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Page 1
Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.
Nagle A, Biggart A, Be C, Srinivas H, Hein A, Caridha D, Sciotti RJ, Pybus B, Kreishman-Deitrick M, Bursulaya B, Lai YH, Gao MY, Liang F, Mathison CJN, Liu X, Yeh V, Smith J, Lerario I, Xie Y, Chianelli D, Gibney M, Berman A, Chen YL, Jiricek J, Davis LC, Liu X, Ballard J, Khare S, Eggimann FK, Luneau A, Groessl T, Shapiro M, Richmond W, Johnson K, Rudewicz PJ, Rao SPS, Thompson C, Tuntland T, Spraggon G, Glynne RJ, Supek F, Wiesmann C, Molteni V. Nagle A, et al. Among authors: chen yl. J Med Chem. 2020 Oct 8;63(19):10773-10781. doi: 10.1021/acs.jmedchem.0c00499. Epub 2020 Jul 29. J Med Chem. 2020. PMID: 32667203 Free PMC article.
Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors.
Saldivia M, Fang E, Ma X, Myburgh E, Carnielli JBT, Bower-Lepts C, Brown E, Ritchie R, Lakshminarayana SB, Chen YL, Patra D, Ornelas E, Koh HXY, Williams SL, Supek F, Paape D, McCulloch R, Kaiser M, Barrett MP, Jiricek J, Diagana TT, Mottram JC, Rao SPS. Saldivia M, et al. Among authors: chen yl. Nat Microbiol. 2020 Oct;5(10):1207-1216. doi: 10.1038/s41564-020-0745-6. Epub 2020 Jul 13. Nat Microbiol. 2020. PMID: 32661312 Free PMC article.
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Taft BR, Yokokawa F, Kirrane T, Mata AC, Huang R, Blaquiere N, Waldron G, Zou B, Simon O, Vankadara S, Chan WL, Ding M, Sim S, Straimer J, Guiguemde A, Lakshminarayana SB, Jain JP, Bodenreider C, Thompson C, Lanshoeft C, Shu W, Fang E, Qumber J, Chan K, Pei L, Chen YL, Schulz H, Lim J, Abas SN, Ang X, Liu Y, Angulo-Barturen I, Jiménez-Díaz MB, Gamo FJ, Crespo-Fernandez B, Rosenthal PJ, Cooper RA, Tumwebaze P, Aguiar ACC, Campo B, Campbell S, Wagner J, Diagana TT, Sarko C. Taft BR, et al. Among authors: chen yl. J Med Chem. 2022 Mar 10;65(5):3798-3813. doi: 10.1021/acs.jmedchem.1c01995. Epub 2022 Mar 1. J Med Chem. 2022. PMID: 35229610 Free PMC article.
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Koester DC, Marx VM, Williams S, Jiricek J, Dauphinais M, René O, Miller SL, Zhang L, Patra D, Chen YL, Cheung H, Gable J, Lakshminarayana SB, Osborne C, Galarneau JR, Kulkarni U, Richmond W, Bretz A, Xiao L, Supek F, Wiesmann C, Honnappa S, Be C, Mäser P, Kaiser M, Ritchie R, Barrett MP, Diagana TT, Sarko C, Rao SPS. Koester DC, et al. Among authors: chen yl. J Med Chem. 2022 Sep 8;65(17):11776-11787. doi: 10.1021/acs.jmedchem.2c00791. Epub 2022 Aug 22. J Med Chem. 2022. PMID: 35993839 Free PMC article.
Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections.
Rao SPS, Gould MK, Noeske J, Saldivia M, Jumani RS, Ng PS, René O, Chen YL, Kaiser M, Ritchie R, Francisco AF, Johnson N, Patra D, Cheung H, Deniston C, Schenk AD, Cortopassi WA, Schmidt RS, Wiedemar N, Thomas B, Palkar R, Ghafar NA, Manoharan V, Luu C, Gable JE, Wan KF, Myburgh E, Mottram JC, Barnes W, Walker J, Wartchow C, Aziz N, Osborne C, Wagner J, Sarko C, Kelly JM, Manjunatha UH, Mäser P, Jiricek J, Lakshminarayana SB, Barrett MP, Diagana TT. Rao SPS, et al. Among authors: chen yl. Science. 2023 Jun 30;380(6652):1349-1356. doi: 10.1126/science.adh0614. Epub 2023 Jun 29. Science. 2023. PMID: 37384702 Free article.
N-sulfonylanthranilic acid derivatives as allosteric inhibitors of dengue viral RNA-dependent RNA polymerase.
Yin Z, Chen YL, Kondreddi RR, Chan WL, Wang G, Ng RH, Lim JY, Lee WY, Jeyaraj DA, Niyomrattanakit P, Wen D, Chao A, Glickman JF, Voshol H, Mueller D, Spanka C, Dressler S, Nilar S, Vasudevan SG, Shi PY, Keller TH. Yin Z, et al. Among authors: chen yl. J Med Chem. 2009 Dec 24;52(24):7934-7. doi: 10.1021/jm901044z. J Med Chem. 2009. PMID: 20014868
Structure-activity relationship of uridine-based nucleoside phosphoramidate prodrugs for inhibition of dengue virus RNA-dependent RNA polymerase.
Wang G, Lim SP, Chen YL, Hunziker J, Rao R, Gu F, Seh CC, Ghafar NA, Xu H, Chan K, Lin X, Saunders OL, Fenaux M, Zhong W, Shi PY, Yokokawa F. Wang G, et al. Among authors: chen yl. Bioorg Med Chem Lett. 2018 Jul 15;28(13):2324-2327. doi: 10.1016/j.bmcl.2018.04.069. Epub 2018 May 3. Bioorg Med Chem Lett. 2018. PMID: 29801997
Functional analysis of two cavities in flavivirus NS5 polymerase.
Zou G, Chen YL, Dong H, Lim CC, Yap LJ, Yau YH, Shochat SG, Lescar J, Shi PY. Zou G, et al. Among authors: chen yl. J Biol Chem. 2011 Apr 22;286(16):14362-72. doi: 10.1074/jbc.M110.214189. Epub 2011 Feb 23. J Biol Chem. 2011. PMID: 21349834 Free PMC article.
Ten years of dengue drug discovery: progress and prospects.
Lim SP, Wang QY, Noble CG, Chen YL, Dong H, Zou B, Yokokawa F, Nilar S, Smith P, Beer D, Lescar J, Shi PY. Lim SP, et al. Among authors: chen yl. Antiviral Res. 2013 Nov;100(2):500-19. doi: 10.1016/j.antiviral.2013.09.013. Epub 2013 Sep 27. Antiviral Res. 2013. PMID: 24076358 Review.
A Cyclic Phosphoramidate Prodrug of 2'-Deoxy-2'-Fluoro-2'-C-Methylguanosine for the Treatment of Dengue Virus Infection.
Karuna R, Yokokawa F, Wang K, Zhang J, Xu H, Wang G, Ding M, Chan WL, Abdul Ghafar N, Leonardi A, Seh CC, Seah PG, Liu W, Srinivasa RPS, Lim SP, Lakshminarayana SB, Growcott E, Babu S, Fenaux M, Zhong W, Gu F, Shi PY, Blasco F, Chen YL. Karuna R, et al. Among authors: chen yl. Antimicrob Agents Chemother. 2020 Nov 17;64(12):e00654-20. doi: 10.1128/AAC.00654-20. Print 2020 Nov 17. Antimicrob Agents Chemother. 2020. PMID: 32958712 Free PMC article.
4,444 results