Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells von Gatfield, John, Mueller Grandjean, Celia, Sasse, Thomas, Clozel, Martine, Nayler, Oliver

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Selexipag: An Oral and Selective IP Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension von Asaki, Tetsuo, Kuwano, Keiichi, Morrison, Keith, Gatfield, John, Hamamoto, Taisuke, Clozel, Martine

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The Antifibrotic Activity of Prostacyclin Receptor Agonism Is Mediated through Inhibition of YAP/TAZ von Zmajkovicova, Katarina, Menyhart, Katalin, Bauer, Yasmina, Studer, Rolf, Renault, Berengere, Schnoebelen, Marie, Bolinger, Matthias, Nayler, Oliver, Gatfield, John

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The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468 von Treiber, Alexander, de Kanter, Ruben, Roch, Catherine, Gatfield, John, Boss, Christoph, von Raumer, Markus, Schindelholz, Benno, Muehlan, Clemens, van Gerven, Joop, Jenck, Francois

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Evaluation of tert-Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities von Westphal, Matthias V., Wolfstädter, Bernd T., Plancher, Jean-Marc, Gatfield, John, Carreira, Erick M.

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GPCR-induced YAP activation sensitizes fibroblasts to profibrotic activity of TGFβ1 von Zmajkovicova, Katarina, Bauer, Yasmina, Menyhart, Katalin, Schnoebelen, Marie, Freti, Diego, Boucher, Maxime, Renault, Bérengère, Studer, Rolf, Birker-Robaczewska, Magdalena, Klenk, Axel, Nayler, Oliver, Gatfield, John

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From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective von Boss, Christoph, Bolli, Martin H., Gatfield, John

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FTY720 Phosphate Activates Sphingosine-1-Phosphate Receptor 2 and Selectively Couples to Gα12/13/Rho/ROCK to Induce Myofibroblast Contraction von Sobel, Katrin, Monnier, Lucile, Menyhart, Katalin, Bolinger, Matthias, Studer, Rolf, Nayler, Oliver, Gatfield, John

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Novel high-throughput myofibroblast assays identify agonists with therapeutic potential in pulmonary fibrosis that act via EP2 and EP4 receptors von Sieber, Patrick, Schäfer, Anny, Lieberherr, Raphael, Le Goff, François, Stritt, Manuel, Welford, Richard W D, Gatfield, John, Peter, Oliver, Nayler, Oliver, Lüthi, Urs

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Ancestral Antibiotic Resistance in Mycobacterium tuberculosis von Morris, Rowan P, Nguyen, Liem, Gatfield, John, Visconti, Kevin, Nguyen, Kien, Schnappinger, Dirk, Ehrt, Sabine, Liu, Yang, Heifets, Leonid, Pieters, Jean, Schoolnik, Gary, Thompson, Charles J

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Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis von Gatfield, John, Mueller Grandjean, Celia, Bur, Daniel, Bolli, Martin H, Nayler, Oliver

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Desensitization by progressive up-titration prevents first-dose effects on the heart: guinea pig study with ponesimod, a selective S1P1 receptor modulator von Rey, Markus, Hess, Patrick, Clozel, Martine, Delahaye, Stéphane, Gatfield, John, Nayler, Oliver, Steiner, Beat

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Orexin Receptor Antagonists: A New Concept In CNS Disorders? von Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph

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Hijacking the host: survival of pathogenic mycobacteria inside macrophages von Pieters, Jean, Gatfield, John

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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 A... von Boss, Christoph, Roch-Brisbare, Catherine, Steiner, Michel A., Treiber, Alexander, Dietrich, Hendrik, Jenck, Francois, von Raumer, Markus, Sifferlen, Thierry, Brotschi, Christine, Heidmann, Bibia, Williams, Jodi T., Aissaoui, Hamed, Siegrist, Romain, Gatfield, John

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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. Par... von Sifferlen, Thierry, Koberstein, Ralf, Cottreel, Emmanuelle, Boller, Amandine, Weller, Thomas, Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph

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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 von Sifferlen, Thierry, Koberstein, Ralf, Cottreel, Emmanuelle, Boller, Amandine, Weller, Thomas, Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph

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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 von Sobel, Katrin, Menyhart, Katalin, Killer, Nina, Renault, Bérengère, Bauer, Yasmina, Studer, Rolf, Steiner, Beat, Bolli, Martin H., Nayler, Oliver, Gatfield, John

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Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies von Bezençon, Olivier, Siegrist, Romain, Heidmann, Bibia, Pozzi, Davide, Stamm, Simon, Remeň, Luboš, Richard, Sylvia, Simons, Lloyd, Gaston, Rick, Downing, Dennis, Grisostomi, Corinna, Roch, Catherine, Kessler, Melanie, Gatfield, John, Moon, Richard, Pfeifer, Thomas, Mosbacher, Johannes, Reymond, Isabelle, Ertel, Eric A, de Kanter, Ruben, Capeleto, Bruno, Fournier, Elvire, Rey, Markus, Moccia, Luca, Toeroek-Schafroth, Michael, Roscher, René, Schindelholz, Benno

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Essential Role for Cholesterol in Entry of Mycobacteria into Macrophages von Gatfield, John, Pieters, Jean

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