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Page 1
Selective Wee1 Inhibitors Led to Antitumor Activity In Vitro and Correlated with Myelosuppression.
Guler S, DiPoto MC, Crespo A, Caldwell R, Doerfel B, Grossmann N, Ho K, Huck B, Jones CC, Lan R, Musil D, Potnick J, Schilke H, Sherer B, Simon S, Sirrenberg C, Zhang Z, Liu-Bujalski L. Guler S, et al. Among authors: schilke h. ACS Med Chem Lett. 2023 Apr 7;14(5):566-576. doi: 10.1021/acsmedchemlett.2c00481. eCollection 2023 May 11. ACS Med Chem Lett. 2023. PMID: 37197456 Free PMC article.
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106.
Heinrich T, Peterson C, Schneider R, Garg S, Schwarz D, Gunera J, Seshire A, Kötzner L, Schlesiger S, Musil D, Schilke H, Doerfel B, Diehl P, Böpple P, Lemos AR, Sousa PMF, Freire F, Bandeiras TM, Carswell E, Pearson N, Sirohi S, Hooker M, Trivier E, Broome R, Balsiger A, Crowden A, Dillon C, Wienke D. Heinrich T, et al. Among authors: schilke h. J Med Chem. 2022 Jul 14;65(13):9206-9229. doi: 10.1021/acs.jmedchem.2c00403. Epub 2022 Jun 28. J Med Chem. 2022. PMID: 35763499
Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology.
Heinrich T, Sala-Hojman A, Ferretti R, Petersson C, Minguzzi S, Gondela A, Ramaswamy S, Bartosik A, Czauderna F, Crowley L, Wahra P, Schilke H, Böpple P, Dudek Ł, Leś M, Niedziejko P, Olech K, Pawlik H, Włoszczak Ł, Zuchowicz K, Suarez Alvarez JR, Martyka J, Sitek E, Mikulski M, Szczęśniak J, Jäckel S, Krier M, Król M, Wegener A, Gałęzowski M, Nowak M, Becker F, Herhaus C. Heinrich T, et al. Among authors: schilke h. J Med Chem. 2021 Aug 26;64(16):11904-11933. doi: 10.1021/acs.jmedchem.1c00448. Epub 2021 Aug 12. J Med Chem. 2021. PMID: 34382802
Discovery of reversible and covalent TEAD 1 selective inhibitors MSC-1254 and MSC-5046 based on one scaffold.
Carswell E, Heinrich T, Petersson C, Gunera J, Garg S, Schwarz D, Schlesiger S, Fischer F, Eichhorn T, Calder M, Smith G, MacDonald E, Wilson H, Hazel K, Trivier E, Broome R, Balsiger A, Sirohi S, Musil D, Freire F, Schilke H, Dillon C, Wienke D. Carswell E, et al. Among authors: schilke h. Bioorg Med Chem Lett. 2024 Dec 1;114:129981. doi: 10.1016/j.bmcl.2024.129981. Epub 2024 Oct 5. Bioorg Med Chem Lett. 2024. PMID: 39369801