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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: harrison ra. 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
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. 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.
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. Nat Chem Biol. 2016 Dec;12(12):1105-1110. doi: 10.1038/nchembio.2208. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775713
The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).
Cheshire DR, Åberg A, Andersson GM, Andrews G, Beaton HG, Birkinshaw TN, Boughton-Smith N, Connolly S, Cook TR, Cooper A, Cooper SL, Cox D, Dixon J, Gensmantel N, Hamley PJ, Harrison R, Hartopp P, Käck H, Leeson PD, Luker T, Mete A, Millichip I, Nicholls DJ, Pimm AD, St-Gallay SA, Wallace AV. Cheshire DR, et al. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2468-71. doi: 10.1016/j.bmcl.2011.02.061. Epub 2011 Feb 18. Bioorg Med Chem Lett. 2011. PMID: 21398123
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Ripa L, Edman K, Dearman M, Edenro G, Hendrickx R, Ullah V, Chang HF, Lepistö M, Chapman D, Geschwindner S, Wissler L, Svanberg P, Lawitz K, Malmberg J, Nikitidis A, Olsson RI, Bird J, Llinas A, Hegelund-Myrbäck T, Berger M, Thorne P, Harrison R, Köhler C, Drmota T. Ripa L, et al. J Med Chem. 2018 Mar 8;61(5):1785-1799. doi: 10.1021/acs.jmedchem.7b01690. Epub 2018 Feb 16. J Med Chem. 2018. PMID: 29424542
Dermonecrosis caused by a spitting cobra snakebite results from toxin potentiation and is prevented by the repurposed drug varespladib.
Bartlett KE, Hall SR, Rasmussen SA, Crittenden E, Dawson CA, Albulescu LO, Laprade W, Harrison RA, Saviola AJ, Modahl CM, Jenkins TP, Wilkinson MC, Gutiérrez JM, Casewell NR. Bartlett KE, et al. Among authors: harrison ra. Proc Natl Acad Sci U S A. 2024 May 7;121(19):e2315597121. doi: 10.1073/pnas.2315597121. Epub 2024 Apr 30. Proc Natl Acad Sci U S A. 2024. PMID: 38687786 Free PMC article.
Synthetic development of a broadly neutralizing antibody against snake venom long-chain α-neurotoxins.
Khalek IS, Senji Laxme RR, Nguyen YTK, Khochare S, Patel RN, Woehl J, Smith JM, Saye-Francisco K, Kim Y, Misson Mindrebo L, Tran Q, Kędzior M, Boré E, Limbo O, Verma M, Stanfield RL, Menzies SK, Ainsworth S, Harrison RA, Burton DR, Sok D, Wilson IA, Casewell NR, Sunagar K, Jardine JG. Khalek IS, et al. Among authors: harrison ra. Sci Transl Med. 2024 Feb 21;16(735):eadk1867. doi: 10.1126/scitranslmed.adk1867. Epub 2024 Feb 21. Sci Transl Med. 2024. PMID: 38381847
439 results