G protein-coupled receptors as promising targets in cancer

Claudia V. Perez Almeria, Irfan M. Setiawan, Marco Siderius, Martine J. Smit*

*Corresponding author for this work

Research output: Contribution to JournalReview articleAcademicpeer-review


G protein-coupled receptors (GPCRs) control diverse cellular functions, and their dysregulation is involved in a plethora of diseases including tumorigenesis. In the last decade, the association of GPCRs with cancer has become apparent and offers new opportunities to target GPCRs in oncology. GPCR overexpression and mutations lead to aberrant activation of pro-oncogenic pathways inducing tumor progression. In this review, we describe how GPCRs activate some main signaling pathways that contribute to different cancer hallmarks, including cell transformation, proliferative signaling, immune evasion, angiogenesis, and metastasis. Thereafter, we highlight different approaches to target GPCRs, including small molecules and biologics (e.g. monoclonal antibodies and nanobodies) and combinatorial (immuno)therapies that are emerging with promising effects for cancer treatment.

Original languageEnglish
Pages (from-to)119-127
Number of pages9
JournalCurrent Opinion in Endocrine and Metabolic Research
Early online date26 Oct 2020
Publication statusPublished - Feb 2021


  • Biologics
  • Cancer
  • GPCRs
  • Small molecules
  • Therapeutics
  • Tumour microenvironment


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