The potential for selective pharmacological therapies through biased receptor signaling (original) (raw)

How can we improve the measurement of receptor signaling bias

Karim Nagi

Expert Opinion on Drug Discovery, 2023

A pluridimensional view of biased agonism

Michel Bouvier

Molecular Pharmacology, 2016

Faculty Opinions recommendation of Biased agonism: An emerging paradigm in GPCR drug discovery

Marcin Chwistek

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature, 2017

A Novel Method for Analyzing Extremely Biased Agonism at G Protein-Coupled Receptors

Frederick Ehlert

Molecular pharmacology, 2015

Fulfilling the Promise of "Biased" G Protein–Coupled Receptor Agonism

Stuart Maudsley

Molecular Pharmacology, 2015

A pharmacological primer of biased agonism

Bradley Andresen

Biased agonism

F1000 biology reports, 2009

Faculty of 1000 evaluation for Biased agonism: An emerging paradigm in GPCR drug discovery

Marcin Chwistek

F1000 - Post-publication peer review of the biomedical literature

Translating in vitro ligand bias into in vivo efficacy

Stuart Maudsley

Cellular Signalling, 2017

A Complementary Scale of Biased Agonism for Agonists with Differing Maximal Responses

Scientific reports, 2017

Systematic errors in detecting biased agonism: Analysis of current methods and development of a new model-free approach

Ongun Onaran

Scientific reports, 2017

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

ACS Chemical Neuroscience, 2012

Can Adding Constitutive Receptor Activity Redefine Biased Signaling Quantification?

Trends in Pharmacological Sciences, 2019

Quantification of Ligand Bias for Clinically Relevant 2-Adrenergic Receptor Ligands: Implications for Drug Taxonomy

Michel Bouvier

Molecular Pharmacology, 2014

Recent developments in biased agonism

Alex Thomsen

2014

Practical guide for calculating and representing biased signaling by GPCR ligands: A stepwise approach.

Karim Nagi

Methods, 2016

A method for the quantification of biased signalling at constitutively active receptors

British journal of pharmacology, 2018

Challenges and Opportunities in Drug Discovery of Biased Ligands

Jana Selent

Methods in Molecular Biology, 2017

Quantifying Ligand Bias at Seven-Transmembrane Receptors

Sudarshan Rajagopal

Molecular Pharmacology, 2011

BiasNet: A model to predict ligand bias towards GPCR signaling

JULIAN FRANCO

2021

Agonist-receptor efficacy I: mechanisms of efficacy and receptor promiscuity

Trends in Pharmacological Sciences, 1995

Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors

Jolien De Neve

RSC Medicinal Chemistry, 2021

Estimation of the receptor-state affinity constants of ligands in functional studies using wild type and constitutively active mutant receptors: Implications for estimation of agonist bias

Frederick Ehlert

Journal of pharmacological and toxicological methods

Beyond Receptor Expression Levels: The Relevance of Target Accessibility in Ligand-Directed Pharmacodelivery Systems

Wadih Arap

Trends in Cardiovascular Medicine, 2008

Identifying Functional Hotspot Residues for Biased Ligand Design in G-Protein-Coupled Receptors

Christofer Tautermann

Molecular pharmacology, 2018

Collateral efficacy in new drug discovery

2007

The measurement of efficacy in the drug discovery agonist selection process

Journal of Pharmacological and Toxicological Methods, 1999

Fulfilling the Promise of 'Biased' GPCR Agonism

Stuart Maudsley

Molecular pharmacology, 2015

The use of stimulus-biased assay systems to detect agonist-specific receptor active states: implications for the trafficking of receptor stimulus by agonists

Molecular pharmacology, 2000

The role of kinetic context in apparent biased agonism at GPCRs

Ben Capuano

Nature Communications, 2016

Being mindful of seven-transmembrane receptor ‘guests’ when assessing agonist selectivity

British Journal of Pharmacology, 2010

Agonist induction, conformational selection, and mutant receptors

FEBS Letters, 2004

Quantification of Ligand Bias for Clinically Relevant β2-Adrenergic Receptor Ligands: Implications for Drug Taxonomy

Emma Van Der Westhuizen

Molecular Pharmacology, 2013

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays

Steven Charlton

British Journal of Pharmacology, 2010