The role of kinetic context in apparent biased agonism at GPCRs

The role of kinetic context in apparent biased agonism at GPCRs

Biased agonism describes the ability of ligands to stabilize different conformations of a GPCR linked to distinct functional outcomes and offers the prospect of designing pathway-specific drugs that avoid on-target side effects. This mechanism is usually inferred from pharmacological data with the a...

Full description

Bibliographic Details
Main Authors:	Klein Herenbrink, Carmen, Sykes, David A., Donthamsetti, Prashant, Canals, Meritxell, Coudrat, Thomas, Shonberg, Jeremy, Scammells, Peter J., Capuano, Ben, Sexton, Patrick M., Charlton, Steven J., Javitch, Jonathan A., Christopoulos, Arthur, Lane, J. Robert
Format:	Online
Language:	English
Published:	Nature Publishing Group 2016
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4770093/

Similar Items

The role of kinetic context in apparent biased agonism at GPCRs
by: Klein Herenbrink, Carmen, et al.
Published: (2016)

Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand
by: Mistry, Shailesh N., et al.
Published: (2015)

A new mechanism of allostery in a G protein-coupled receptor dimer
by: Lane, J. Robert, et al.
Published: (2014)

Biased agonism in drug discovery: is it too soon to choose a path?
by: Michel, Martin C., et al.
Published: (2018)

The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism
by: Wootten, Denise, et al.
Published: (2016)

A Pharmacological Primer of Biased Agonism
by: Andresen, Bradley T
Published: (2011)

Structure–activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor
by: Shonberg, Jeremy, et al.
Published: (2015)

Reply to ‘Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects’
by: David A. Sykes, et al.
Published: (2018-09-01)

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor
by: Mistry, Shailesh N., et al.
Published: (2013)

Biased Agonism of Three Different Cannabinoid Receptor Agonists in Mouse Brain Cortex
by: Diez-Alarcia, Rebeca, et al.
Published: (2016)

Agonizing Hedgehog
by: Weitzman, Jonathan B
Published: (2002)

Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor
by: Wootten, Denise, et al.
Published: (2016)

Neuropeptide GPCRs in C. elegans
by: Frooninckx, Lotte, et al.
Published: (2012)

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics
by: Cook, A.E., et al.
Published: (2014)

Illuminating the life of GPCRs
by: Böhme, Ilka, et al.
Published: (2009)

The folding interactome of GPCRs
by: Bergmayr, Christian, et al.
Published: (2011)

Agonism and Antagonism at the Insulin Receptor
by: Knudsen, Louise, et al.
Published: (2012)

Neuropeptide GPCRs in Neuroendocrinology
by: Vaudry, Hubert, et al.
Published: (2014)

Why endosomes recycle GPCRs
by: Leslie, Mitch
Published: (2016)

Connecting inflammation with glutamate agonism in suicidality
by: Erhardt, Sophie, et al.
Published: (2013)

Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2016)

4-Phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2015)

Testing for partial agonism of the aryl hydrocarbon receptor
by: Wall, Richard J.
Published: (2008)

Low Affinity GPCRs for Metabolic Intermediates: Challenges for Pharmacologists
by: Smith, Nicola J.
Published: (2012)

Inverse agonism and its therapeutic significance
by: Khilnani, Gurudas, et al.
Published: (2011)

Membrane Driven Spatial Organization of GPCRs
by: Mondal, Sayan, et al.
Published: (2013)

Novel Therapeutic GPCRs for Psychiatric Disorders
by: Komatsu, Hidetoshi
Published: (2015)

Advancements in therapeutically targeting orphan GPCRs
by: Stockert, Jennifer A., et al.
Published: (2015)

Russian agon and the quest for theoretical sociology
by: Sergey B., Kulikov
Published: (2017)

Editorial: The Physiology and Pharmacology of Leucine-rich Repeat GPCRs
by: Arey, Brian J., et al.
Published: (2016)

Super-complexes of adhesion GPCRs and neural guidance receptors
by: Jackson, Verity A., et al.
Published: (2016)

The future of EPAC-targeted therapies: agonism versus antagonism
by: Parnell, Euan, et al.
Published: (2015)

Application of BRET to monitor ligand binding to GPCRs
by: Stoddart, Leigh A., et al.
Published: (2015)

Application of BRET to monitor ligand binding to GPCRs
by: Stoddart, Leigh A, et al.
Published: (2015)

A database for G proteins and their interaction with GPCRs
by: Elefsinioti, Antigoni L, et al.
Published: (2004)

The Origin of GPCRs: Identification of Mammalian like Rhodopsin, Adhesion, Glutamate and Frizzled GPCRs in Fungi
by: Krishnan, Arunkumar, et al.
Published: (2012)

G Protein-Coupled Receptors (GPCRs) in Alzheimer’s Disease: A Focus on BACE1 Related GPCRs
by: Zhao, Juan, et al.
Published: (2016)

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)

Conformational signatures in β-arrestin2 reveal natural biased agonism at a G-protein-coupled receptor
by: Arfaxad Reyes-Alcaraz, et al.
Published: (2018-09-01)