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Page 1
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Weiss A, Lorthiois E, Barys L, Beyer KS, Bomio-Confaglia C, Burks H, Chen X, Cui X, de Kanter R, Dharmarajan L, Fedele C, Gerspacher M, Guthy DA, Head V, Jaeger A, Núñez EJ, Kearns JD, Leblanc C, Maira SM, Murphy J, Oakman H, Ostermann N, Ottl J, Rigollier P, Roman D, Schnell C, Sedrani R, Shimizu T, Stringer R, Vaupel A, Voshol H, Wessels P, Widmer T, Wilcken R, Xu K, Zecri F, Farago AF, Cotesta S, Brachmann SM. Weiss A, et al. Among authors: cotesta s. Cancer Discov. 2022 Jun 2;12(6):1500-1517. doi: 10.1158/2159-8290.CD-22-0158. Cancer Discov. 2022. PMID: 35404998 Free PMC article.
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, Piechon P, Villard F, Bouhelal R, Piller F, Harlfinger S, Stringer R, Fehlmann D, Kaupmann K, Littlewood-Evans A, Haffke M, Gommermann N. Velcicky J, et al. Among authors: cotesta s. J Med Chem. 2020 Sep 10;63(17):9856-9875. doi: 10.1021/acs.jmedchem.0c01020. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32856916
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. Lorthiois E, et al. Among authors: cotesta s. J Med Chem. 2022 Dec 22;65(24):16173-16203. doi: 10.1021/acs.jmedchem.2c01438. Epub 2022 Nov 18. J Med Chem. 2022. PMID: 36399068
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Jahnke W, Rondeau JM, Cotesta S, Marzinzik A, Pellé X, Geiser M, Strauss A, Götte M, Bitsch F, Hemmig R, Henry C, Lehmann S, Glickman JF, Roddy TP, Stout SJ, Green JR. Jahnke W, et al. Among authors: cotesta s. Nat Chem Biol. 2010 Sep;6(9):660-6. doi: 10.1038/nchembio.421. Epub 2010 Aug 15. Nat Chem Biol. 2010. PMID: 20711197
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P. Schoepfer J, et al. Among authors: cotesta s. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. J Med Chem. 2018. PMID: 30137981
BET bromodomain inhibitors regulate keratinocyte plasticity.
Schutzius G, Kolter C, Bergling S, Tortelli F, Fuchs F, Renner S, Guagnano V, Cotesta S, Rueeger H, Faller M, Bouchez L, Salathe A, Nigsch F, Richards SM, Louis M, Gruber V, Aebi A, Turner J, Grandjean F, Li J, Dimitri C, Thomas JR, Schirle M, Blank J, Drueckes P, Vaupel A, Tiedt R, Manley PW, Klopp J, Hemmig R, Zink F, Leroy N, Carbone W, Roma G, Keller CG, Dales N, Beyerbach A, Zimmerlin A, Bonenfant D, Terranova R, Berwick A, Sahambi S, Reynolds A, Jennings LL, Ruffner H, Tarsa P, Bouwmeester T, Driver V, Frederiksen M, Lohmann F, Kirkland S. Schutzius G, et al. Among authors: cotesta s. Nat Chem Biol. 2021 Mar;17(3):280-290. doi: 10.1038/s41589-020-00716-z. Epub 2021 Jan 18. Nat Chem Biol. 2021. PMID: 33462494
Identification and evaluation of novel acetolactate synthase inhibitors as antifungal agents.
Richie DL, Thompson KV, Studer C, Prindle VC, Aust T, Riedl R, Estoppey D, Tao J, Sexton JA, Zabawa T, Drumm J, Cotesta S, Eichenberger J, Schuierer S, Hartmann N, Movva NR, Tallarico JA, Ryder NS, Hoepfner D. Richie DL, et al. Among authors: cotesta s. Antimicrob Agents Chemother. 2013 May;57(5):2272-80. doi: 10.1128/AAC.01809-12. Epub 2013 Mar 11. Antimicrob Agents Chemother. 2013. PMID: 23478965 Free PMC article.
Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding.
Marzinzik AL, Amstutz R, Bold G, Bourgier E, Cotesta S, Glickman JF, Götte M, Henry C, Lehmann S, Hartwieg JC, Ofner S, Pellé X, Roddy TP, Rondeau JM, Stauffer F, Stout SJ, Widmer A, Zimmermann J, Zoller T, Jahnke W. Marzinzik AL, et al. Among authors: cotesta s. ChemMedChem. 2015 Nov;10(11):1884-91. doi: 10.1002/cmdc.201500338. Epub 2015 Sep 18. ChemMedChem. 2015. PMID: 26381451
27 results