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A small-molecule SUMOylation inhibitor activates antitumor immune responses and potentiates immune therapies in preclinical models.
Lightcap ES, Yu P, Grossman S, Song K, Khattar M, Xega K, He X, Gavin JM, Imaichi H, Garnsey JJ, Koenig E, Zhang H, Lu Z, Shah P, Fu Y, Milhollen MA, Hatton BA, Riceberg J, Shinde V, Li C, Minissale J, Yang X, England D, Klinghoffer RA, Langston S, Galvin K, Shapiro G, Pulukuri SM, Fuchs SY, Huszar D. Lightcap ES, et al. Among authors: england d. Sci Transl Med. 2021 Sep 15;13(611):eaba7791. doi: 10.1126/scitranslmed.aba7791. Epub 2021 Sep 15. Sci Transl Med. 2021. PMID: 34524860 Free PMC article.
Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor.
He X, Riceberg J, Soucy T, Koenig E, Minissale J, Gallery M, Bernard H, Yang X, Liao H, Rabino C, Shah P, Xega K, Yan ZH, Sintchak M, Bradley J, Xu H, Duffey M, England D, Mizutani H, Hu Z, Guo J, Chau R, Dick LR, Brownell JE, Newcomb J, Langston S, Lightcap ES, Bence N, Pulukuri SM. He X, et al. Among authors: england d. Nat Chem Biol. 2017 Nov;13(11):1164-1171. doi: 10.1038/nchembio.2463. Epub 2017 Sep 11. Nat Chem Biol. 2017. PMID: 28892090
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.
Langston SP, Grossman S, England D, Afroze R, Bence N, Bowman D, Bump N, Chau R, Chuang BC, Claiborne C, Cohen L, Connolly K, Duffey M, Durvasula N, Freeze S, Gallery M, Galvin K, Gaulin J, Gershman R, Greenspan P, Grieves J, Guo J, Gulavita N, Hailu S, He X, Hoar K, Hu Y, Hu Z, Ito M, Kim MS, Lane SW, Lok D, Lublinsky A, Mallender W, McIntyre C, Minissale J, Mizutani H, Mizutani M, Molchinova N, Ono K, Patil A, Qian M, Riceberg J, Shindi V, Sintchak MD, Song K, Soucy T, Wang Y, Xu H, Yang X, Zawadzka A, Zhang J, Pulukuri SM. Langston SP, et al. Among authors: england d. J Med Chem. 2021 Mar 11;64(5):2501-2520. doi: 10.1021/acs.jmedchem.0c01491. Epub 2021 Feb 25. J Med Chem. 2021. PMID: 33631934 Free article.
Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG.
Huang SC, Adhikari S, Afroze R, Brewer K, Calderwood EF, Chouitar J, England DB, Fisher C, Galvin KM, Gaulin J, Greenspan PD, Harrison SJ, Kim MS, Langston SP, Ma LT, Menon S, Mizutani H, Rezaei M, Smith MD, Zhang DM, Gould AE. Huang SC, et al. Among authors: england db. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1156-60. doi: 10.1016/j.bmcl.2016.01.049. Epub 2016 Jan 21. Bioorg Med Chem Lett. 2016. PMID: 26804230
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Gould AE, Adams R, Adhikari S, Aertgeerts K, Afroze R, Blackburn C, Calderwood EF, Chau R, Chouitar J, Duffey MO, England DB, Farrer C, Forsyth N, Garcia K, Gaulin J, Greenspan PD, Guo R, Harrison SJ, Huang SC, Iartchouk N, Janowick D, Kim MS, Kulkarni B, Langston SP, Liu JX, Ma LT, Menon S, Mizutani H, Paske E, Renou CC, Rezaei M, Rowland RS, Sintchak MD, Smith MD, Stroud SG, Tregay M, Tian Y, Veiby OP, Vos TJ, Vyskocil S, Williams J, Xu T, Yang JJ, Yano J, Zeng H, Zhang DM, Zhang Q, Galvin KM. Gould AE, et al. Among authors: england db. J Med Chem. 2011 Mar 24;54(6):1836-46. doi: 10.1021/jm101479y. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341678
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
Vyskocil S, Cardin D, Ciavarri J, Conlon J, Cullis C, England D, Gershman R, Gigstad K, Gipson K, Gould A, Greenspan P, Griffin R, Gulavita N, Harrison S, Hu Z, Hu Y, Hata A, Huang J, Huang SC, Janowick D, Jones M, Kolev V, Langston SP, Lee HM, Li G, Lok D, Ma L, Mai D, Malley J, Matsuda A, Mizutani H, Mizutani M, Molchanova N, Nunes E, Pusalkar S, Renou C, Rowland S, Sato Y, Shaw M, Shen L, Shi Z, Skene R, Soucy F, Stroud S, Xu H, Xu T, Abu-Yousif AO, Zhang J. Vyskocil S, et al. Among authors: england d. J Med Chem. 2021 May 27;64(10):6902-6923. doi: 10.1021/acs.jmedchem.1c00374. Epub 2021 May 17. J Med Chem. 2021. PMID: 34000802 Free article.
Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors.
Huang SC, Adhikari S, Brownell JE, Calderwood EF, Chouitar J, D'Amore NR, England DB, Foley K, Harrison SJ, LeRoy PJ, Lok D, Lublinsky A, Ma LT, Menon S, Yang Y, Zhang J, Gould AE. Huang SC, et al. Among authors: england db, d amore nr. Bioorg Med Chem. 2020 Oct 1;28(19):115681. doi: 10.1016/j.bmc.2020.115681. Epub 2020 Aug 4. Bioorg Med Chem. 2020. PMID: 32912429 Free article.
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
Blackburn C, Barrett C, Brunson M, Chin J, England D, Garcia K, Gigstad K, Gould A, Gutierrez J, Hoar K, Rowland RS, Tsu C, Ringeling J, Wager K, Xu H. Blackburn C, et al. Among authors: england d. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5450-4. doi: 10.1016/j.bmcl.2014.10.022. Bioorg Med Chem Lett. 2014. PMID: 25454270
206 results