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; Neubig, Rick R.; Onaran, H. Ongun; Rajagopal, Sudarshan; Roth, Bryan L.; Selent, Jana; Shukla, Arun K.; Sommer, Martha E.; Gloriam, David E.

doi:10.1111/bph.15811

All Outputs (7)

Use of NanoBiT and NanoBRET to characterise interleukin-23 receptor dimer formation in living cells (2022)
Journal Article

Background and Purpose: Interleukin-23 (IL-23) and its receptor are important drug targets for the treatment of auto-inflammatory diseases. IL-23 binds to a receptor complex composed of two single transmembrane spanning proteins IL23R and IL12Rβ1. In... Read More about Use of NanoBiT and NanoBRET to characterise interleukin-23 receptor dimer formation in living cells.

Kinetic analysis of endogenous β2-adrenoceptor-mediated cAMP GloSensorTM responses in HEK293 cells (2022)
Journal Article

Background and Aim: Standard pharmacological analysis of agonist activity utilises measurements of receptor-mediated responses at a set time-point, or at the peak response level, to characterise ligands. However, the occurrence of non-equilibrium con... Read More about Kinetic analysis of endogenous β2-adrenoceptor-mediated cAMP GloSensorTM responses in HEK293 cells.

Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells (2022)
Journal Article

Introduction: The Epidermal Growth Factor Receptor is a member of the Erb receptor tyrosine kinase family. It binds several ligands including EGF, betacellulin (BTC) and TGF-α, controls cellular proliferation and invasion and is overexpressed in vari... Read More about Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells.

Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor (2022)
Journal Article

The histamine H1 receptor (H1R) has recently been implicated in mediating cell proliferation and cancer progression, therefore high affinity H1R-selective fluorescent ligands are desirable tools for further investigation of this behaviour in vitro an... Read More about Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor.

Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists (2022)
Journal Article

A2A and A2B adenosine receptors produce regionally selective regulation of vascular tone and elicit differing effects on mean arterial pressure (MAP), whilst inducing tachycardia. The tachycardia induced by the stimulation of A2A or A2B receptors has... Read More about Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists.

Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation (2022)
Journal Article

Adenosine is a local mediator that regulates changes in the cardiovascular system via activation of four G protein-coupled receptors (A1, A2A, A2B, A3). Here, we have investigated the effect of A2A and A2B-selective agonists on vasodilatation in thre... Read More about Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation.

Community guidelines for GPCR ligand bias: IUPHAR review 32 (2022)
Journal Article

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 requ... Read More about Community guidelines for GPCR ligand bias: IUPHAR review 32.