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Items: 41

1.

Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure-Activity Relationships, and Sleep-Promoting Properties in Rats.

Brotschi C, Roch C, Gatfield J, Treiber A, Williams JT, Sifferlen T, Heidmann B, Jenck F, Bolli MH, Boss C.

ChemMedChem. 2019 Jul 3;14(13):1257-1270. doi: 10.1002/cmdc.201900242. Epub 2019 Jun 5.

PMID:
31066976
2.

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

Zmajkovicova K, Menyhart K, Bauer Y, Studer R, Renault B, Schnoebelen M, Bolinger M, Nayler O, Gatfield J.

Am J Respir Cell Mol Biol. 2019 May;60(5):578-591. doi: 10.1165/rcmb.2018-0142OC.

PMID:
30537446
3.

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

Sieber P, Schäfer A, Lieberherr R, Le Goff F, Stritt M, Welford RWD, Gatfield J, Peter O, Nayler O, Lüthi U.

PLoS One. 2018 Nov 28;13(11):e0207872. doi: 10.1371/journal.pone.0207872. eCollection 2018.

4.

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

Bezençon O, Siegrist R, Heidmann B, Pozzi D, Stamm S, Remeň L, Richard S, Simons L, Gaston R, Downing D, Grisostomi C, Roch C, Kessler M, Gatfield J, Moon R, Pfeifer T, Mosbacher J, Reymond I, Ertel EA, de Kanter R, Capeleto B, Fournier E, Rey M, Moccia L, Toeroek-Schafroth M, Roscher R, Schindelholz B.

Chimia (Aarau). 2017 Oct 25;71(10):722-729. doi: 10.2533/chimia.2017.722.

PMID:
29070417
5.

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

Treiber A, de Kanter R, Roch C, Gatfield J, Boss C, von Raumer M, Schindelholz B, Muehlan C, van Gerven J, Jenck F.

J Pharmacol Exp Ther. 2017 Sep;362(3):489-503. doi: 10.1124/jpet.117.241596. Epub 2017 Jun 29.

PMID:
28663311
6.

Selexipag Active Metabolite ACT-333679 Displays Strong Anticontractile and Antiremodeling Effects but Low β-Arrestin Recruitment and Desensitization Potential.

Gatfield J, Menyhart K, Wanner D, Gnerre C, Monnier L, Morrison K, Hess P, Iglarz M, Clozel M, Nayler O.

J Pharmacol Exp Ther. 2017 Jul;362(1):186-199. doi: 10.1124/jpet.116.239665. Epub 2017 May 5.

PMID:
28476928
7.

Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.

Remen L, Bezençon O, Simons L, Gaston R, Downing D, Gatfield J, Roch C, Kessler M, Mosbacher J, Pfeifer T, Grisostomi C, Rey M, Ertel EA, Moon R.

J Med Chem. 2016 Sep 22;59(18):8398-411. doi: 10.1021/acs.jmedchem.6b00756. Epub 2016 Sep 12.

PMID:
27579577
8.

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach.

Heidmann B, Gatfield J, Roch C, Treiber A, Tortoioli S, Brotschi C, Williams JT, Bolli MH, Abele S, Sifferlen T, Jenck F, Boss C.

ChemMedChem. 2016 Oct 6;11(19):2132-2146. doi: 10.1002/cmdc.201600175. Epub 2016 Jul 8.

PMID:
27390287
9.

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

Boss C, Bolli MH, Gatfield J.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3381-94. doi: 10.1016/j.bmcl.2016.06.014. Epub 2016 Jun 10. Review.

PMID:
27321813
10.

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

Asaki T, Kuwano K, Morrison K, Gatfield J, Hamamoto T, Clozel M.

J Med Chem. 2015 Sep 24;58(18):7128-37. doi: 10.1021/acs.jmedchem.5b00698. Epub 2015 Sep 16.

PMID:
26291199
11.

Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.

Renneberg D, Hubler F, Rey M, Hess P, Delahaye S, Gatfield J, Iglarz M, Hilpert K.

Bioorg Med Chem Lett. 2015 Sep 15;25(18):3941-6. doi: 10.1016/j.bmcl.2015.07.038. Epub 2015 Jul 21.

PMID:
26231163
12.

Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.

Sifferlen T, Boller A, Chardonneau A, Cottreel E, Gatfield J, Treiber A, Roch C, Jenck F, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Boss C.

Bioorg Med Chem Lett. 2015 May 1;25(9):1884-91. doi: 10.1016/j.bmcl.2015.03.035. Epub 2015 Mar 21.

PMID:
25838147
13.

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

Sobel K, Monnier L, Menyhart K, Bolinger M, Studer R, Nayler O, Gatfield J.

Mol Pharmacol. 2015 Jun;87(6):916-27. doi: 10.1124/mol.114.097261. Epub 2015 Mar 11.

PMID:
25762025
14.

Evaluation of tert-butyl isosteres: case studies of physicochemical and pharmacokinetic properties, efficacies, and activities.

Westphal MV, Wolfstädter BT, Plancher JM, Gatfield J, Carreira EM.

ChemMedChem. 2015 Mar;10(3):461-9. doi: 10.1002/cmdc.201402502. Epub 2015 Jan 28.

PMID:
25630804
15.

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

Gatfield J, Mueller Grandjean C, Bur D, Bolli MH, Nayler O.

PLoS One. 2014 Sep 16;9(9):e107809. doi: 10.1371/journal.pone.0107809. eCollection 2014.

16.

Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.

Boss C, Roch-Brisbare C, Steiner MA, Treiber A, Dietrich H, Jenck F, von Raumer M, Sifferlen T, Brotschi C, Heidmann B, Williams JT, Aissaoui H, Siegrist R, Gatfield J.

ChemMedChem. 2014 Nov;9(11):2486-96. doi: 10.1002/cmdc.201402258. Epub 2014 Aug 21.

PMID:
25147058
17.

Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling.

Gatfield J, Monnier L, Studer R, Bolli MH, Steiner B, Nayler O.

Cell Signal. 2014 Jul;26(7):1576-88. doi: 10.1016/j.cellsig.2014.03.029. Epub 2014 Apr 2.

PMID:
24704119
18.

Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1.

Sifferlen T, Boller A, Chardonneau A, Cottreel E, Hoecker J, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Gatfield J, Treiber A, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1201-8. doi: 10.1016/j.bmcl.2013.12.092. Epub 2013 Dec 30.

PMID:
24447850
19.

Desensitization by progressive up-titration prevents first-dose effects on the heart: guinea pig study with ponesimod, a selective S1P1 receptor modulator.

Rey M, Hess P, Clozel M, Delahaye S, Gatfield J, Nayler O, Steiner B.

PLoS One. 2013 Sep 12;8(9):e74285. doi: 10.1371/journal.pone.0074285. eCollection 2013.

20.

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.

Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3857-63. doi: 10.1016/j.bmcl.2013.04.071. Epub 2013 May 8.

PMID:
23719231
21.

Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist.

Steiner MA, Gatfield J, Brisbare-Roch C, Dietrich H, Treiber A, Jenck F, Boss C.

ChemMedChem. 2013 Jun;8(6):898-903. doi: 10.1002/cmdc.201300003. Epub 2013 Apr 15.

PMID:
23589487
22.

Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad-independent signaling.

Sobel K, Menyhart K, Killer N, Renault B, Bauer Y, Studer R, Steiner B, Bolli MH, Nayler O, Gatfield J.

J Biol Chem. 2013 May 24;288(21):14839-51. doi: 10.1074/jbc.M112.426726. Epub 2013 Apr 15.

23.

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.

Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2212-6. doi: 10.1016/j.bmcl.2013.01.088. Epub 2013 Jan 29.

PMID:
23434414
24.

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

Gatfield J, Mueller Grandjean C, Sasse T, Clozel M, Nayler O.

PLoS One. 2012;7(10):e47662. doi: 10.1371/journal.pone.0047662. Epub 2012 Oct 15.

25.

Orexin receptor antagonists: a new concept in CNS disorders?

Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

ChemMedChem. 2010 Aug 2;5(8):1197-214. doi: 10.1002/cmdc.201000132. Review. No abstract available.

PMID:
20544785
26.

2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.

Bolli MH, Abele S, Binkert C, Bravo R, Buchmann S, Bur D, Gatfield J, Hess P, Kohl C, Mangold C, Mathys B, Menyhart K, Müller C, Nayler O, Scherz M, Schmidt G, Sippel V, Steiner B, Strasser D, Treiber A, Weller T.

J Med Chem. 2010 May 27;53(10):4198-211. doi: 10.1021/jm100181s.

PMID:
20446681
27.

Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.

Sifferlen T, Boss C, Cottreel E, Koberstein R, Gude M, Aissaoui H, Weller T, Gatfield J, Brisbare-Roch C, Jenck F.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1539-42. doi: 10.1016/j.bmcl.2010.01.070. Epub 2010 Jan 22.

PMID:
20144866
28.

N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.

Aissaoui H, Koberstein R, Zumbrunn C, Gatfield J, Brisbare-Roch C, Jenck F, Treiber A, Boss C.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5729-33. doi: 10.1016/j.bmcl.2008.09.079. Epub 2008 Sep 26.

PMID:
18845436
29.

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

Iglarz M, Binkert C, Morrison K, Fischli W, Gatfield J, Treiber A, Weller T, Bolli MH, Boss C, Buchmann S, Capeleto B, Hess P, Qiu C, Clozel M.

J Pharmacol Exp Ther. 2008 Dec;327(3):736-45. doi: 10.1124/jpet.108.142976. Epub 2008 Sep 9.

PMID:
18780830
30.

Regulation of T cell survival through coronin-1-mediated generation of inositol-1,4,5-trisphosphate and calcium mobilization after T cell receptor triggering.

Mueller P, Massner J, Jayachandran R, Combaluzier B, Albrecht I, Gatfield J, Blum C, Ceredig R, Rodewald HR, Rolink AG, Pieters J.

Nat Immunol. 2008 Apr;9(4):424-31. doi: 10.1038/ni1570. Epub 2008 Mar 16.

PMID:
18345003
31.

RNA interference in J774 macrophages reveals a role for coronin 1 in mycobacterial trafficking but not in actin-dependent processes.

Jayachandran R, Gatfield J, Massner J, Albrecht I, Zanolari B, Pieters J.

Mol Biol Cell. 2008 Mar;19(3):1241-51. Epub 2007 Dec 27.

32.

Antigen 84, an effector of pleiomorphism in Mycobacterium smegmatis.

Nguyen L, Scherr N, Gatfield J, Walburger A, Pieters J, Thompson CJ.

J Bacteriol. 2007 Nov;189(21):7896-910. Epub 2007 Aug 31.

33.

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

Albrecht I, Gatfield J, Mini T, Jeno P, Pieters J.

Int Immunol. 2006 May;18(5):755-65. Epub 2006 Apr 11.

PMID:
16608901
34.

Ancestral antibiotic resistance in Mycobacterium tuberculosis.

Morris RP, Nguyen L, Gatfield J, Visconti K, Nguyen K, Schnappinger D, Ehrt S, Liu Y, Heifets L, Pieters J, Schoolnik G, Thompson CJ.

Proc Natl Acad Sci U S A. 2005 Aug 23;102(34):12200-5. Epub 2005 Aug 15.

35.

Association of the leukocyte plasma membrane with the actin cytoskeleton through coiled coil-mediated trimeric coronin 1 molecules.

Gatfield J, Albrecht I, Zanolari B, Steinmetz MO, Pieters J.

Mol Biol Cell. 2005 Jun;16(6):2786-98. Epub 2005 Mar 30.

36.

Molecular mechanisms of host-pathogen interaction: entry and survival of mycobacteria in macrophages.

Gatfield J, Pieters J.

Adv Immunol. 2003;81:45-96. Review. No abstract available.

PMID:
14711053
37.

Hijacking the host: survival of pathogenic mycobacteria inside macrophages.

Pieters J, Gatfield J.

Trends Microbiol. 2002 Mar;10(3):142-6.

PMID:
11864824
38.

Efficient replication of adenovirus despite the overexpression of active and nondegradable p53.

Koch P, Gatfield J, Löber C, Hobom U, Lenz-Stöppler C, Roth J, Dobbelstein M.

Cancer Res. 2001 Aug 1;61(15):5941-7.

39.

Essential role for cholesterol in entry of mycobacteria into macrophages.

Gatfield J, Pieters J.

Science. 2000 Jun 2;288(5471):1647-50.

40.

The HLA-A*6601 peptide motif: prediction by pocket structure and verification by peptide analysis.

Seeger FH, Schirle M, Gatfield J, Arnold D, Keilholz W, Nickolaus P, Rammensee HG, Stevanović S.

Immunogenetics. 1999 Jun;49(6):571-6. No abstract available.

PMID:
10380706
41.

Cell lines transfected with the TAP inhibitor ICP47 allow testing peptide binding to a variety of HLA class I molecules.

Gatfield J, Lammert E, Nickolaus P, Münz C, Rothenfusser S, Fisch P, Stevanović S, Schild H, Rammensee HG, Arnold D.

Int Immunol. 1998 Nov;10(11):1665-72.

PMID:
9846695

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