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Page 1
Dipeptidyl nitrile inhibitors of Cathepsin L.
Asaad N, Bethel PA, Coulson MD, Dawson JE, Ford SJ, Gerhardt S, Grist M, Hamlin GA, James MJ, Jones EV, Karoutchi GI, Kenny PW, Morley AD, Oldham K, Rankine N, Ryan D, Wells SL, Wood L, Augustin M, Krapp S, Simader H, Steinbacher S. Asaad N, et al. Among authors: krapp s. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3. doi: 10.1016/j.bmcl.2009.05.071. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19515558
Design of selective Cathepsin inhibitors.
Bethel PA, Gerhardt S, Jones EV, Kenny PW, Karoutchi GI, Morley AD, Oldham K, Rankine N, Augustin M, Krapp S, Simader H, Steinbacher S. Bethel PA, et al. Among authors: krapp s. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4622-5. doi: 10.1016/j.bmcl.2009.06.090. Epub 2009 Jun 27. Bioorg Med Chem Lett. 2009. PMID: 19616430
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, MacFaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M. Dossetter AG, et al. Among authors: krapp s. J Med Chem. 2012 Jul 26;55(14):6363-74. doi: 10.1021/jm3007257. Epub 2012 Jul 10. J Med Chem. 2012. PMID: 22742641
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Dossetter AG, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, MacFaul PA, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C. Dossetter AG, et al. Among authors: krapp s. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5563-8. doi: 10.1016/j.bmcl.2012.07.012. Epub 2012 Jul 15. Bioorg Med Chem Lett. 2012. PMID: 22858142
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Crawford JJ, Kenny PW, Bowyer J, Cook CR, Finlayson JE, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Martin S, Macfaul PA, McDermott BP, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Dossetter AG. Crawford JJ, et al. Among authors: krapp s. J Med Chem. 2012 Oct 25;55(20):8827-37. doi: 10.1021/jm301119s. Epub 2012 Oct 11. J Med Chem. 2012. PMID: 22984809
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.
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
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.
26 results