barbadin

Barbadin is a selective, small-molecule inhibitor of the interaction between beta-arrestin and the beta2-adaptin subunit of the clathrin adaptor protein AP-2. It was identified through virtual screening and cell-based assays by researchers at the Université de Montréal and McGill University. Barbadin selectively blocks agonist-promoted endocytosis of G protein-coupled receptors (GPCRs), such as the beta2-adrenergic receptor, V2 vasopressin receptor, and angiotensin II type 1 receptor, by disrupting the binding of the beta-arrestin C-tail to the platform domain of beta2-adaptin. It serves as a valuable research tool for studying GPCR trafficking, receptor desensitization, and beta-arrestin-mediated signaling pathways.

Other names

3-amino-5-(4-benzylphenyl)-3H,4H-thieno[2,3-d]pyrimidin-4-one3-amino-5-(4-benzylphenyl)thieno[2,3-d]pyrimidin-4-one