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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. Among authors: dick lr. Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474. Epub 2018 Jan 15. Nat Med. 2018. PMID: 29334375
Treatment-emergent mutations in NAEβ confer resistance to the NEDD8-activating enzyme inhibitor MLN4924.
Milhollen MA, Thomas MP, Narayanan U, Traore T, Riceberg J, Amidon BS, Bence NF, Bolen JB, Brownell J, Dick LR, Loke HK, McDonald AA, Ma J, Manfredi MG, Sells TB, Sintchak MD, Yang X, Xu Q, Koenig EM, Gavin JM, Smith PG. Milhollen MA, et al. Among authors: dick lr. Cancer Cell. 2012 Mar 20;21(3):388-401. doi: 10.1016/j.ccr.2012.02.009. Cancer Cell. 2012. PMID: 22439935 Free 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: dick lr. Nat Chem Biol. 2017 Nov;13(11):1164-1171. doi: 10.1038/nchembio.2463. Epub 2017 Sep 11. Nat Chem Biol. 2017. PMID: 28892090
An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer.
Soucy TA, Smith PG, Milhollen MA, Berger AJ, Gavin JM, Adhikari S, Brownell JE, Burke KE, Cardin DP, Critchley S, Cullis CA, Doucette A, Garnsey JJ, Gaulin JL, Gershman RE, Lublinsky AR, McDonald A, Mizutani H, Narayanan U, Olhava EJ, Peluso S, Rezaei M, Sintchak MD, Talreja T, Thomas MP, Traore T, Vyskocil S, Weatherhead GS, Yu J, Zhang J, Dick LR, Claiborne CF, Rolfe M, Bolen JB, Langston SP. Soucy TA, et al. Among authors: dick lr. Nature. 2009 Apr 9;458(7239):732-6. doi: 10.1038/nature07884. Nature. 2009. PMID: 19360080
Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer.
Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu J, Yang Y, Hales P, Bruzzese F, Liu J, Blank J, Garcia K, Tsu C, Dick L, Fleming P, Yu L, Manfredi M, Rolfe M, Bolen J. Kupperman E, et al. Cancer Res. 2010 Mar 1;70(5):1970-80. doi: 10.1158/0008-5472.CAN-09-2766. Epub 2010 Feb 16. Cancer Res. 2010. PMID: 20160034
Mechanistic studies on activation of ubiquitin and di-ubiquitin-like protein, FAT10, by ubiquitin-like modifier activating enzyme 6, Uba6.
Gavin JM, Chen JJ, Liao H, Rollins N, Yang X, Xu Q, Ma J, Loke HK, Lingaraj T, Brownell JE, Mallender WD, Gould AE, Amidon BS, Dick LR. Gavin JM, et al. Among authors: dick lr. J Biol Chem. 2012 May 4;287(19):15512-22. doi: 10.1074/jbc.M111.336198. Epub 2012 Mar 15. J Biol Chem. 2012. PMID: 22427669 Free PMC 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: dick lr. 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.
54 results