Repurposing ARBs as treatments for breast cancer

Abstract

An increased understanding of G-protein-coupled receptors (GPCRs) has greatly influenced modern medicine, where approximately 30 to 50% of all marketed drugs act by binding to GPCRs. The angiotensin II receptor type 1 (AT1R), a classic seven transmembrane domain GPCR, is activated by the endogenously expressed peptide angiotensin II (AngII). Specific AT1R antagonists (angiotensin receptor blockers, ARBs) were first developed in the 1980s and are well characterised for their effects in treating cardiovascular disease (CVD). Extensive clinical studies indicating excellent patient tolerance to ARB treatment in the context of CVD, combined with recent evidence demonstrating a role for AT1R signalling in the pathogenesis of some forms of cancer, highlights the need to evaluate the therapeutic potential of repurposing this class of medications in the treatment of cancer [1-3].