Literature DB >> 23681006

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

Sudarshan Rajagopal.   

Abstract

Mesh：

Year:  2013        PMID： 23681006     DOI： 10.1038/nrd3954-c1

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


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  9 in total

1.  A modification of receptor theory.

Authors:  R P STEPHENSON
Journal:  Br J Pharmacol Chemother       Date:  1956-12

2.  Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory.

Authors:  E J ARIENS
Journal:  Arch Int Pharmacodyn Ther       Date:  1954-09-01

3.  Quantifying ligand bias at seven-transmembrane receptors.

Authors:  Sudarshan Rajagopal; Seungkirl Ahn; David H Rominger; William Gowen-MacDonald; Christopher M Lam; Scott M Dewire; Jonathan D Violin; Robert J Lefkowitz
Journal:  Mol Pharmacol       Date:  2011-05-24       Impact factor: 4.436

4.  The cubic ternary complex receptor-occupancy model. III. resurrecting efficacy.

Authors:  J M Weiss; P H Morgan; M W Lutz; T P Kenakin
Journal:  J Theor Biol       Date:  1996-08-21       Impact factor: 2.691

5.  A simple method for quantifying functional selectivity and agonist bias.

Authors:  Terry Kenakin; Christian Watson; Vanessa Muniz-Medina; Arthur Christopoulos; Steven Novick
Journal:  ACS Chem Neurosci       Date:  2011-12-20       Impact factor: 4.418

Review 6.  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

7.  Operational models of pharmacological agonism.

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

8.  A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

Authors:  P Samama; S Cotecchia; T Costa; R J Lefkowitz
Journal:  J Biol Chem       Date:  1993-03-05       Impact factor: 5.157

9.  A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.

Authors:  A De Lean; J M Stadel; R J Lefkowitz
Journal:  J Biol Chem       Date:  1980-08-10       Impact factor: 5.157
  9 in total
  16 in total

Review 1.  Superagonism at G protein-coupled receptors and beyond.

Authors:  R Schrage; A De Min; K Hochheiser; E Kostenis; K Mohr
Journal:  Br J Pharmacol       Date:  2015-10-24       Impact factor: 8.739

2.  Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.

Authors:  Zhan-Guo Gao; Ramachandran Balasubramanian; Evgeny Kiselev; Qiang Wei; Kenneth A Jacobson
Journal:  Biochem Pharmacol       Date:  2014-05-20       Impact factor: 5.858

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

Authors:  Tarsis F Brust; Michael P Hayes; David L Roman; Kevin D Burris; Val J Watts
Journal:  J Pharmacol Exp Ther       Date:  2014-12-24       Impact factor: 4.030

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

Authors:  Edward L Stahl; Lei Zhou; Frederick J Ehlert; Laura M Bohn
Journal:  Mol Pharmacol       Date:  2015-02-13       Impact factor: 4.436

Review 5.  Pancreatic islet inflammation: an emerging role for chemokines.

Authors:  J Jason Collier; Tim E Sparer; Michael D Karlstad; Susan J Burke
Journal:  J Mol Endocrinol       Date:  2017-04-18       Impact factor: 5.098

6.  Measurements of ligand bias and functional affinity.

Authors:  Terry Kenakin; Arthur Christopoulos
Journal:  Nat Rev Drug Discov       Date:  2013-05-17       Impact factor: 84.694

Review 7.  Identifying ligand-specific signalling within biased responses: focus on δ opioid receptor ligands.

Authors:  I Charfi; N Audet; H Bagheri Tudashki; G Pineyro
Journal:  Br J Pharmacol       Date:  2014-07-01       Impact factor: 8.739

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

Authors:  Xiao Zhu; David B Finlay; Michelle Glass; Stephen B Duffull
Journal:  Br J Pharmacol       Date:  2018-03-30       Impact factor: 8.739

Review 9.  Biased signalling: from simple switches to allosteric microprocessors.

Authors:  Jeffrey S Smith; Robert J Lefkowitz; Sudarshan Rajagopal
Journal:  Nat Rev Drug Discov       Date:  2018-01-05       Impact factor: 84.694

10.  Structure-based discovery of opioid analgesics with reduced side effects.

Authors:  Aashish Manglik; Henry Lin; Dipendra K Aryal; John D McCorvy; Daniela Dengler; Gregory Corder; Anat Levit; Ralf C Kling; Viachaslau Bernat; Harald Hübner; Xi-Ping Huang; Maria F Sassano; Patrick M Giguère; Stefan Löber; Grégory Scherrer; Brian K Kobilka; Peter Gmeiner; Bryan L Roth; Brian K Shoichet
Journal:  Nature       Date:  2016-08-17       Impact factor: 49.962
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