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Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells

PloS one, 2012-10, Vol.7 (10), p.e47662-e47662

2012

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Selexipag: An Oral and Selective IP Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension

Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7128-7137

2015

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The Antifibrotic Activity of Prostacyclin Receptor Agonism Is Mediated through Inhibition of YAP/TAZ

American journal of respiratory cell and molecular biology, 2019-05, Vol.60 (5), p.578-591

2019

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The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468

The Journal of pharmacology and experimental therapeutics, 2017-09, Vol.362 (3), p.489

2017

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Evaluation of tert-Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities

ChemMedChem, 2015-03, Vol.10 (3), p.461-469

2015

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Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist

The Journal of pharmacology and experimental therapeutics, 2008-12, Vol.327 (3), p.736

2008

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GPCR-induced YAP activation sensitizes fibroblasts to profibrotic activity of TGFβ1

PloS one, 2020-02, Vol.15 (2), p.e0228195-e0228195

2020

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From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

Bioorganic & medicinal chemistry letters, 2016-08, Vol.26 (15), p.3381-3394

2016

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FTY720 Phosphate Activates Sphingosine-1-Phosphate Receptor 2 and Selectively Couples to Gα12/13/Rho/ROCK to Induce Myofibroblast Contraction

Molecular pharmacology, 2015-06, Vol.87 (6), p.916-927

2015

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Novel high-throughput myofibroblast assays identify agonists with therapeutic potential in pulmonary fibrosis that act via EP2 and EP4 receptors

PloS one, 2018-11, Vol.13 (11), p.e0207872-e0207872

2018

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Ancestral Antibiotic Resistance in Mycobacterium tuberculosis

Proceedings of the National Academy of Sciences - PNAS, 2005-08, Vol.102 (34), p.12200-12205

2005

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Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis

PloS one, 2014-09, Vol.9 (9), p.e107809

2014

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Orexin Receptor Antagonists: A New Concept In CNS Disorders?

ChemMedChem, 2010-08, Vol.5 (8), p.1197-1214

2010

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Hijacking the host: survival of pathogenic mycobacteria inside macrophages

Trends in Microbiology, 2002-03, Vol.10 (3), p.142-146

2002

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Structure-Activity Relationship, Biological, and Pharmacological Characterization of the Proline Sulfonamide ACT-462206: a Potent, Brain-Penetrant Dual Orexin 1/Orexin 2 Receptor Antagonist

ChemMedChem, 2014-11, Vol.9 (11), p.2486-2496

2014

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Structure–activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2

Bioorganic & medicinal chemistry letters, 2013-07, Vol.23 (13), p.3857-3863

2013

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Synthesis, structure–activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (7), p.2212-2216

2013

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Sphingosine 1-Phosphate (S1P) Receptor Agonists Mediate Pro-fibrotic Responses in Normal Human Lung Fibroblasts via S1P2 and S1P3 Receptors and Smad-independent Signaling

The Journal of biological chemistry, 2013-05, Vol.288 (21), p.14839-14851

2013

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Essential Role for Cholesterol in Entry of Mycobacteria into Macrophages

Science (American Association for the Advancement of Science), 2000-06, Vol.288 (5471), p.1647-1650

2000

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Essential role for cholesterol in the delivery of exogenous antigens to the MHC class I-presentation pathway

International immunology, 2006-05, Vol.18 (5), p.755-765

2006

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Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist

ChemMedChem, 2013-06, Vol.8 (6), p.898-903

2013

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Discovery of Nivasorexant (ACT-539313): The First Selective Orexin‑1 Receptor Antagonist (SO1RA) Investigated in Clinical Trials

Journal of medicinal chemistry, 2024-02, Vol.67 (4), p.2337-2348

2024

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The metabolism of the dual orexin receptor antagonist daridorexant

Xenobiotica, 2023-03, Vol.53 (3), p.173-183

2023

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059 Daridorexant: A dual, equipotent, and insurmountable antagonist of both orexin-1 and orexin-2 receptors

Sleep (New York, N.Y.), 2021-05, Vol.44 (Supplement_2), p.A25-A25

2021

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Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells

Selexipag: An Oral and Selective IP Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension

The Antifibrotic Activity of Prostacyclin Receptor Agonism Is Mediated through Inhibition of YAP/TAZ

The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468

Evaluation of tert-Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities

Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist

GPCR-induced YAP activation sensitizes fibroblasts to profibrotic activity of TGFβ1

From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

FTY720 Phosphate Activates Sphingosine-1-Phosphate Receptor 2 and Selectively Couples to Gα12/13/Rho/ROCK to Induce Myofibroblast Contraction

Novel high-throughput myofibroblast assays identify agonists with therapeutic potential in pulmonary fibrosis that act via EP2 and EP4 receptors

Ancestral Antibiotic Resistance in Mycobacterium tuberculosis

Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis

Orexin Receptor Antagonists: A New Concept In CNS Disorders?

Hijacking the host: survival of pathogenic mycobacteria inside macrophages

Structure-Activity Relationship, Biological, and Pharmacological Characterization of the Proline Sulfonamide ACT-462206: a Potent, Brain-Penetrant Dual Orexin 1/Orexin 2 Receptor Antagonist

Structure–activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2

Synthesis, structure–activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1

Sphingosine 1-Phosphate (S1P) Receptor Agonists Mediate Pro-fibrotic Responses in Normal Human Lung Fibroblasts via S1P2 and S1P3 Receptors and Smad-independent Signaling

Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies

Essential Role for Cholesterol in Entry of Mycobacteria into Macrophages

Essential role for cholesterol in the delivery of exogenous antigens to the MHC class I-presentation pathway

Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist

Discovery of Nivasorexant (ACT-539313): The First Selective Orexin‑1 Receptor Antagonist (SO1RA) Investigated in Clinical Trials

The metabolism of the dual orexin receptor antagonist daridorexant

059 Daridorexant: A dual, equipotent, and insurmountable antagonist of both orexin-1 and orexin-2 receptors

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