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

Scharf, Magdalena M. and Humphrys, Laura J. and Berndt, Sandra and Di Pizio, Antonella and Lehmann, Juliane and Liebscher, Ines and Nicoli, Alessandro and Niv, Masha Y. and Peri, Lior and Schihada, Hannes and Schulte, Gunnar (2025) The dark sides of the GPCR tree - research progress on understudied GPCRs. WILEY, HOBOKEN.

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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. image

Item Type: Other
Uncontrolled Keywords: PROTEIN-COUPLED RECEPTOR; STRUCTURAL BASIS; INTERNATIONAL UNION; SIGNALING PATHWAYS; TASTE RECEPTORS; ADHESION GPCRS; GPRC6A RECEPTOR; DRUG DISCOVERY; MALE-FERTILITY; IN-VITRO; adhesion GPCRs; Frizzleds; G protein-coupled receptors; odorant receptors; orphan receptors; taste receptors; understudied GPCRs
Subjects: 600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy
Depositing User: Dr. Gernot Deinzer
Date Deposited: 31 Mar 2026 07:06
Last Modified: 31 Mar 2026 07:06
URI: https://pred.uni-regensburg.de/id/eprint/65168

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