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Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome.
Deni I, Stokes BH, Ward KE, Fairhurst KJ, Pasaje CFA, Yeo T, Akbar S, Park H, Muir R, Bick DS, Zhan W, Zhang H, Liu YJ, Ng CL, Kirkman LA, Almaliti J, Gould AE, Duffey M, O'Donoghue AJ, Uhlemann AC, Niles JC, da Fonseca PCA, Gerwick WH, Lin G, Bogyo M, Fidock DA. Deni I, et al. Among authors: lin g. Cell Chem Biol. 2023 May 18;30(5):470-485.e6. doi: 10.1016/j.chembiol.2023.03.002. Epub 2023 Mar 23. Cell Chem Biol. 2023. PMID: 36963402 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: lin g. 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.
Improvement of Asparagine Ethylenediamines as Anti-malarial Plasmodium-Selective Proteasome Inhibitors.
Zhan W, Visone J, Ouellette T, Harris JC, Wang R, Zhang H, Singh PK, Ginn J, Sukenick G, Wong TT, Okoro JI, Scales RM, Tumwebaze PK, Rosenthal PJ, Kafsack BFC, Cooper RA, Meinke PT, Kirkman LA, Lin G. Zhan W, et al. Among authors: lin g. J Med Chem. 2019 Jul 11;62(13):6137-6145. doi: 10.1021/acs.jmedchem.9b00363. Epub 2019 Jun 20. J Med Chem. 2019. PMID: 31177777 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: lin g. 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.
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: lin g. 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.
Microbial proteasomes as drug targets.
Zhang H, Lin G. Zhang H, et al. Among authors: lin g. PLoS Pathog. 2021 Dec 9;17(12):e1010058. doi: 10.1371/journal.ppat.1010058. eCollection 2021 Dec. PLoS Pathog. 2021. PMID: 34882737 Free PMC article. Review.
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: lin g. 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.
Susceptibilities of Ugandan Plasmodium falciparum Isolates to Proteasome Inhibitors.
Garg S, Kreutzfeld O, Chelebieva S, Tumwebaze PK, Byaruhanga O, Okitwi M, Orena S, Katairo T, Nsobya SL, Conrad MD, Aydemir O, Legac J, Gould AE, Bayles BR, Bailey JA, Duffey M, Lin G, Kirkman LA, Cooper RA, Rosenthal PJ. Garg S, et al. Among authors: lin g. Antimicrob Agents Chemother. 2022 Oct 18;66(10):e0081722. doi: 10.1128/aac.00817-22. Epub 2022 Sep 12. Antimicrob Agents Chemother. 2022. PMID: 36094216 Free PMC article.
7,383 results