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Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT. Hamilton MM, et al. Among authors: krapp s. J Med Chem. 2021 Aug 12;64(15):11302-11329. doi: 10.1021/acs.jmedchem.1c00679. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292726
Aerosol-based ligand soaking of reservoir-free protein crystals.
Ross B, Krapp S, Geiss-Friedlander R, Littmann W, Huber R, Kiefersauer R. Ross B, et al. Among authors: krapp s. J Appl Crystallogr. 2021 May 28;54(Pt 3):895-902. doi: 10.1107/S1600576721003551. eCollection 2021 Jun 1. J Appl Crystallogr. 2021. PMID: 34188616 Free PMC article.
Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry.
Guilinger JP, Archna A, Augustin M, Bergmann A, Centrella PA, Clark MA, Cuozzo JW, Däther M, Guié MA, Habeshian S, Kiefersauer R, Krapp S, Lammens A, Lercher L, Liu J, Liu Y, Maskos K, Mrosek M, Pflügler K, Siegert M, Thomson HA, Tian X, Zhang Y, Konz Makino DL, Keefe AD. Guilinger JP, et al. Among authors: krapp s. Bioorg Med Chem. 2021 Jul 15;42:116223. doi: 10.1016/j.bmc.2021.116223. Epub 2021 May 19. Bioorg Med Chem. 2021. PMID: 34091303 Free article.
β-Glucocerebrosidase Modulators Promote Dimerization of β-Glucocerebrosidase and Reveal an Allosteric Binding Site.
Zheng J, Chen L, Skinner OS, Ysselstein D, Remis J, Lansbury P, Skerlj R, Mrosek M, Heunisch U, Krapp S, Charrow J, Schwake M, Kelleher NL, Silverman RB, Krainc D. Zheng J, et al. Among authors: krapp s. J Am Chem Soc. 2018 May 9;140(18):5914-5924. doi: 10.1021/jacs.7b13003. Epub 2018 Apr 30. J Am Chem Soc. 2018. PMID: 29676907 Free PMC article.
IR laser-induced protein crystal transformation.
Kiefersauer R, Grandl B, Krapp S, Huber R. Kiefersauer R, et al. Among authors: krapp s. Acta Crystallogr D Biol Crystallogr. 2014 May;70(Pt 5):1224-32. doi: 10.1107/S1399004714002223. Epub 2014 Apr 26. Acta Crystallogr D Biol Crystallogr. 2014. PMID: 24816092 Free PMC article.
26 results