Integrin αV Inhibitors

Integrins are a family of transmembrane receptors that mediate cell-cell and cell-extracellular matrix (ECM) interactions. These heterodimeric proteins are composed of an alpha (α) and a beta (β) subunit, and they play vital roles in various cellular processes, including adhesion, migration, and signal transduction. Among the integrin family, integrin αV is particularly noteworthy. It can pair with different β subunits to form various heterodimers, each with distinct ligand-binding specificities and cellular functions. When engaged with their respective ligands, integrin αV-containing heterodimers can activate intracellular signaling pathways, influencing cell behavior and fate. Given their central role in cellular adhesion and signaling, the precise regulation of integrin αV functions is crucial for maintaining cellular homeostasis and tissue integrity.

Integrin αV inhibitors are a class of chemical compounds designed to target and modulate the activity of integrin αV-containing heterodimers. These inhibitors function by preventing the binding of integrins to their ligands, thereby disrupting integrin-mediated signaling and cellular responses. The mechanism of inhibition can vary among compounds. Some might directly block the ligand-binding site on the integrin, while others might induce conformational changes that render the integrin inactive or less receptive to ligand binding. Additionally, some inhibitors might target the intracellular domains of the integrin, disrupting its association with cytoplasmic proteins and thus its ability to transduce signals.