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Page 1
Fragment-based screening targeting an open form of the SARS-CoV-2 main protease binding pocket.
Huang CY, Metz A, Lange R, Artico N, Potot C, Hazemann J, Müller M, Dos Santos M, Chambovey A, Ritz D, Eris D, Meyer S, Bourquin G, Sharpe M, Mac Sweeney A. Huang CY, et al. Among authors: mac sweeney a. Acta Crystallogr D Struct Biol. 2024 Feb 1;80(Pt 2):123-136. doi: 10.1107/S2059798324000329. Epub 2024 Jan 30. Acta Crystallogr D Struct Biol. 2024. PMID: 38289714 Free PMC article.
Discovery and binding mode of small molecule inhibitors of the apo form of human TDO2.
Lotz-Jenne C, Lange R, Cren S, Bourquin G, Goglia L, Kimmerlin T, Wicki M, Müller M, Artico N, Ackerknecht S, Pfaff P, Joesch C, Mac Sweeney A. Lotz-Jenne C, et al. Among authors: mac sweeney a. Sci Rep. 2024 Nov 14;14(1):27937. doi: 10.1038/s41598-024-78981-4. Sci Rep. 2024. PMID: 39537789 Free PMC article.
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM. Mainolfi N, et al. Among authors: mac sweeney a. J Med Chem. 2020 Jun 11;63(11):5697-5722. doi: 10.1021/acs.jmedchem.9b01870. Epub 2020 Feb 19. J Med Chem. 2020. PMID: 32073845
Discovery of Novel Inhibitors of LpxC Displaying Potent in Vitro Activity against Gram-Negative Bacteria.
Surivet JP, Panchaud P, Specklin JL, Diethelm S, Blumstein AC, Gauvin JC, Jacob L, Masse F, Mathieu G, Mirre A, Schmitt C, Lange R, Tidten-Luksch N, Gnerre C, Seeland S, Herrmann C, Seiler P, Enderlin-Paput M, Mac Sweeney A, Wicki M, Hubschwerlen C, Ritz D, Rueedi G. Surivet JP, et al. Among authors: mac sweeney a. J Med Chem. 2020 Jan 9;63(1):66-87. doi: 10.1021/acs.jmedchem.9b01604. Epub 2019 Dec 24. J Med Chem. 2020. PMID: 31804826
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Karki RG, Powers J, Mainolfi N, Anderson K, Belanger DB, Liu D, Ji N, Jendza K, Gelin CF, Mac Sweeney A, Solovay C, Delgado O, Crowley M, Liao SM, Argikar UA, Flohr S, La Bonte LR, Lorthiois EL, Vulpetti A, Brown A, Long D, Prentiss M, Gradoux N, de Erkenez A, Cumin F, Adams C, Jaffee B, Mogi M. Karki RG, et al. Among authors: mac sweeney a. J Med Chem. 2019 May 9;62(9):4656-4668. doi: 10.1021/acs.jmedchem.9b00271. Epub 2019 Apr 30. J Med Chem. 2019. PMID: 30995036
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J. Schubart A, et al. Among authors: mac sweeney a. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29. Proc Natl Acad Sci U S A. 2019. PMID: 30926668 Free PMC article.
27 results