Community guidelines for GPCR ligand bias: IUPHAR review 32
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Community guidelines for GPCR ligand bias : IUPHAR review 32. / Kolb, Peter; Kenakin, Terry; Alexander, Stephen P.H.; Bermudez, Marcel; Bohn, Laura M.; Breinholt, Christian S.; Bouvier, Michel; Hill, Stephen J.; Kostenis, Evi; Martemyanov, Kirill A.; Neubig, Rick R.; Onaran, H. Ongun; Rajagopal, Sudarshan; Roth, Bryan L.; Selent, Jana; Shukla, Arun K.; Sommer, Martha E.; Gloriam, David E.
In: British Journal of Pharmacology, Vol. 179, No. 14, 2022, p. 3651-3674.Research output: Contribution to journal › Review › Research › peer-review
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TY - JOUR
T1 - Community guidelines for GPCR ligand bias
T2 - IUPHAR review 32
AU - Kolb, Peter
AU - Kenakin, Terry
AU - Alexander, Stephen P.H.
AU - Bermudez, Marcel
AU - Bohn, Laura M.
AU - Breinholt, Christian S.
AU - Bouvier, Michel
AU - Hill, Stephen J.
AU - Kostenis, Evi
AU - Martemyanov, Kirill A.
AU - Neubig, Rick R.
AU - Onaran, H. Ongun
AU - Rajagopal, Sudarshan
AU - Roth, Bryan L.
AU - Selent, Jana
AU - Shukla, Arun K.
AU - Sommer, Martha E.
AU - Gloriam, David E.
N1 - Themed Issue: Structure Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary)
PY - 2022
Y1 - 2022
N2 - 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.
AB - 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.
U2 - 10.1111/bph.15811
DO - 10.1111/bph.15811
M3 - Review
C2 - 35106752
AN - SCOPUS:85127292425
VL - 179
SP - 3651
EP - 3674
JO - British Journal of Pharmacology
JF - British Journal of Pharmacology
SN - 0007-1188
IS - 14
ER -
ID: 303173212