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Page 1
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
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate.
Douangamath A, Dale GE, D'Arcy A, Almstetter M, Eckl R, Frutos-Hoener A, Henkel B, Illgen K, Nerdinger S, Schulz H, Mac Sweeney A, Thormann M, Treml A, Pierau S, Wadman S, Oefner C. Douangamath A, et al. Among authors: mac sweeney a. J Med Chem. 2004 Mar 11;47(6):1325-8. doi: 10.1021/jm034188j. J Med Chem. 2004. PMID: 14998322
Discovery and structure-based optimization of adenain inhibitors.
Mac Sweeney A, Grosche P, Ellis D, Combrink K, Erbel P, Hughes N, Sirockin F, Melkko S, Bernardi A, Ramage P, Jarousse N, Altmann E. Mac Sweeney A, et al. ACS Med Chem Lett. 2014 Jun 20;5(8):937-41. doi: 10.1021/ml500224t. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147618 Free PMC article.
Structure-based design and optimization of potent inhibitors of the adenoviral protease.
Grosche P, Sirockin F, Mac Sweeney A, Ramage P, Erbel P, Melkko S, Bernardi A, Hughes N, Ellis D, Combrink KD, Jarousse N, Altmann E. Grosche P, et al. Among authors: mac sweeney a. Bioorg Med Chem Lett. 2015 Feb 1;25(3):438-43. doi: 10.1016/j.bmcl.2014.12.057. Epub 2014 Dec 24. Bioorg Med Chem Lett. 2015. PMID: 25571794
Small-molecule factor D inhibitors targeting the alternative complement pathway.
Maibaum J, Liao SM, Vulpetti A, Ostermann N, Randl S, Rüdisser S, Lorthiois E, Erbel P, Kinzel B, Kolb FA, Barbieri S, Wagner J, Durand C, Fettis K, Dussauge S, Hughes N, Delgado O, Hommel U, Gould T, Mac Sweeney A, Gerhartz B, Cumin F, Flohr S, Schubart A, Jaffee B, Harrison R, Risitano AM, Eder J, Anderson K. Maibaum J, et al. Among authors: mac sweeney a. Nat Chem Biol. 2016 Dec;12(12):1105-1110. doi: 10.1038/nchembio.2208. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775713
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.
Vulpetti A, Randl S, Rüdisser S, Ostermann N, Erbel P, Mac Sweeney A, Zoller T, Salem B, Gerhartz B, Cumin F, Hommel U, Dalvit C, Lorthiois E, Maibaum J. Vulpetti A, et al. Among authors: mac sweeney a. J Med Chem. 2017 Mar 9;60(5):1946-1958. doi: 10.1021/acs.jmedchem.6b01684. Epub 2017 Feb 20. J Med Chem. 2017. PMID: 28157311
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J. Lorthiois E, et al. Among authors: mac sweeney a. J Med Chem. 2017 Jul 13;60(13):5717-5735. doi: 10.1021/acs.jmedchem.7b00425. Epub 2017 Jun 30. J Med Chem. 2017. PMID: 28621538
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.
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
27 results