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Page 1
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: langston sp. Mol Cell. 2010 Jan 15;37(1):102-11. doi: 10.1016/j.molcel.2009.12.024. Mol Cell. 2010. PMID: 20129059 Free article.
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: langston sp. Nature. 2009 Apr 9;458(7239):732-6. doi: 10.1038/nature07884. Nature. 2009. PMID: 19360080
MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF-{kappa}B-dependent lymphoma.
Milhollen MA, Traore T, Adams-Duffy J, Thomas MP, Berger AJ, Dang L, Dick LR, Garnsey JJ, Koenig E, Langston SP, Manfredi M, Narayanan U, Rolfe M, Staudt LM, Soucy TA, Yu J, Zhang J, Bolen JB, Smith PG. Milhollen MA, et al. Among authors: langston sp. Blood. 2010 Sep 2;116(9):1515-23. doi: 10.1182/blood-2010-03-272567. Epub 2010 Jun 4. Blood. 2010. PMID: 20525923 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.
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. Nat Chem Biol. 2017 Nov;13(11):1164-1171. doi: 10.1038/nchembio.2463. Epub 2017 Sep 11. Nat Chem Biol. 2017. PMID: 28892090
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: langston sp. J Med Chem. 2011 Mar 24;54(6):1836-46. doi: 10.1021/jm101479y. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341678
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. 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.
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: langston sp. 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.
29 results