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Page 1
Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).
Behnke D, Cotesta S, Hintermann S, Fendt M, Gee CE, Jacobson LH, Laue G, Meyer A, Wagner T, Badiger S, Chaudhari V, Chebrolu M, Pandit C, Hoyer D, Betschart C. Behnke D, et al. Among authors: cotesta s. Bioorg Med Chem Lett. 2015 Dec 1;25(23):5555-60. doi: 10.1016/j.bmcl.2015.10.055. Epub 2015 Oct 19. Bioorg Med Chem Lett. 2015. PMID: 26522950
Distinct effects of IPSU and suvorexant on mouse sleep architecture.
Hoyer D, Dürst T, Fendt M, Jacobson LH, Betschart C, Hintermann S, Behnke D, Cotesta S, Laue G, Ofner S, Legangneux E, Gee CE. Hoyer D, et al. Among authors: cotesta s. Front Neurosci. 2013 Dec 10;7:235. doi: 10.3389/fnins.2013.00235. eCollection 2013. Front Neurosci. 2013. PMID: 24368893 Free PMC article.
Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors.
Callander GE, Olorunda M, Monna D, Schuepbach E, Langenegger D, Betschart C, Hintermann S, Behnke D, Cotesta S, Fendt M, Laue G, Ofner S, Briard E, Gee CE, Jacobson LH, Hoyer D. Callander GE, et al. Among authors: cotesta s. Front Neurosci. 2013 Dec 3;7:230. doi: 10.3389/fnins.2013.00230. eCollection 2013. Front Neurosci. 2013. PMID: 24376396 Free PMC article.
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
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
Evolution of Novartis' Small Molecule Screening Deck Design.
Schuffenhauer A, Schneider N, Hintermann S, Auld D, Blank J, Cotesta S, Engeloch C, Fechner N, Gaul C, Giovannoni J, Jansen J, Joslin J, Krastel P, Lounkine E, Manchester J, Monovich LG, Pelliccioli AP, Schwarze M, Shultz MD, Stiefl N, Baeschlin DK. Schuffenhauer A, et al. Among authors: cotesta s. J Med Chem. 2020 Dec 10;63(23):14425-14447. doi: 10.1021/acs.jmedchem.0c01332. Epub 2020 Nov 3. J Med Chem. 2020. PMID: 33140646 Review.
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
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.
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
28 results