Literature DB >> 17700724

Pharmacological onomastics: what's in a name?

T P Kenakin1.   

Abstract

Drugs are named for their primary receptor target and overt action (agonism, antagonism) but the observation of multiple or collateral efficacies emanating from drugs activating a single receptor target is posing a challenge for drug classification and nomenclature. With increasing abilities to detect alteration in cellular function has come the identification of efficacies that are not necessarily manifest in obvious changes in cell response. Specifically, some agonists selectively activate cellular pathways, demonstrate phenotypic behaviour associated with cell type and some antagonists actively induce receptor internalization without activation. In addition, the effects of allosteric modulators can be linked to the nature of the co-binding ligand posing a similar complication in classification and naming. Thus, accurate labels for this new generation of selective drugs may require identification of receptor partners (G-protein type, beta-arrestin) or pathway or, in the case of allosteric modulators, identification of co-binding ligands. The association of distinct phenotypic behaviours with molecules opens the opportunity to better associate clinical effects with distinct pharmacological properties.

Mesh:

Substances:

Year:  2007        PMID: 17700724      PMCID: PMC2241801          DOI: 10.1038/sj.bjp.0707407

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  52 in total

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

Authors:  C Watson; G Chen; P Irving; J Way; W J Chen; T Kenakin
Journal:  Mol Pharmacol       Date:  2000-12       Impact factor: 4.436

2.  Receptor activity-independent recruitment of betaarrestin2 reveals specific signalling modes.

Authors:  Sonia Terrillon; Michel Bouvier
Journal:  EMBO J       Date:  2004-09-23       Impact factor: 11.598

Review 3.  What's next in translational medicine?

Authors:  Bruce H Littman; Linda Di Mario; Mario Plebani; Francesco M Marincola
Journal:  Clin Sci (Lond)       Date:  2007-02       Impact factor: 6.124

4.  Bombesin and substance P analogues differentially regulate G-protein coupling to the bombesin receptor. Direct evidence for biased agonism.

Authors:  A C MacKinnon; C Waters; D Jodrell; C Haslett; T Sethi
Journal:  J Biol Chem       Date:  2001-04-25       Impact factor: 5.157

Review 5.  Drug efficacy at G protein-coupled receptors.

Authors:  Terry Kenakin
Journal:  Annu Rev Pharmacol Toxicol       Date:  2002       Impact factor: 13.820

6.  Pharmacological proteus?

Authors:  T Kenakin
Journal:  Trends Pharmacol Sci       Date:  1995-08       Impact factor: 14.819

Review 7.  Agonist-receptor efficacy. II. Agonist trafficking of receptor signals.

Authors:  T Kenakin
Journal:  Trends Pharmacol Sci       Date:  1995-07       Impact factor: 14.819

8.  Chemically distinct ligands promote differential CB1 cannabinoid receptor-Gi protein interactions.

Authors:  Somnath Mukhopadhyay; Allyn C Howlett
Journal:  Mol Pharmacol       Date:  2005-03-04       Impact factor: 4.436

9.  Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors.

Authors:  Mounia Azzi; Pascale G Charest; Stéphane Angers; Guy Rousseau; Trudy Kohout; Michel Bouvier; Graciela Piñeyro
Journal:  Proc Natl Acad Sci U S A       Date:  2003-09-17       Impact factor: 11.205

10.  Achieving signalling selectivity of ligands for the corticotropin-releasing factor type 1 receptor by modifying the agonist's signalling domain.

Authors:  M Beyermann; N Heinrich; K Fechner; J Furkert; W Zhang; O Kraetke; M Bienert; H Berger
Journal:  Br J Pharmacol       Date:  2007-05-29       Impact factor: 8.739

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  13 in total

Review 1.  Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.

Authors:  Terry Kenakin; Laurence J Miller
Journal:  Pharmacol Rev       Date:  2010-04-14       Impact factor: 25.468

2.  Being mindful of seven-transmembrane receptor 'guests' when assessing agonist selectivity.

Authors:  Terry Kenakin
Journal:  Br J Pharmacol       Date:  2010-07       Impact factor: 8.739

Review 3.  Ensemble of G protein-coupled receptor active states.

Authors:  P S-H Park
Journal:  Curr Med Chem       Date:  2012       Impact factor: 4.530

4.  Identification of G protein-biased agonists that fail to recruit β-arrestin or promote internalization of the D1 dopamine receptor.

Authors:  Jennie L Conroy; R Benjamin Free; David R Sibley
Journal:  ACS Chem Neurosci       Date:  2015-02-20       Impact factor: 4.418

5.  Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor.

Authors:  R Benjamin Free; Lani S Chun; Amy E Moritz; Brittney N Miller; Trevor B Doyle; Jennie L Conroy; Adrian Padron; Julie A Meade; Jingbo Xiao; Xin Hu; Andrés E Dulcey; Yang Han; Lihua Duan; Steve Titus; Melanie Bryant-Genevier; Elena Barnaeva; Marc Ferrer; Jonathan A Javitch; Thijs Beuming; Lei Shi; Noel T Southall; Juan J Marugan; David R Sibley
Journal:  Mol Pharmacol       Date:  2014-04-22       Impact factor: 4.436

Review 6.  New concepts in pharmacological efficacy at 7TM receptors: IUPHAR review 2.

Authors:  Terry Kenakin
Journal:  Br J Pharmacol       Date:  2013-02       Impact factor: 8.739

7.  Morphine-like opiates selectively antagonize receptor-arrestin interactions.

Authors:  Paola Molinari; Vanessa Vezzi; Maria Sbraccia; Cristina Grò; Daniela Riitano; Caterina Ambrosio; Ida Casella; Tommaso Costa
Journal:  J Biol Chem       Date:  2010-02-26       Impact factor: 5.157

8.  Biased agonism.

Authors:  Terry Kenakin
Journal:  F1000 Biol Rep       Date:  2009-11-26

9.  Ligand-specific interactions modulate kinetic, energetic, and mechanical properties of the human β2 adrenergic receptor.

Authors:  Michael Zocher; Juan J Fung; Brian K Kobilka; Daniel J Müller
Journal:  Structure       Date:  2012-06-28       Impact factor: 5.006

10.  The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex.

Authors:  Xiao Jie Yao; Gisselle Vélez Ruiz; Matthew R Whorton; Søren G F Rasmussen; Brian T DeVree; Xavier Deupi; Roger K Sunahara; Brian Kobilka
Journal:  Proc Natl Acad Sci U S A       Date:  2009-05-22       Impact factor: 11.205

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