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Page 1
Macrocyclic Peptides that Selectively Inhibit the Mycobacterium tuberculosis Proteasome.
Zhang H, Hsu HC, Kahne SC, Hara R, Zhan W, Jiang X, Burns-Huang K, Ouellette T, Imaeda T, Okamoto R, Kawasaki M, Michino M, Wong TT, Toita A, Yukawa T, Moraca F, Vendome J, Saha P, Sato K, Aso K, Ginn J, Meinke PT, Foley M, Nathan CF, Darwin KH, Li H, Lin G. Zhang H, et al. Among authors: michino m. J Med Chem. 2021 May 13;64(9):6262-6272. doi: 10.1021/acs.jmedchem.1c00296. Epub 2021 May 5. J Med Chem. 2021. PMID: 33949190 Free PMC article.
Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance.
Kirkman LA, Zhan W, Visone J, Dziedziech A, Singh PK, Fan H, Tong X, Bruzual I, Hara R, Kawasaki M, Imaeda T, Okamoto R, Sato K, Michino M, Alvaro EF, Guiang LF, Sanz L, Mota DJ, Govindasamy K, Wang R, Ling Y, Tumwebaze PK, Sukenick G, Shi L, Vendome J, Bhanot P, Rosenthal PJ, Aso K, Foley MA, Cooper RA, Kafsack B, Doggett JS, Nathan CF, Lin G. Kirkman LA, et al. Among authors: michino m. Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6863-E6870. doi: 10.1073/pnas.1806109115. Epub 2018 Jul 2. Proc Natl Acad Sci U S A. 2018. PMID: 29967165 Free PMC article.
Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression.
Lama L, Adura C, Xie W, Tomita D, Kamei T, Kuryavyi V, Gogakos T, Steinberg JI, Miller M, Ramos-Espiritu L, Asano Y, Hashizume S, Aida J, Imaeda T, Okamoto R, Jennings AJ, Michino M, Kuroita T, Stamford A, Gao P, Meinke P, Glickman JF, Patel DJ, Tuschl T. Lama L, et al. Among authors: michino m. Nat Commun. 2019 May 21;10(1):2261. doi: 10.1038/s41467-019-08620-4. Nat Commun. 2019. PMID: 31113940 Free PMC article.
Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.
Mullarky E, Xu J, Robin AD, Huggins DJ, Jennings A, Noguchi N, Olland A, Lakshminarasimhan D, Miller M, Tomita D, Michino M, Su T, Zhang G, Stamford AW, Meinke PT, Kargman S, Cantley LC. Mullarky E, et al. Among authors: michino m. Bioorg Med Chem Lett. 2019 Sep 1;29(17):2503-2510. doi: 10.1016/j.bmcl.2019.07.011. Epub 2019 Jul 6. Bioorg Med Chem Lett. 2019. PMID: 31327531 Free PMC article.
Selective Phenylimidazole-Based Inhibitors of the Mycobacterium tuberculosis Proteasome.
Zhan W, Hsu HC, Morgan T, Ouellette T, Burns-Huang K, Hara R, Wright AG, Imaeda T, Okamoto R, Sato K, Michino M, Ramjee M, Aso K, Meinke PT, Foley M, Nathan CF, Li H, Lin G. Zhan W, et al. Among authors: michino m. J Med Chem. 2019 Oct 24;62(20):9246-9253. doi: 10.1021/acs.jmedchem.9b01187. Epub 2019 Oct 15. J Med Chem. 2019. PMID: 31560200 Free PMC article.
Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti-malaria Activity in Humanized Mice.
Zhan W, Zhang H, Ginn J, Leung A, Liu YJ, Michino M, Toita A, Okamoto R, Wong TT, Imaeda T, Hara R, Yukawa T, Chelebieva S, Tumwebaze PK, Lafuente-Monasterio MJ, Martinez-Martinez MS, Vendome J, Beuming T, Sato K, Aso K, Rosenthal PJ, Cooper RA, Meinke PT, Nathan CF, Kirkman LA, Lin G. Zhan W, et al. Among authors: michino m. Angew Chem Int Ed Engl. 2021 Apr 19;60(17):9279-9283. doi: 10.1002/anie.202015845. Epub 2021 Mar 11. Angew Chem Int Ed Engl. 2021. PMID: 33433953 Free PMC article.
Whole Cell Active Inhibitors of Mycobacterial Lipoamide Dehydrogenase Afford Selectivity over the Human Enzyme through Tight Binding Interactions.
Ginn J, Jiang X, Sun S, Michino M, Huggins DJ, Mbambo Z, Jansen R, Rhee KY, Arango N, Lima CD, Liverton N, Imaeda T, Okamoto R, Kuroita T, Aso K, Stamford A, Foley M, Meinke PT, Nathan C, Bryk R. Ginn J, et al. Among authors: michino m. ACS Infect Dis. 2021 Feb 12;7(2):435-444. doi: 10.1021/acsinfecdis.0c00788. Epub 2021 Feb 2. ACS Infect Dis. 2021. PMID: 33527832 Free PMC article.
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).
Fushimi M, Buck H, Balbach M, Gorovyy A, Ferreira J, Rossetti T, Kaur N, Levin LR, Buck J, Quast J, van den Heuvel J, Steegborn C, Finkin-Groner E, Kargman S, Michino M, Foley MA, Miller M, Liverton NJ, Huggins DJ, Meinke PT. Fushimi M, et al. Among authors: michino m. ACS Med Chem Lett. 2021 Jul 14;12(8):1283-1287. doi: 10.1021/acsmedchemlett.1c00273. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34413957 Free PMC article.
A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors.
Liang R, Tomita D, Sasaki Y, Ginn J, Michino M, Huggins DJ, Baxt L, Kargman S, Shahid M, Aso K, Duggan M, Stamford AW, DeStanchina E, Liverton N, Meinke PT, Foley MA, Phillips RE. Liang R, et al. Among authors: michino m. ACS Med Chem Lett. 2022 Feb 10;13(3):377-387. doi: 10.1021/acsmedchemlett.1c00448. eCollection 2022 Mar 10. ACS Med Chem Lett. 2022. PMID: 35300079 Free PMC article.
Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors.
Zhang H, Ginn J, Zhan W, Liu YJ, Leung A, Toita A, Okamoto R, Wong TT, Imaeda T, Hara R, Yukawa T, Michino M, Vendome J, Beuming T, Sato K, Aso K, Meinke PT, Nathan CF, Kirkman LA, Lin G. Zhang H, et al. Among authors: michino m. J Med Chem. 2022 Jul 14;65(13):9350-9375. doi: 10.1021/acs.jmedchem.2c00611. Epub 2022 Jun 21. J Med Chem. 2022. PMID: 35727231 Free PMC article.
38 results