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

doi:10.1111/bph.16325

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

Institute of Biochemistry, Food Science and Nutrition

Research output: Contribution to journal › Review article › peer-review

3 Scopus citations

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 language	English
Journal	British Journal of Pharmacology
DOIs	https://doi.org/10.1111/bph.16325
State	Accepted/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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10.1111/bph.16325

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title = "The dark sides of the GPCR tree - research progress on understudied GPCRs",

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.",

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

note = "Publisher Copyright: {\textcopyright} 2024 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.",

year = "2024",

doi = "10.1111/bph.16325",

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AU - Berndt, Sandra

AU - Di Pizio, Antonella

AU - Lehmann, Juliane

AU - Liebscher, Ines

AU - Nicoli, Alessandro

AU - Niv, Masha Y.

AU - Peri, Lior

AU - Schihada, Hannes

AU - Schulte, Gunnar

PY - 2024

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AB - 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.

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KW - G protein-coupled receptors

KW - adhesion GPCRs

KW - odorant receptors

KW - orphan receptors

KW - taste receptors

KW - understudied GPCRs

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

Abstract

Bibliographical note

Keywords

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