The dark sides of the GPCR tree - research progress on understudied GPCRs

Magdalena M. Scharf*, Laura J. Humphrys, Sandra Berndt, Antonella Di Pizio, Juliane Lehmann, Ines Liebscher, Alessandro Nicoli, Masha Y. Niv, Lior Peri, Hannes Schihada, Gunnar Schulte

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

Abstract

A large portion of the human GPCRome is still in the dark and understudied, consisting even of entire subfamilies of GPCRs such as odorant receptors, class A and C orphans, adhesion GPCRs, Frizzleds and taste receptors. However, it is undeniable that these GPCRs bring an untapped therapeutic potential that should be explored further. Open questions on these GPCRs span diverse topics such as deorphanisation, the development of tool compounds and tools for studying these GPCRs, as well as understanding basic signalling mechanisms. This review gives an overview of the current state of knowledge for each of the diverse subfamilies of understudied receptors regarding their physiological relevance, molecular mechanisms, endogenous ligands and pharmacological tools. Furthermore, it identifies some of the largest knowledge gaps that should be addressed in the foreseeable future and lists some general strategies that might be helpful in this process.

Original languageAmerican English
JournalBritish Journal of Pharmacology
DOIs
StateAccepted/In press - 2024

Bibliographical note

Publisher Copyright:
© 2024 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.

Keywords

  • Frizzleds
  • G protein-coupled receptors
  • adhesion GPCRs
  • odorant receptors
  • orphan receptors
  • taste receptors
  • understudied GPCRs

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