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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: yang x. 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: yang x. 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: yang x. 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.
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: yang x. Cancer Cell. 2012 Mar 20;21(3):388-401. doi: 10.1016/j.ccr.2012.02.009. Cancer Cell. 2012. PMID: 22439935 Free article.
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: yang x. Mol Cell. 2010 Jan 15;37(1):102-11. doi: 10.1016/j.molcel.2009.12.024. Mol Cell. 2010. PMID: 20129059 Free article.
Mechanistic studies of substrate-assisted inhibition of ubiquitin-activating enzyme by adenosine sulfamate analogues.
Chen JJ, Tsu CA, Gavin JM, Milhollen MA, Bruzzese FJ, Mallender WD, Sintchak MD, Bump NJ, Yang X, Ma J, Loke HK, Xu Q, Li P, Bence NF, Brownell JE, Dick LR. Chen JJ, et al. Among authors: yang x. J Biol Chem. 2011 Nov 25;286(47):40867-77. doi: 10.1074/jbc.M111.279984. Epub 2011 Oct 3. J Biol Chem. 2011. PMID: 21969368 Free PMC article.
., Bruzzese, F. J., Bump, N. J., Soucy, T. A., Milhollen, M. A., Yang, X., Burkhardt, A. L., Ma, J., Loke, H. K., Lingaraj, T., Wu, D., Hamman, K. ...
., Bruzzese, F. J., Bump, N. J., Soucy, T. A., Milhollen, M. A., Yang, X., Burkhardt, A. L., Ma, J., Loke, H. K., Lingaraj, T. …
Antibody-free detection of cellular neddylation dynamics of Cullin1.
Schwinn MK, Hoang T, Yang X, Zhao X, Ma J, Li P, Wood KV, Mallender WD, Bembenek ME, Yan ZH. Schwinn MK, et al. Among authors: yang x. Anal Biochem. 2018 Aug 15;555:67-72. doi: 10.1016/j.ab.2018.05.002. Epub 2018 May 5. Anal Biochem. 2018. PMID: 29733811
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