Community guidelines for GPCR ligand bias: IUPHAR review 32
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- dc.contributor.author Kolb, Peter
- dc.contributor.author Kenakin, Terry
- dc.contributor.author Alexander, Stephen P. H.
- dc.contributor.author Bermudez, Marcel
- dc.contributor.author Bohn, Laura M.
- dc.contributor.author Breinholt, Christian S.
- dc.contributor.author Bouvier, Michel
- dc.contributor.author Hill, Stephen J.
- dc.contributor.author Kostenis, Evi
- dc.contributor.author Martemyanov, Kirill A.
- dc.contributor.author Neubig, Rick R.
- dc.contributor.author Onaran, H. Ongun
- dc.contributor.author Rajagopal, Sudarshan
- dc.contributor.author Roth, Bryan L.
- dc.contributor.author Selent, Jana
- dc.contributor.author Shukla, Arun K.
- dc.contributor.author Sommer, Martha E.
- dc.contributor.author Gloriam, David E.
- dc.date.accessioned 2022-06-10T05:55:18Z
- dc.date.available 2022-06-10T05:55:18Z
- dc.date.issued 2022
- dc.description.abstract 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.
- dc.format.mimetype application/pdf
- dc.identifier.citation Kolb P, Kenakin T, Alexander SPH, Bermudez M, Bohn LM, Breinholt CS, Bouvier M, Hill SJ, Kostenis E, Martemyanov KA, Neubig RR, Onaran HO, Rajagopal S, Roth BL, Selent J, Shukla AK, Sommer ME, Gloriam DE. Community guidelines for GPCR ligand bias: IUPHAR review 32. Br J Pharmacol. 2022 Jul;179(14):3651-74. DOI: 10.1111/bph.15811
- dc.identifier.doi http://dx.doi.org/10.1111/bph.15811
- dc.identifier.issn 0007-1188
- dc.identifier.uri http://hdl.handle.net/10230/53439
- dc.language.iso eng
- dc.publisher Wiley
- dc.relation.ispartof Br J Pharmacol. 2022 Jul;179(14):3651-74
- dc.rights © 2022 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
- dc.rights.accessRights info:eu-repo/semantics/openAccess
- dc.rights.uri http://creativecommons.org/licenses/by/4.0/
- dc.title Community guidelines for GPCR ligand bias: IUPHAR review 32
- dc.type info:eu-repo/semantics/article
- dc.type.version info:eu-repo/semantics/publishedVersion