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Literature DB >> 23681003

Measurements of ligand bias and functional affinity.

Terry Kenakin, Arthur Christopoulos.

Abstract

Mesh：

Year: 2013 PMID： 23681003 DOI： 10.1038/nrd3954-c2

Source DB: PubMed Journal: Nat Rev Drug Discov ISSN： 1474-1776 Impact factor: 84.694

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9 in total

Review 1. Signalling bias in new drug discovery: detection, quantification and therapeutic impact.

Authors: Terry Kenakin; Arthur Christopoulos
Journal: Nat Rev Drug Discov Date: 2012-02-15 Impact factor: 84.694

2. Quantifying biased agonism: understanding the links between affinity and efficacy.

Authors: Sudarshan Rajagopal
Journal: Nat Rev Drug Discov Date: 2013-05-17 Impact factor: 84.694

3. Divergent agonist selectivity in activating β1- and β2-adrenoceptors for G-protein and arrestin coupling.

Authors: Ida Casella; Caterina Ambrosio; Maria Cristina Grò; Paola Molinari; Tommaso Costa
Journal: Biochem J Date: 2011-08-15 Impact factor: 3.857

4. Operational models of pharmacological agonism.

Authors: J W Black; P Leff
Journal: Proc R Soc Lond B Biol Sci Date: 1983-12-22

5. Structure of a nanobody-stabilized active state of the β(2) adrenoceptor.

Authors: Søren G F Rasmussen; Hee-Jung Choi; Juan Jose Fung; Els Pardon; Paola Casarosa; Pil Seok Chae; Brian T Devree; Daniel M Rosenbaum; Foon Sun Thian; Tong Sun Kobilka; Andreas Schnapp; Ingo Konetzki; Roger K Sunahara; Samuel H Gellman; Alexander Pautsch; Jan Steyaert; William I Weis; Brian K Kobilka
Journal: Nature Date: 2011-01-13 Impact factor: 49.962

6. Galpha-subunits differentially alter the conformation and agonist affinity of kappa-opioid receptors.

Authors: Feng Yan; Philip D Mosier; Richard B Westkaemper; Bryan L Roth
Journal: Biochemistry Date: 2008-01-19 Impact factor: 3.162

7. An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation.

Authors: J W Black; P Leff; N P Shankley; J Wood
Journal: Br J Pharmacol Date: 1985-02 Impact factor: 8.739

8. Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15.

Authors: Michael T Griffin; Katherine W Figueroa; Sarah Liller; Frederick J Ehlert
Journal: J Pharmacol Exp Ther Date: 2007-03-28 Impact factor: 4.030

9. Crystal structure of the β2 adrenergic receptor-Gs protein complex.

Authors: Søren G F Rasmussen; Brian T DeVree; Yaozhong Zou; Andrew C Kruse; Ka Young Chung; Tong Sun Kobilka; Foon Sun Thian; Pil Seok Chae; Els Pardon; Diane Calinski; Jesper M Mathiesen; Syed T A Shah; Joseph A Lyons; Martin Caffrey; Samuel H Gellman; Jan Steyaert; Georgios Skiniotis; William I Weis; Roger K Sunahara; Brian K Kobilka
Journal: Nature Date: 2011-07-19 Impact factor: 49.962

9 in total

25 in total

1. Identification of the first biased NPS receptor agonist that retains anxiolytic and memory promoting effects with reduced levels of locomotor stimulation.

Authors: Stewart D Clark; Terrence P Kenakin; Steven Gertz; Carla Hassler; Elaine A Gay; Tiffany L Langston; Rainer K Reinscheid; Scott P Runyon
Journal: Neuropharmacology Date: 2017-03-03 Impact factor: 5.250

Measurements of ligand bias and functional affinity.

Review 1. Signalling bias in new drug discovery: detection, quantification and therapeutic impact.

2. Quantifying biased agonism: understanding the links between affinity and efficacy.

3. Divergent agonist selectivity in activating β1- and β2-adrenoceptors for G-protein and arrestin coupling.

4. Operational models of pharmacological agonism.

5. Structure of a nanobody-stabilized active state of the β(2) adrenoceptor.

6. Galpha-subunits differentially alter the conformation and agonist affinity of kappa-opioid receptors.

7. An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation.

8. Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15.

9. Crystal structure of the β2 adrenergic receptor-Gs protein complex.

1. Identification of the first biased NPS receptor agonist that retains anxiolytic and memory promoting effects with reduced levels of locomotor stimulation.

2. Bias analyses of preclinical and clinical D2 dopamine ligands: studies with immediate and complex signaling pathways.

3. A novel method for analyzing extremely biased agonism at G protein-coupled receptors.

Review 4. Identifying ligand-specific signalling within biased responses: focus on δ opioid receptor ligands.

Review 5. Molecular Pharmacology of δ-Opioid Receptors.

6. An evaluation of the operational model when applied to quantify functional selectivity.

Review 7. Biased signalling: from simple switches to allosteric microprocessors.

Review 8. Biased agonism: An emerging paradigm in GPCR drug discovery.

Review 9. Biased GPCR signaling: Possible mechanisms and inherent limitations.

10. Divergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR).