G protein-coupled receptor-targeting antibody-drug conjugates: Current status and future directions

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 malig-nancies. 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.

Automated summary

In recent years, antibody-drug conjugates (ADCs) have shown great potential as anti-cancer therapeutic agents, and some have been approved for the treatment of solid tumors and hematological malignancies. G protein-coupled receptors (GPCRs), which are known therapeutic targets in various human diseases including cancer, have emerged as a promising target for ADCs. This review discusses the past and current therapeutic targeting of GPCRs and describes the use of ADCs as a therapeutic modality. Additionally, the status of preclinical and clinical GPCR-targeted ADCs is summarized, and the potential of GPCRs as novel targets for future ADC development is addressed.