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Page 1
MoA Studies of the TEAD P-Site Binding Ligand MSC-4106 and Its Optimization to TEAD1-Selective Amide M3686.
Heinrich T, Schwarz D, Petersson C, Gunera J, Garg S, Schneider R, Keil M, Grimmeisen L, Unzue Lopez A, Albers L, Schlesiger S, Gambardella A, Bomke J, Carswell E, Schilke H, Diehl P, Doerfel B, Musil D, Trivier E, Broome R, Marshall S, Balsiger A, Friedrich E, Lemos AR, Santos SP, Sousa PMF, Freire F, Bandeiras TM, Bortoluzzi A, Wienke D. Heinrich T, et al. Among authors: schlesiger s. J Med Chem. 2024 Dec 20. doi: 10.1021/acs.jmedchem.4c01949. Online ahead of print. J Med Chem. 2024. PMID: 39704449
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: schlesiger s. 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
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: schlesiger s. 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
PARP1 catalytic variants reveal branching and chain length-specific functions of poly(ADP-ribose) in cellular physiology and stress response.
Aberle L, Krüger A, Reber JM, Lippmann M, Hufnagel M, Schmalz M, Trussina IREA, Schlesiger S, Zubel T, Schütz K, Marx A, Hartwig A, Ferrando-May E, Bürkle A, Mangerich A. Aberle L, et al. Among authors: schlesiger s. Nucleic Acids Res. 2020 Oct 9;48(18):10015-10033. doi: 10.1093/nar/gkaa590. Nucleic Acids Res. 2020. PMID: 32667640 Free PMC article.