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24 results

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Page 1
Discovery of KT-474─a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases.
Zheng X, Ji N, Campbell V, Slavin A, Zhu X, Chen D, Rong H, Enerson B, Mayo M, Sharma K, Browne CM, Klaus CR, Li H, Massa G, McDonald AA, Shi Y, Sintchak M, Skouras S, Walther DM, Yuan K, Zhang Y, Kelleher J, Liu G, Luo X, Mainolfi N, Weiss MM. Zheng X, et al. Among authors: mainolfi n. J Med Chem. 2024 Oct 24;67(20):18022-18037. doi: 10.1021/acs.jmedchem.4c01305. Epub 2024 Aug 16. J Med Chem. 2024. PMID: 39151120 Free PMC article. Clinical Trial.
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.
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
Weiss MM, Zheng X, Ji N, Browne CM, Campbell V, Chen D, Enerson B, Fei X, Huang X, Klaus CR, Li H, Mayo M, McDonald AA, Paul A, Rong H, Sharma K, Shi Y, Slavin A, Walther DM, Yuan K, Zhang Y, Zhu X, Kelleher J, Walker D, Mainolfi N. Weiss MM, et al. Among authors: mainolfi n. J Med Chem. 2024 Jul 11;67(13):10548-10566. doi: 10.1021/acs.jmedchem.3c01823. Epub 2024 Jun 26. J Med Chem. 2024. PMID: 38920289
KT-253, A Novel MDM2 Degrader and p53 Stabilizer, Has Superior Potency and Efficacy Than MDM2 Small Molecule Inhibitors.
Chutake YK, Mayo MF, Dumont N, Filiatrault J, Breitkopf SB, Cho P, Chen D, Dixit VS, Proctor WR, Kuhn EW, Bollinger Martinez S, McDonald AA, Qi J, Hu KN, Karnik R, Growney JD, Sharma K, Schalm SS, Gollerkeri AM, Mainolfi N, Williams JA, Weiss MM. Chutake YK, et al. Among authors: mainolfi n. Mol Cancer Ther. 2024 Dec 9. doi: 10.1158/1535-7163.MCT-24-0306. Online ahead of print. Mol Cancer Ther. 2024. PMID: 39648478
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
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