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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: spraggon g. 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: spraggon g. Nature. 2016 Sep 8;537(7619):229-233. doi: 10.1038/nature19339. Epub 2016 Aug 8. Nature. 2016. PMID: 27501246 Free PMC article.
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY. Lelais G, et al. Among authors: spraggon g. J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19. J Med Chem. 2016. PMID: 27433829
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: spraggon g. 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.
Structure-Based Design of Selective LONP1 Inhibitors for Probing In Vitro Biology.
Kingsley LJ, He X, McNeill M, Nelson J, Nikulin V, Ma Z, Lu W, Zhou VW, Manuia M, Kreusch A, Gao MY, Witmer D, Vaillancourt MT, Lu M, Greenblatt S, Lee C, Vashisht A, Bender S, Spraggon G, Michellys PY, Jia Y, Haling JR, Lelais G. Kingsley LJ, et al. Among authors: spraggon g. J Med Chem. 2021 Apr 22;64(8):4857-4869. doi: 10.1021/acs.jmedchem.0c02152. Epub 2021 Apr 6. J Med Chem. 2021. PMID: 33821636
Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design.
Tully DC, Vidal A, Chatterjee AK, Williams JA, Roberts MJ, Petrassi HM, Spraggon G, Bursulaya B, Pacoma R, Shipway A, Schumacher AM, Danahay H, Harris JL. Tully DC, et al. Among authors: spraggon g. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5895-9. doi: 10.1016/j.bmcl.2008.08.029. Epub 2008 Aug 14. Bioorg Med Chem Lett. 2008. PMID: 18752942
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
Tully DC, Liu H, Alper PB, Chatterjee AK, Epple R, Roberts MJ, Williams JA, Nguyen KT, Woodmansee DH, Tumanut C, Li J, Spraggon G, Chang J, Tuntland T, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: spraggon g. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1975-80. doi: 10.1016/j.bmcl.2005.12.095. Epub 2006 Jan 30. Bioorg Med Chem Lett. 2006. PMID: 16446091
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.
Tully DC, Liu H, Chatterjee AK, Alper PB, Epple R, Williams JA, Roberts MJ, Woodmansee DH, Masick BT, Tumanut C, Li J, Spraggon G, Hornsby M, Chang J, Tuntland T, Hollenbeck T, Gordon P, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: spraggon g. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5112-7. doi: 10.1016/j.bmcl.2006.07.033. Epub 2006 Jul 28. Bioorg Med Chem Lett. 2006. PMID: 16876402
125 results