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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. 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.
Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness.
Khare S, Nagle AS, Biggart A, Lai YH, Liang F, Davis LC, Barnes SW, Mathison CJ, Myburgh E, Gao MY, Gillespie JR, Liu X, Tan JL, Stinson M, Rivera IC, Ballard J, Yeh V, Groessl T, Federe G, Koh HX, Venable JD, Bursulaya B, Shapiro M, Mishra PK, Spraggon G, Brock A, Mottram JC, Buckner FS, Rao SP, Wen BG, Walker JR, Tuntland T, Molteni V, Glynne RJ, Supek F. Khare S, et al. Among authors: nagle as. Nature. 2016 Sep 8;537(7619):229-233. doi: 10.1038/nature19339. Epub 2016 Aug 8. Nature. 2016. PMID: 27501246 Free PMC article.
Anti-Trypanosomal Proteasome Inhibitors Cure Hemolymphatic and Meningoencephalic Murine Infection Models of African Trypanosomiasis.
Rao SPS, Lakshminarayana SB, Jiricek J, Kaiser M, Ritchie R, Myburgh E, Supek F, Tuntland T, Nagle A, Molteni V, Mäser P, Mottram JC, Barrett MP, Diagana TT. Rao SPS, et al. Among authors: nagle a. Trop Med Infect Dis. 2020 Feb 17;5(1):28. doi: 10.3390/tropicalmed5010028. Trop Med Infect Dis. 2020. PMID: 32079320 Free PMC article.
Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.
Nagle A, Wu T, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Liu B, Hollenbeck T, Tuntland T, Isbell J, Chuan T, Alper PB, Fischli C, Brun R, Lakshminarayana SB, Rottmann M, Diagana TT, Winzeler EA, Glynne R, Tully DC, Chatterjee AK. Nagle A, et al. J Med Chem. 2012 May 10;55(9):4244-73. doi: 10.1021/jm300041e. Epub 2012 Apr 23. J Med Chem. 2012. PMID: 22524250 Free PMC article.
Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
Tatipaka HB, Gillespie JR, Chatterjee AK, Norcross NR, Hulverson MA, Ranade RM, Nagendar P, Creason SA, McQueen J, Duster NA, Nagle A, Supek F, Molteni V, Wenzler T, Brun R, Glynne R, Buckner FS, Gelb MH. Tatipaka HB, et al. Among authors: nagle a. J Med Chem. 2014 Feb 13;57(3):828-35. doi: 10.1021/jm401178t. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24354316 Free PMC article.
Imidazolopiperazines: hit to lead optimization of new antimalarial agents.
Wu T, Nagle A, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Goh A, Lakshminarayana SB, Wu J, Ang HQ, Zeng P, Kang ML, Tan W, Tan M, Ye N, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Hollenbeck T, Tuntland T, Isbell J, Fischli C, Brun R, Rottmann M, Dartois V, Keller T, Diagana T, Winzeler E, Glynne R, Tully DC, Chatterjee AK. Wu T, et al. Among authors: nagle a. J Med Chem. 2011 Jul 28;54(14):5116-30. doi: 10.1021/jm2003359. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21644570 Free PMC article.
Cell-based optimization of novel benzamides as potential antimalarial leads.
Wu T, Nagle A, Sakata T, Henson K, Borboa R, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, Isbell J, Deng X, Gray NS, Tully DC, Chatterjee AK. Wu T, et al. Among authors: nagle a. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6970-4. doi: 10.1016/j.bmcl.2009.10.050. Epub 2009 Oct 29. Bioorg Med Chem Lett. 2009. PMID: 19879133 Free PMC article.
Lead optimization of imidazopyrazines: a new class of antimalarial with activity on Plasmodium liver stages.
Zou B, Nagle A, Chatterjee AK, Leong SY, Tan LJ, Sim WL, Mishra P, Guntapalli P, Tully DC, Lakshminarayana SB, Lim CS, Tan YC, Abas SN, Bodenreider C, Kuhen KL, Gagaring K, Borboa R, Chang J, Li C, Hollenbeck T, Tuntland T, Zeeman AM, Kocken CH, McNamara C, Kato N, Winzeler EA, Yeung BK, Diagana TT, Smith PW, Roland J. Zou B, et al. Among authors: nagle a. ACS Med Chem Lett. 2014 Jul 6;5(8):947-50. doi: 10.1021/ml500244m. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147620 Free PMC article.
Targeting Plasmodium PI(4)K to eliminate malaria.
McNamara CW, Lee MC, Lim CS, Lim SH, Roland J, Simon O, Yeung BK, Chatterjee AK, McCormack SL, Manary MJ, Zeeman AM, Dechering KJ, Kumar TS, Henrich PP, Gagaring K, Ibanez M, Kato N, Kuhen KL, Fischli C, Nagle A, Rottmann M, Plouffe DM, Bursulaya B, Meister S, Rameh L, Trappe J, Haasen D, Timmerman M, Sauerwein RW, Suwanarusk R, Russell B, Renia L, Nosten F, Tully DC, Kocken CH, Glynne RJ, Bodenreider C, Fidock DA, Diagana TT, Winzeler EA. McNamara CW, et al. Among authors: nagle a. Nature. 2013 Dec 12;504(7479):248-253. doi: 10.1038/nature12782. Epub 2013 Nov 27. Nature. 2013. PMID: 24284631 Free PMC article.
160 results