G protein-coupled receptors (GPCRs), which play crucial roles in various physiological functions, often assembled into dimers and higher-order oligomers. This oligomerization phenomenon has been observed in diverse physiological and pathological contexts, presenting promising opportunities for drug discovery targeting vital systems such as the cardiovascular, nervous, endocrine, and renal systems. This review offers a concise understanding of GPCR dimerization, its signaling mechanisms, and its implications. Furthermore, we explored therapeutic strategies aimed at modulating receptors involved in dimer/oligomer formation within the renin-angiotensin system.