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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.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.issn 0007-1188
dc.identifier.uri http://hdl.handle.net/10230/53439
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.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.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.identifier.doi http://dx.doi.org/10.1111/bph.15811
dc.rights.accessRights info:eu-repo/semantics/openAccess
dc.type.version info:eu-repo/semantics/publishedVersion


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