Mounting evidence indicates that single-target drugs might be inadequate to achieve satisfactory therapeutic effects on complex diseases. Recently, increasing attention has been paid to developing drugs that can manipulate multiple targets to generate beneficial effects through potential synergy. G-protein-coupled receptors (GPCRs) become desirable targets for developing multitarget-directed ligands (MTDLs) because of their crucial roles in the pathophysiology of various human diseases and the accessibility of druggable sites at the cell surface. Herein, we review the most recent advances in the development of GPCR-targeted MTDLs in treating complex diseases, and discuss their potential therapeutic strategies to reveal current trends and shed insights into the utility of GPCR-targeted MTDLs for future drug design and development.

越来越多的证据表明，单靶点药物可能不足以对复杂疾病取得令人满意的治疗效果。最近，人们越来越关注开发可以操纵多个靶点以通过潜在的协同作用产生有益效果的药物。G 蛋白偶联受体 (GPCR) 成为开发多靶点定向配体 (MTDL) 的理想靶点，因为它们在各种人类疾病的病理生理学中发挥着至关重要的作用，并且在细胞表面的药物位点的可及性方面发挥着重要作用。在此，我们回顾了 GPCR 靶向 MTDL 在治疗复杂疾病方面的最新进展，并讨论了其潜在的治疗策略，以揭示当前趋势，并深入了解 GPCR 靶向 MTDL 在未来药物设计和开发中的实用性。