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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: tuntland t. 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.
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: tuntland t. Trop Med Infect Dis. 2020 Feb 17;5(1):28. doi: 10.3390/tropicalmed5010028. Trop Med Infect Dis. 2020. PMID: 32079320 Free PMC article.
Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.
He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S, Jia Y, Bursulaya B, Kreusch A, Gao MY, Spraggon G, Baaten J, Clemmer L, Meeusen S, Huang D, Hill R, Nguyen-Tran V, Fathman J, Liu B, Tuntland T, Gordon P, Hollenbeck T, Ng K, Shi J, Bordone L, Liu H. He X, et al. Among authors: tuntland t. ACS Med Chem Lett. 2017 Sep 27;8(10):1048-1053. doi: 10.1021/acsmedchemlett.7b00258. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057049 Free PMC article.
Dual ALK and CDK4/6 Inhibition Demonstrates Synergy against Neuroblastoma.
Wood AC, Krytska K, Ryles HT, Infarinato NR, Sano R, Hansel TD, Hart LS, King FJ, Smith TR, Ainscow E, Grandinetti KB, Tuntland T, Kim S, Caponigro G, He YQ, Krupa S, Li N, Harris JL, Mossé YP. Wood AC, et al. Among authors: tuntland t. Clin Cancer Res. 2017 Jun 1;23(11):2856-2868. doi: 10.1158/1078-0432.CCR-16-1114. Epub 2016 Dec 16. Clin Cancer Res. 2017. PMID: 27986745 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: tuntland t. Nature. 2016 Sep 8;537(7619):229-233. doi: 10.1038/nature19339. Epub 2016 Aug 8. Nature. 2016. PMID: 27501246 Free PMC article.
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.
Michellys PY, Chen B, Jiang T, Jin Y, Lu W, Marsilje TH, Pei W, Uno T, Zhu X, Wu B, Nguyen TN, Bursulaya B, Lee C, Li N, Kim S, Tuntland T, Liu B, Sun F, Steffy A, Hood T. Michellys PY, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2016 Feb 1;26(3):1090-1096. doi: 10.1016/j.bmcl.2015.11.049. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26750252
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Choi HS, Rucker PV, Wang Z, Fan Y, Albaugh P, Chopiuk G, Gessier F, Sun F, Adrian F, Liu G, Hood T, Li N, Jia Y, Che J, McCormack S, Li A, Li J, Steffy A, Culazzo A, Tompkins C, Phung V, Kreusch A, Lu M, Hu B, Chaudhary A, Prashad M, Tuntland T, Liu B, Harris J, Seidel HM, Loren J, Molteni V. Choi HS, et al. Among authors: tuntland t. ACS Med Chem Lett. 2015 Mar 16;6(5):562-7. doi: 10.1021/acsmedchemlett.5b00050. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005534 Free PMC article.
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