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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: eder j. Nat Chem Biol. 2016 Dec;12(12):1105-1110. doi: 10.1038/nchembio.2208. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775713
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: eder j. 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 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: eder j. 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
Mechanisms Driving Neutrophil-Induced T-cell Immunoparalysis in Ovarian Cancer.
Emmons TR, Giridharan T, Singel KL, Khan ANH, Ricciuti J, Howard K, Silva-Del Toro SL, Debreceni IL, Aarts CEM, Brouwer MC, Suzuki S, Kuijpers TW, Jongerius I, Allen LH, Ferreira VP, Schubart A, Sellner H, Eder J, Holland SM, Ram S, Lederer JA, Eng KH, Moysich KB, Odunsi K, Yaffe MB, Zsiros E, Segal BH. Emmons TR, et al. Among authors: eder j. Cancer Immunol Res. 2021 Jul;9(7):790-810. doi: 10.1158/2326-6066.CIR-20-0922. Epub 2021 May 14. Cancer Immunol Res. 2021. PMID: 33990375 Free PMC article.
Aspartic proteases in drug discovery.
Eder J, Hommel U, Cumin F, Martoglio B, Gerhartz B. Eder J, et al. Curr Pharm Des. 2007;13(3):271-85. doi: 10.2174/138161207779313560. Curr Pharm Des. 2007. PMID: 17313361 Review.
Pharmacological inhibition of IKKβ dampens NLRP3 inflammasome activation after priming in the human myeloid cell line THP-1.
Unterreiner A, Rubert J, Kauffmann M, Fruhauf A, Heiser D, Erbel P, Schlapbach A, Eder J, Bodendorf U, Boettcher A, Farady CJ, Bornancin F. Unterreiner A, et al. Among authors: eder j. Biochem Biophys Res Commun. 2021 Mar 19;545:177-182. doi: 10.1016/j.bbrc.2021.01.051. Epub 2021 Feb 6. Biochem Biophys Res Commun. 2021. PMID: 33561652
339 results