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Structure-based discovery of pyrazolamides as novel ERRγ inverse agonists

European journal of medicinal chemistry, 2023-03, Vol.250, p.115174-115174, Article 115174

2023

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Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity

The international journal of neuropsychopharmacology, 2018-10, Vol.21 (10), p.962-977

2018

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Design and Optimization of 1 H -1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16829-16859

2022

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Virtual discovery of melatonin receptor ligands to modulate circadian rhythms

Nature (London), 2020-03, Vol.579 (7800), p.609-614

2020

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Histamine H 3 receptor antagonists/inverse agonists: Where do they go?

Pharmacology & therapeutics (Oxford), 2019-08, Vol.200, p.69

2019

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Transformation of a Dopamine D 2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents

Journal of medicinal chemistry, 2023-05, Vol.66 (9), p.6274-6287

2023

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Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

Nature (London), 2016-03, Vol.531 (7594), p.335-340

2016

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Cannabinoid Receptors: Where They are and What They do

Journal of neuroendocrinology, 2008-05, Vol.20 (s1), p.10-14

Mackie, K.

2008

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(Inverse) Agonists of Retinoic Acid-Related Orphan Receptor γ: Regulation of Immune Responses, Inflammation, and Autoimmune Disease

Annual review of pharmacology and toxicology, 2020-01, Vol.60, p.371

2020

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Current topics in angiotensin II type 1 receptor research: Focus on inverse agonism, receptor dimerization and biased agonism

Pharmacological research, 2017-09, Vol.123, p.40-50

2017

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Late-stage oxidative C(sp 3 )-H methylation

Nature (London), 2020-04, Vol.580 (7805), p.621-627

2020

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Backbone Modification Provides a Long-Acting Inverse Agonist of Pathogenic, Constitutively Active PTH1R Variants

Journal of the American Chemical Society, 2024-03, Vol.146 (10), p.6522-6529

2024

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Turn On, Tune In, Turnover! Target Biology Impacts In Vivo Potency, Efficacy, and Clearance

Pharmacological reviews, 2023-05, Vol.75 (3), p.416-462

2023

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Structure, function and pharmacology of human itch GPCRs

Nature (London), 2021-12, Vol.600 (7887), p.170-175

2021

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An Inverse Agonist GSK5182 Increases Protein Stability of the Orphan Nuclear Receptor ERRγ via Inhibition of Ubiquitination

International journal of molecular sciences, 2022-12, Vol.24 (1), p.96

2022

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Preliminary studies of 1,5-benzoxazepine derivatives as potential histamine H 3 receptor antagonists

Future medicinal chemistry, 2024-02, Vol.16 (3), p.197-204

2024

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Peripheral Cannabinoid-1 Receptor Inverse Agonism Reduces Obesity by Reversing Leptin Resistance

Cell metabolism, 2012-08, Vol.16 (2), p.167-179

2012

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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists

Bioorganic & medicinal chemistry, 2023-01, Vol.78, p.117130-117130, Article 117130

2023

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In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A 2A Receptor Antagonist/Inverse Agonist

Molecular pharmacology, 2023-06, Vol.103 (6), p.311

2023

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GPR3 and GPR6, novel molecular targets for cannabidiol

Biochemical and biophysical research communications, 2017-08, Vol.490 (1), p.17-21

2017

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Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Nature (London), 2011-05, Vol.474 (7352), p.521-525

2011

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Constitutive activity of the dopamine (D 5 ) receptor, highly expressed in CA1 hippocampal neurons, selectively reduces Ca V 3.2 and Ca V 3.3 currents

British journal of pharmacology, 2023-05, Vol.180 (9), p.1210-1231

2023

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Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets

Biochemical pharmacology, 2017-03, Vol.128, p.1-11

2017

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GPR3, GPR6, and GPR12 as novel molecular targets: their biological functions and interaction with cannabidiol

Acta pharmacologica Sinica, 2019-03, Vol.40 (3), p.300-308

2019

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Modulators of the Nuclear Receptor Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc)

Journal of medicinal chemistry, 2014-07, Vol.57 (14), p.5871-5892

2014

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Structure-based discovery of pyrazolamides as novel ERRγ inverse agonists

Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity

Design and Optimization of 1 H -1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

Virtual discovery of melatonin receptor ligands to modulate circadian rhythms

Histamine H 3 receptor antagonists/inverse agonists: Where do they go?

Transformation of a Dopamine D 2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

Cannabinoid Receptors: Where They are and What They do

(Inverse) Agonists of Retinoic Acid-Related Orphan Receptor γ: Regulation of Immune Responses, Inflammation, and Autoimmune Disease

Current topics in angiotensin II type 1 receptor research: Focus on inverse agonism, receptor dimerization and biased agonism

Late-stage oxidative C(sp 3 )-H methylation

Backbone Modification Provides a Long-Acting Inverse Agonist of Pathogenic, Constitutively Active PTH1R Variants

Turn On, Tune In, Turnover! Target Biology Impacts In Vivo Potency, Efficacy, and Clearance

Structure, function and pharmacology of human itch GPCRs

An Inverse Agonist GSK5182 Increases Protein Stability of the Orphan Nuclear Receptor ERRγ via Inhibition of Ubiquitination

Preliminary studies of 1,5-benzoxazepine derivatives as potential histamine H 3 receptor antagonists

Peripheral Cannabinoid-1 Receptor Inverse Agonism Reduces Obesity by Reversing Leptin Resistance

Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists

In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A 2A Receptor Antagonist/Inverse Agonist

GPR3 and GPR6, novel molecular targets for cannabidiol

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Constitutive activity of the dopamine (D 5 ) receptor, highly expressed in CA1 hippocampal neurons, selectively reduces Ca V 3.2 and Ca V 3.3 currents

Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets

GPR3, GPR6, and GPR12 as novel molecular targets: their biological functions and interaction with cannabidiol

Modulators of the Nuclear Receptor Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc)

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