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Cellular assays as portals to seven-transmembrane receptor-based drug discovery

Nature reviews. Drug discovery, 2009-08, Vol.8 (8), p.617-626

Kenakin, Terry P

2009

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7TM Receptor Allostery: Putting Numbers to Shapeshifting Proteins

Trends in pharmacological sciences (Regular ed.), 2009-09, Vol.30 (9), p.460-469

Kenakin, Terry P

2009

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International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands

Pharmacological reviews, 2014-10, Vol.66 (4), p.918-947

2014

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Biased signalling and allosteric machines: new vistas and challenges for drug discovery

British journal of pharmacology, 2012-03, Vol.165 (6), p.1659-1669

Kenakin, Terry P

2012

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Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7

Cell chemical biology, 2019-10, Vol.26 (10), p.1365-1379.e22

2019

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Refining efficacy: allosterism and bias in G protein-coupled receptor signaling

Methods in molecular biology (Clifton, N.J.), 2011, Vol.756, p.3

2011

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Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules

British journal of pharmacology, 2006-07, Vol.148 (5), p.619-628

2006

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Seven Transmembrane Receptors as Nature's Prototype Allosteric Protein: De-emphasizing the Geography of Binding

Molecular pharmacology, 2008-09, Vol.74 (3), p.541-543

Kenakin, Terry P

2008

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Synoptic pharmacology: Detecting and assessing the pharmacological significance of ligands for orphan receptors

Pharmacological research, 2016-12, Vol.114, p.284-290

Kenakin, Terry P.

2016

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Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor

Medicinal research reviews, 2017-05, Vol.37 (3), p.441-474

2017

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Interdependent allosteric free fatty acid receptor 2 modulators synergistically induce functional selective activation and desensitization in neutrophils

Biochimica et biophysica acta. Molecular cell research, 2020-06, Vol.1867 (6), p.118689, Article 118689

2020

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Neutrophil priming that turns natural FFA2R agonists into potent activators of the superoxide generating NADPH‐oxidase

Journal of leukocyte biology, 2018-12, Vol.104 (6), p.1117-1132

2018

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Ligand Detection in the Allosteric World

Journal of biomolecular screening, 2010-02, Vol.15 (2), p.119-130

Kenakin, Terry P.

2010

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Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68)

Journal of medicinal chemistry, 2019-08, Vol.62 (16), p.7557-7574

2019

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Development of 3‑(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type‑1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior

Journal of medicinal chemistry, 2022-01, Vol.65 (1), p.257-270

2022

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Editors in Chief Overview

Current opinion in pharmacology, 2017-08, Vol.35, p.iv-v

2017

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Structure–activity relationships of substituted 1H-indole-2-carboxamides as CB1 receptor allosteric modulators

Bioorganic & medicinal chemistry, 2015-05, Vol.23 (9), p.2195-2203

2015

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In memory of Norman Bowery (1944–2016)

Current opinion in pharmacology, 2017-08, Vol.35, p.89-93

2017

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Detailed Characterization of the In Vitro Pharmacological and Pharmacokinetic Properties of N -(2-Hydroxybenzyl)-2,5-Dimethoxy-4-Cyanophenylethylamine (25CN-NBOH), a Highly Selective and Brain-Penetrant 5-HT 2A Receptor Agonist

The Journal of pharmacology and experimental therapeutics, 2017-06, Vol.361 (3), p.441-453

2017

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Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

Pharmacological reviews, 2010-06, Vol.62 (2), p.265-304

2010

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The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

Molecular pharmacology, 2009-03, Vol.75 (3), p.490-501

2009

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Diarylureas Containing 5-Membered Heterocycles as CB 1 Receptor Allosteric Modulators: Design, Synthesis, and Pharmacological Evaluation

ACS chemical neuroscience, 2019-01, Vol.10 (1), p.518-527

2019

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Diarylureas Containing 5‑Membered Heterocycles as CB1 Receptor Allosteric Modulators: Design, Synthesis, and Pharmacological Evaluation

ACS chemical neuroscience, 2019-01, Vol.10 (1), p.518-527

2019

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New eyes to see texture in ligand efficacy

Nature methods, 2005-03, Vol.2 (3), p.163-164

Kenakin, Terry P

2005

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Peptide, Peptidomimetic and Small-molecule Drug Discovery Targeting HIV-1 Host-cell Attachment and Entry through gp120, gp41, CCR5 and CXCR4

Chemical biology & drug design, 2006-01, Vol.67 (1), p.13-26

2006

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Cellular assays as portals to seven-transmembrane receptor-based drug discovery

7TM Receptor Allostery: Putting Numbers to Shapeshifting Proteins

International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands

Biased signalling and allosteric machines: new vistas and challenges for drug discovery

Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7

Refining efficacy: allosterism and bias in G protein-coupled receptor signaling

Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules

Seven Transmembrane Receptors as Nature's Prototype Allosteric Protein: De-emphasizing the Geography of Binding

Synoptic pharmacology: Detecting and assessing the pharmacological significance of ligands for orphan receptors

Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor

Interdependent allosteric free fatty acid receptor 2 modulators synergistically induce functional selective activation and desensitization in neutrophils

Neutrophil priming that turns natural FFA2R agonists into potent activators of the superoxide generating NADPH‐oxidase

Ligand Detection in the Allosteric World

Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68)

Development of 3‑(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type‑1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior

Editors in Chief Overview

Structure–activity relationships of substituted 1H-indole-2-carboxamides as CB1 receptor allosteric modulators

In memory of Norman Bowery (1944–2016)

Detailed Characterization of the In Vitro Pharmacological and Pharmacokinetic Properties of N -(2-Hydroxybenzyl)-2,5-Dimethoxy-4-Cyanophenylethylamine (25CN-NBOH), a Highly Selective and Brain-Penetrant 5-HT 2A Receptor Agonist

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

Diarylureas Containing 5-Membered Heterocycles as CB 1 Receptor Allosteric Modulators: Design, Synthesis, and Pharmacological Evaluation

Diarylureas Containing 5‑Membered Heterocycles as CB1 Receptor Allosteric Modulators: Design, Synthesis, and Pharmacological Evaluation

New eyes to see texture in ligand efficacy

Peptide, Peptidomimetic and Small-molecule Drug Discovery Targeting HIV-1 Host-cell Attachment and Entry through gp120, gp41, CCR5 and CXCR4

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