1. Academic Validation
  2. G protein-coupled receptor-targeting antibody-drug conjugates: Current status and future directions

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

  • Cancer Lett. 2023 Jun 28:564:216191. doi: 10.1016/j.canlet.2023.216191.
Peyton High 1 Kendra S Carmon 2
Affiliations

Affiliations

  • 1 Center for Translational Cancer Research, The Brown Foundation Institute of Molecular Medicine, The University of Texas Health Science Center at Houston, Houston, TX, 77030, USA; The University of Texas MD Anderson Cancer Center UTHealth Houston Graduate School of Biomedical Sciences, Houston, TX, 77030, USA.
  • 2 Center for Translational Cancer Research, The Brown Foundation Institute of Molecular Medicine, The University of Texas Health Science Center at Houston, Houston, TX, 77030, USA. Electronic address: [email protected].
Abstract

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.

Keywords

Antibody; Drug conjugate; G protein-coupled receptor; Linker; Payload.

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