential survival signals during vessel sprouting (NIH, 2024). It also encompasses key receptor tyrosine kinases, most notably the Vascular endothelial growth factor receptors (VEGFR-1, -2, and -3) and the Tie-2 receptor, which respond to growth factors to drive endothelial cell proliferation and migration (PubMed, 2023). These receptors are critical therapeutic targets because they are often overexpressed in the vasculature of solid tumors and in the retina during pathological neovascularization, such as in wet age-related macular degeneration (Nature Reviews Drug Discovery, 2010). Drugs targeting these molecules, including monoclonal antibodies like ramucirumab and small-molecule inhibitors like sunitinib, aim to inhibit these pathways to suppress tumor growth or prevent vision loss. However, because these receptors are also involved in maintaining normal vascular homeostasis, their pharmacological inhibition is associated with systemic toxicities, including hypertension, proteinuria, and impaired wound healing (StatPearls, 2023). The development of these therapies has faced challenges, such as the emergence of resistance through the activation of alternative angiogenic pathways, necessitating combination strategies.

Other names

Angiogenesis receptorsVascular integrinsPro-angiogenic receptorsEndothelial adhesion molecules

Antagonism of endothelial cell surface receptors, including integrins and receptor tyrosine kinases, to disrupt signaling and adhesion processes required for pathological neovascularization.