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Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ.
Brownell JE, Sintchak MD, Gavin JM, Liao H, Bruzzese FJ, Bump NJ, Soucy TA, Milhollen MA, Yang X, Burkhardt AL, Ma J, Loke HK, Lingaraj T, Wu D, Hamman KB, Spelman JJ, Cullis CA, Langston SP, Vyskocil S, Sells TB, Mallender WD, Visiers I, Li P, Claiborne CF, Rolfe M, Bolen JB, Dick LR. Brownell JE, et al. Among authors: bump nj. Mol Cell. 2010 Jan 15;37(1):102-11. doi: 10.1016/j.molcel.2009.12.024. Mol Cell. 2010. PMID: 20129059 Free article.
A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment.
Hyer ML, Milhollen MA, Ciavarri J, Fleming P, Traore T, Sappal D, Huck J, Shi J, Gavin J, Brownell J, Yang Y, Stringer B, Griffin R, Bruzzese F, Soucy T, Duffy J, Rabino C, Riceberg J, Hoar K, Lublinsky A, Menon S, Sintchak M, Bump N, Pulukuri SM, Langston S, Tirrell S, Kuranda M, Veiby P, Newcomb J, Li P, Wu JT, Powe J, Dick LR, Greenspan P, Galvin K, Manfredi M, Claiborne C, Amidon BS, Bence NF. Hyer ML, et al. Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474. Epub 2018 Jan 15. Nat Med. 2018. PMID: 29334375
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. 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.
Mechanistic study of Uba5 enzyme and the Ufm1 conjugation pathway.
Gavin JM, Hoar K, Xu Q, Ma J, Lin Y, Chen J, Chen W, Bruzzese FJ, Harrison S, Mallender WD, Bump NJ, Sintchak MD, Bence NF, Li P, Dick LR, Gould AE, Chen JJ. Gavin JM, et al. Among authors: bump nj. J Biol Chem. 2014 Aug 15;289(33):22648-22658. doi: 10.1074/jbc.M114.573972. Epub 2014 Jun 25. J Biol Chem. 2014. PMID: 24966333 Free PMC article.
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Duffey MO, Vos TJ, Adams R, Alley J, Anthony J, Barrett C, Bharathan I, Bowman D, Bump NJ, Chau R, Cullis C, Driscoll DL, Elder A, Forsyth N, Frazer J, Guo J, Guo L, Hyer ML, Janowick D, Kulkarni B, Lai SJ, Lasky K, Li G, Li J, Liao D, Little J, Peng B, Qian MG, Reynolds DJ, Rezaei M, Scott MP, Sells TB, Shinde V, Shi QJ, Sintchak MD, Soucy F, Sprott KT, Stroud SG, Nestor M, Visiers I, Weatherhead G, Ye Y, D'Amore N. Duffey MO, et al. Among authors: bump nj. J Med Chem. 2012 Jan 12;55(1):197-208. doi: 10.1021/jm2011172. Epub 2011 Dec 5. J Med Chem. 2012. PMID: 22070629
Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Blackburn C, Barrett C, Blank JL, Bruzzese FJ, Bump N, Dick LR, Fleming P, Garcia K, Hales P, Hu Z, Jones M, Liu JX, Sappal DS, Sintchak MD, Tsu C, Gigstad KM. Blackburn C, et al. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6581-6. doi: 10.1016/j.bmcl.2010.09.032. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20875739
20 results