Community guidelines for GPCR ligand bias: IUPHAR review 32
Publikation: Bidrag til tidsskrift › Review › Forskning › fagfællebedømt
Dokumenter
- Fulltext
Forlagets udgivne version, 6,61 MB, PDF-dokument
GPCRs modulate a plethora of physiological processes and mediate the effects of one-third of FDA-approved drugs. Depending on which ligand activates a receptor, it can engage different intracellular transducers. This ‘biased signalling’ paradigm requires that we now characterize physiological signalling not just by receptors but by ligand–receptor pairs. Ligands eliciting biased signalling may constitute better drugs with higher efficacy and fewer adverse effects. However, ligand bias is very complex, making reproducibility and description challenging. Here, we provide guidelines and terminology for any scientists to design and report ligand bias experiments. The guidelines will aid consistency and clarity, as the basic receptor research and drug discovery communities continue to advance our understanding and exploitation of ligand bias. Scientific insight, biosensors, and analytical methods are still evolving and should benefit from and contribute to the implementation of the guidelines, together improving translation from in vitro to disease-relevant in vivo models.
| Originalsprog | Engelsk |
|---|---|
| Tidsskrift | British Journal of Pharmacology |
| Vol/bind | 179 |
| Udgave nummer | 14 |
| Sider (fra-til) | 3651-3674 |
| ISSN | 0007-1188 |
| DOI | |
| Status | Udgivet - 2022 |
Bibliografisk note
Funding Information:
Deutsche Forschungsgemeinschaft, Grant/Award Numbers: 290847012, DFG‐407626949, KO1582/10‐1, KO1582/10‐2, KO4095/5‐1; Horizon 2020 Framework, Programme, Grant/Award Number: CA18133; Lundbeckfonden, Grant/Award Number: R313‐2019‐526; Novo Nordisk Fonden, Grant/Award Number: NNF18OC0031226; COST; COST Action ERNEST, Grant/Award Number: CA18133; ERA‐NET NEURON & Ministry of Economy, Industry and Competitiveness, Grant/Award Number: AC18/00030; Instituto de Salud Carlos III FEDER, Grant/Award Number: PI18/00094; Novo Nordisk Foundation, Grant/Award Number: NNF18OC0031226; Lundbeck Foundation, Grant/Award Number: R313‐2019‐526 A off on
Funding Information:
We acknowledge Kasper Harpsøe, Mette M. Rosenkilde, and Nevin Lambert for comments on this manuscript. D.E.G. received financial support from the Lundbeck Foundation (grant R313‐2019‐526) and Novo Nordisk Foundation (grant NNF18OC0031226). P.K. thanks the German Research Foundation DFG for Heisenberg professorship (grant KO4095/5‐1). M.B. (Marcel Bermudez) thanks the German Research Foundation DFG for funding (grant DFG‐407626949). E.K. was supported by the German Research Foundation DFG‐funded research unit FOR2372 (grant 290847012). J.S. acknowledges financial support from the Instituto de Salud Carlos III FEDER (grant PI18/00094) and the ERA‐NET NEURON & Ministry of Economy, Industry and Competitiveness (grant AC18/00030). This article is based upon work from COST Action ERNEST (CA18133), supported by COST (European Cooperation in Science and Technology, www.cost.eu ). M.Bo. holds the Canada Research Chair in Signal Transduction and Molecular Pharmacology.
Publisher Copyright:
© 2022 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.
Antal downloads er baseret på statistik fra Google Scholar og www.ku.dk
ID: 303173212