G protein-coupled receptors: novel targets for drug discovery in cancer

Nat Rev Drug Discov. 2011 Jan;10(1):47-60. doi: 10.1038/nrd3320.


G protein-coupled receptors (GPCRs) belong to a superfamily of cell surface signalling proteins that have a pivotal role in many physiological functions and in multiple diseases, including the development of cancer and cancer metastasis. Current drugs that target GPCRs - many of which have excellent therapeutic benefits - are directed towards only a few GPCR members. Therefore, huge efforts are currently underway to develop new GPCR-based drugs, particularly for cancer. We review recent findings that present unexpected opportunities to interfere with major tumorigenic signals by manipulating GPCR-mediated pathways. We also discuss current data regarding novel GPCR targets that may provide promising opportunities for drug discovery in cancer prevention and treatment.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Drug Delivery Systems
  • Drug Design
  • Drug Discovery
  • Humans
  • Neoplasm Metastasis
  • Neoplasms / drug therapy*
  • Neoplasms / physiopathology
  • Neoplasms / prevention & control
  • Receptors, G-Protein-Coupled / drug effects*
  • Receptors, G-Protein-Coupled / metabolism


  • Antineoplastic Agents
  • Receptors, G-Protein-Coupled