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GPR103 antagonists demonstrating anorexigenic activity in vivo: design and development of pyrrolo[2,3-c]pyridines that mimic the C-terminal Arg-Phe motif of QRFP26.
Georgsson J, Bergström F, Nordqvist A, Watson MJ, Blundell CD, Johansson MJ, Petersson AU, Yuan ZQ, Zhou Y, Kristensson L, Kakol-Palm D, Tyrchan C, Wellner E, Bauer U, Brodin P, Svensson Henriksson A. Georgsson J, et al. Among authors: tyrchan c. J Med Chem. 2014 Jul 24;57(14):5935-48. doi: 10.1021/jm401951t. Epub 2014 Jul 2. J Med Chem. 2014. PMID: 24937104
New Hits as Antagonists of GPR103 Identified by HTS.
Nordqvist A, Kristensson L, Johansson KE, Isaksson da Silva K, Fex T, Tyrchan C, Svensson Henriksson A, Nilsson K. Nordqvist A, et al. Among authors: tyrchan c. ACS Med Chem Lett. 2014 Feb 22;5(5):527-32. doi: 10.1021/ml400519h. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900874 Free PMC article.
Correction to GPR103 Antagonists Demonstrating Anorexigenic Activity in Vivo: Design and Development of Pyrrolo[2,3-c]pyridines That Mimic the C-Terminal Arg-Phe Motif of QRFP26.
Georgsson J, Bergström F, Nordqvist A, Watson MJ, Blundell CD, Johansson MJ, Petersson AU, Yuan ZQ, Zhou Y, Kristensson L, Kakol-Palm D, Tyrchan C, Wellner E, Bauer U, Brodin P, Svensson Henriksson A. Georgsson J, et al. Among authors: tyrchan c. J Med Chem. 2015 May 14;58(9):4086. doi: 10.1021/acs.jmedchem.5b00479. Epub 2015 Apr 15. J Med Chem. 2015. PMID: 25875054 No abstract available.
Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration.
Perry MWD, Björhall K, Bonn B, Carlsson J, Chen Y, Eriksson A, Fredlund L, Hao H, Holden NS, Karabelas K, Lindmark H, Liu F, Pemberton N, Petersen J, Rodrigo Blomqvist S, Smith RW, Svensson T, Terstiege I, Tyrchan C, Yang W, Zhao S, Öster L. Perry MWD, et al. Among authors: tyrchan c. J Med Chem. 2017 Jun 22;60(12):5057-5071. doi: 10.1021/acs.jmedchem.7b00401. Epub 2017 Jun 7. J Med Chem. 2017. PMID: 28520415 Free article.
Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1S,2S)-2-({5-[(5-Chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbonyl)cyclopropanecarboxylic Acid (AZD9898) as a New Treatment for Asthma.
Munck Af Rosenschöld M, Johannesson P, Nikitidis A, Tyrchan C, Chang HF, Rönn R, Chapman D, Ullah V, Nikitidis G, Glader P, Käck H, Bonn B, Wågberg F, Björkstrand E, Andersson U, Swedin L, Rohman M, Andreasson T, Bergström EL, Jiang F, Zhou XH, Lundqvist AJ, Malmberg A, Ek M, Gordon E, Pettersen A, Ripa L, Davis AM. Munck Af Rosenschöld M, et al. Among authors: tyrchan c. J Med Chem. 2019 Sep 12;62(17):7769-7787. doi: 10.1021/acs.jmedchem.9b00555. Epub 2019 Aug 30. J Med Chem. 2019. PMID: 31415176
Identification of novel GPR81 agonist lead series for target biology evaluation.
Davidsson Ö, Nilsson K, Brånalt J, Andersson T, Berggren K, Chen Y, Fjellström O, Gradén H, Gustafsson L, Hermansson NO, Jansen F, Johannesson P, Ohlsson B, Tyrchan C, Wellner A, Wellner E, Ölwegård-Halvarsson M. Davidsson Ö, et al. Among authors: tyrchan c. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126953. doi: 10.1016/j.bmcl.2020.126953. Epub 2020 Jan 7. Bioorg Med Chem Lett. 2020. PMID: 31932225
Mining Natural Products for Macrocycles to Drug Difficult Targets.
Begnini F, Poongavanam V, Over B, Castaldo M, Geschwindner S, Johansson P, Tyagi M, Tyrchan C, Wissler L, Sjö P, Schiesser S, Kihlberg J. Begnini F, et al. Among authors: tyrchan c. J Med Chem. 2021 Jan 28;64(2):1054-1072. doi: 10.1021/acs.jmedchem.0c01569. Epub 2020 Dec 18. J Med Chem. 2021. PMID: 33337880 Free PMC article.
Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma.
Perry MWD, Björhall K, Bold P, Brűlls M, Börjesson U, Carlsson J, Chang HA, Chen Y, Eriksson A, Fihn BM, Fransson R, Fredlund L, Ge H, Huang H, Karabelas K, Lamm Bergström E, Lever S, Lindmark H, Mogemark M, Nikitidis A, Palmgren AP, Pemberton N, Petersen J, Rodrigo Blomqvist M, Smith RW, Thomas MJ, Ullah V, Tyrchan C, Wennberg T, Westin Eriksson A, Yang W, Zhao S, Öster L. Perry MWD, et al. Among authors: tyrchan c. J Med Chem. 2021 Jun 24;64(12):8053-8075. doi: 10.1021/acs.jmedchem.1c00434. Epub 2021 Jun 3. J Med Chem. 2021. PMID: 34080862
53 results