近年来，抗体药物结合物（ADCs）已成为有前途的抗癌治疗药物，其中一些已经获得市场批准，用于实体肿瘤和血液恶性肿瘤的治疗。随着ADC技术的不断改进和ADC可治疗的适应症范围的增加，靶抗原的种类已经扩展，并且无疑将继续增长。G蛋白偶联受体（GPCRs）是已很好研究的治疗靶点，与许多人类病理学（包括癌症）有关，并代表ADC的有前途的新靶点。在这篇综述中，我们将讨论过去和现在GPCRs作为治疗靶点的应用，并描述ADC作为治疗手段。此外，我们将总结现有的临床前和临床的GPCR靶向ADC的现状，并探讨GPCRs作为未来ADC开发的新靶点的潜力。Copyright © 2023. Published by Elsevier B.V.

In recent years, antibody-drug conjugates (ADCs) have emerged as promising anti-cancer therapeutic agents with several having already received market approval for the treatment of solid tumor and hematological malignancies. As ADC technology continues to improve and the range of indications treatable by ADCs increases, the repertoire of target antigens has expanded and will undoubtedly continue to grow. G protein-coupled receptors (GPCRs) are well-characterized therapeutic targets implicated in many human pathologies, including cancer, and represent a promising emerging target of ADCs. In this review, we will discuss the past and present therapeutic targeting of GPCRs and describe ADCs as therapeutic modalities. Moreover, we will summarize the status of existing preclinical and clinical GPCR-targeted ADCs and address the potential of GPCRs as novel targets for future ADC development.Copyright © 2023. Published by Elsevier B.V.