G-protein-coupled receptors (GPCRs) are activated by a diverse range of ligands, from large proteins and proteases to small peptides, metabolites, neurotransmitters and ions. They are expressed on all cells in the body and have key roles in physiology and homeostasis. As such, GPCRs are one of the most important target classes for therapeutic drug discovery. The development of drugs targeting GPCRs has therapeutic value across a wide range of diseases, including cancer, immune and inflammatory disorders as well as neurological and metabolic diseases. The progress made by targeting GPCRs with antibody-based therapeutics, as well as technical hurdles to overcome, are presented and discussed in this Review. Antibody therapeutics targeting C-C chemokine receptor type 4 (CCR4), CCR5 and calcitonin gene-related peptide (CGRP) are used as illustrative clinical case studies.

G蛋白偶联受体（GPCR）被多种配体激活，从大蛋白和蛋白酶到小肽，代谢物，神经递质和离子。它们在人体所有细胞中表达，在生理和体内平衡中起关键作用。因此，GPCR是治疗药物发现中最重要的目标类别之一。针对GPCR的药物的开发对多种疾病具有治疗价值，包括癌症，免疫和炎性疾病以及神经系统和代谢性疾病。本综述介绍并讨论了以基于抗体的疗法靶向GPCR所取得的进展以及需要克服的技术障碍。靶向4型CC趋化因子受体（CCR4）的抗体治疗剂，