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Page 1
IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial.
Ackerman L, Acloque G, Bacchelli S, Schwartz H, Feinstein BJ, La Stella P, Alavi A, Gollerkeri A, Davis J, Campbell V, McDonald A, Agarwal S, Karnik R, Shi K, Mishkin A, Culbertson J, Klaus C, Enerson B, Massa V, Kuhn E, Sharma K, Keaney E, Barnes R, Chen D, Zheng X, Rong H, Sabesan V, Ho C, Mainolfi N, Slavin A, Gollob JA. Ackerman L, et al. Among authors: mainolfi n. Nat Med. 2023 Dec;29(12):3127-3136. doi: 10.1038/s41591-023-02635-7. Epub 2023 Nov 13. Nat Med. 2023. PMID: 37957373 Free PMC article. Clinical Trial.
Serine synthesis pathway inhibition cooperates with dietary serine and glycine limitation for cancer therapy.
Tajan M, Hennequart M, Cheung EC, Zani F, Hock AK, Legrave N, Maddocks ODK, Ridgway RA, Athineos D, Suárez-Bonnet A, Ludwig RL, Novellasdemunt L, Angelis N, Li VSW, Vlachogiannis G, Valeri N, Mainolfi N, Suri V, Friedman A, Manfredi M, Blyth K, Sansom OJ, Vousden KH. Tajan M, et al. Among authors: mainolfi n. Nat Commun. 2021 Jan 14;12(1):366. doi: 10.1038/s41467-020-20223-y. Nat Commun. 2021. PMID: 33446657 Free PMC article.
Limited Environmental Serine and Glycine Confer Brain Metastasis Sensitivity to PHGDH Inhibition.
Ngo B, Kim E, Osorio-Vasquez V, Doll S, Bustraan S, Liang RJ, Luengo A, Davidson SM, Ali A, Ferraro GB, Fischer GM, Eskandari R, Kang DS, Ni J, Plasger A, Rajasekhar VK, Kastenhuber ER, Bacha S, Sriram RK, Stein BD, Bakhoum SF, Snuderl M, Cotzia P, Healey JH, Mainolfi N, Suri V, Friedman A, Manfredi M, Sabatini DM, Jones DR, Yu M, Zhao JJ, Jain RK, Keshari KR, Davies MA, Vander Heiden MG, Hernando E, Mann M, Cantley LC, Pacold ME. Ngo B, et al. Among authors: mainolfi n. Cancer Discov. 2020 Sep;10(9):1352-1373. doi: 10.1158/2159-8290.CD-19-1228. Epub 2020 Jun 22. Cancer Discov. 2020. PMID: 32571778 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. 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
A small-molecule inhibitor of C5 complement protein.
Jendza K, Kato M, Salcius M, Srinivas H, De Erkenez A, Nguyen A, McLaughlin D, Be C, Wiesmann C, Murphy J, Bolduc P, Mogi M, Duca J, Namil A, Capparelli M, Darsigny V, Meredith E, Tichkule R, Ferrara L, Heyder J, Liu F, Horton PA, Romanowski MJ, Schirle M, Mainolfi N, Anderson K, Michaud GA. Jendza K, et al. Among authors: mainolfi n. Nat Chem Biol. 2019 Jul;15(7):666-668. doi: 10.1038/s41589-019-0303-9. Epub 2019 Jun 17. Nat Chem Biol. 2019. PMID: 31209353
Targeted protein degradation mechanisms.
Zhang Y, Loh C, Chen J, Mainolfi N. Zhang Y, et al. Among authors: mainolfi n. Drug Discov Today Technol. 2019 Apr;31:53-60. doi: 10.1016/j.ddtec.2019.01.001. Epub 2019 Jan 28. Drug Discov Today Technol. 2019. PMID: 31200860 Review.
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: mainolfi n. 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: mainolfi n. 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.
Serine Metabolism Supports Macrophage IL-1β Production.
Rodriguez AE, Ducker GS, Billingham LK, Martinez CA, Mainolfi N, Suri V, Friedman A, Manfredi MG, Weinberg SE, Rabinowitz JD, Chandel NS. Rodriguez AE, et al. Among authors: mainolfi n. Cell Metab. 2019 Apr 2;29(4):1003-1011.e4. doi: 10.1016/j.cmet.2019.01.014. Epub 2019 Feb 14. Cell Metab. 2019. PMID: 30773464 Free PMC article.
The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
Adams CM, Anderson K, Artman G 3rd, Bizec JC, Cepeda R, Elliott J, Fassbender E, Ghosh M, Hanks S, Hardegger LA, Hosagrahara VP, Jaffee B, Jendza K, Ji N, Johnson L, Lee W, Liu D, Liu F, Long D, Ma F, Mainolfi N, Meredith EL, Miranda K, Peng Y, Poor S, Powers J, Qiu Y, Rao C, Shen S, Sivak JM, Solovay C, Tarsa P, Woolfenden A, Zhang C, Zhang Y. Adams CM, et al. Among authors: mainolfi n. J Med Chem. 2018 Feb 22;61(4):1622-1635. doi: 10.1021/acs.jmedchem.7b01731. Epub 2018 Feb 5. J Med Chem. 2018. PMID: 29400470
21 results