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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.
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.
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.
NITD-688, a pan-serotype inhibitor of the dengue virus NS4B protein, shows favorable pharmacokinetics and efficacy in preclinical animal models.
Moquin SA, Simon O, Karuna R, Lakshminarayana SB, Yokokawa F, Wang F, Saravanan C, Zhang J, Day CW, Chan K, Wang QY, Lu S, Dong H, Wan KF, Lim SP, Liu W, Seh CC, Chen YL, Xu H, Barkan DT, Kounde CS, Sim WLS, Wang G, Yeo HQ, Zou B, Chan WL, Ding M, Song JG, Li M, Osborne C, Blasco F, Sarko C, Beer D, Bonamy GMC, Sasseville VG, Shi PY, Diagana TT, Yeung BKS, Gu F. Moquin SA, et al. Among authors: chen yl. Sci Transl Med. 2021 Feb 3;13(579):eabb2181. doi: 10.1126/scitranslmed.abb2181. Sci Transl Med. 2021. PMID: 33536278
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 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.
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.
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
Chen YL, Yin Z, Lakshminarayana SB, Qing M, Schul W, Duraiswamy J, Kondreddi RR, Goh A, Xu HY, Yip A, Liu B, Weaver M, Dartois V, Keller TH, Shi PY. Chen YL, et al. Antimicrob Agents Chemother. 2010 Aug;54(8):3255-61. doi: 10.1128/AAC.00397-10. Epub 2010 Jun 1. Antimicrob Agents Chemother. 2010. PMID: 20516277 Free PMC article.
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
An adenosine nucleoside inhibitor of dengue virus.
Yin Z, Chen YL, Schul W, Wang QY, Gu F, Duraiswamy J, Kondreddi RR, Niyomrattanakit P, Lakshminarayana SB, Goh A, Xu HY, Liu W, Liu B, Lim JY, Ng CY, Qing M, Lim CC, Yip A, Wang G, Chan WL, Tan HP, Lin K, Zhang B, Zou G, Bernard KA, Garrett C, Beltz K, Dong M, Weaver M, He H, Pichota A, Dartois V, Keller TH, Shi PY. Yin Z, et al. Among authors: chen yl. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20435-9. doi: 10.1073/pnas.0907010106. Epub 2009 Nov 16. Proc Natl Acad Sci U S A. 2009. PMID: 19918064 Free PMC article.
4,259 results