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Page 1
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: thomas mp. 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.
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: thomas mp. Nature. 2009 Apr 9;458(7239):732-6. doi: 10.1038/nature07884. Nature. 2009. PMID: 19360080
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: thomas mp. Cancer Cell. 2012 Mar 20;21(3):388-401. doi: 10.1016/j.ccr.2012.02.009. Cancer Cell. 2012. PMID: 22439935 Free article.
Nedd8-activating enzyme inhibitor MLN4924 provides synergy with mitomycin C through interactions with ATR, BRCA1/BRCA2, and chromatin dynamics pathways.
Garcia K, Blank JL, Bouck DC, Liu XJ, Sappal DS, Hather G, Cosmopoulos K, Thomas MP, Kuranda M, Pickard MD, Liu R, Bandi S, Smith PG, Lightcap ES. Garcia K, et al. Among authors: thomas mp. Mol Cancer Ther. 2014 Jun;13(6):1625-35. doi: 10.1158/1535-7163.MCT-13-0634. Epub 2014 Mar 26. Mol Cancer Ther. 2014. PMID: 24672057
Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.
Puyang X, Furman C, Zheng GZ, Wu ZJ, Banka D, Aithal K, Agoulnik S, Bolduc DM, Buonamici S, Caleb B, Das S, Eckley S, Fekkes P, Hao MH, Hart A, Houtman R, Irwin S, Joshi JJ, Karr C, Kim A, Kumar N, Kumar P, Kuznetsov G, Lai WG, Larsen N, Mackenzie C, Martin LA, Melchers D, Moriarty A, Nguyen TV, Norris J, O'Shea M, Pancholi S, Prajapati S, Rajagopalan S, Reynolds DJ, Rimkunas V, Rioux N, Ribas R, Siu A, Sivakumar S, Subramanian V, Thomas M, Vaillancourt FH, Wang J, Wardell S, Wick MJ, Yao S, Yu L, Warmuth M, Smith PG, Zhu P, Korpal M. Puyang X, et al. Cancer Discov. 2018 Sep;8(9):1176-1193. doi: 10.1158/2159-8290.CD-17-1229. Epub 2018 Jul 10. Cancer Discov. 2018. PMID: 29991605
Modulation of splicing catalysis for therapeutic targeting of leukemia with mutations in genes encoding spliceosomal proteins.
Lee SC, Dvinge H, Kim E, Cho H, Micol JB, Chung YR, Durham BH, Yoshimi A, Kim YJ, Thomas M, Lobry C, Chen CW, Pastore A, Taylor J, Wang X, Krivtsov A, Armstrong SA, Palacino J, Buonamici S, Smith PG, Bradley RK, Abdel-Wahab O. Lee SC, et al. Nat Med. 2016 Jun;22(6):672-8. doi: 10.1038/nm.4097. Epub 2016 May 2. Nat Med. 2016. PMID: 27135740 Free PMC article.
Splicing modulation sensitizes chronic lymphocytic leukemia cells to venetoclax by remodeling mitochondrial apoptotic dependencies.
Ten Hacken E, Valentin R, Regis FFD, Sun J, Yin S, Werner L, Deng J, Gruber M, Wong J, Zheng M, Gill AL, Seiler M, Smith P, Thomas M, Buonamici S, Ghia EM, Kim E, Rassenti LZ, Burger JA, Kipps TJ, Meyerson ML, Bachireddy P, Wang L, Reed R, Neuberg D, Carrasco RD, Brooks AN, Letai A, Davids MS, Wu CJ. Ten Hacken E, et al. JCI Insight. 2018 Oct 4;3(19):e121438. doi: 10.1172/jci.insight.121438. JCI Insight. 2018. PMID: 30282833 Free PMC article.
H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers.
Seiler M, Yoshimi A, Darman R, Chan B, Keaney G, Thomas M, Agrawal AA, Caleb B, Csibi A, Sean E, Fekkes P, Karr C, Klimek V, Lai G, Lee L, Kumar P, Lee SC, Liu X, Mackenzie C, Meeske C, Mizui Y, Padron E, Park E, Pazolli E, Peng S, Prajapati S, Taylor J, Teng T, Wang J, Warmuth M, Yao H, Yu L, Zhu P, Abdel-Wahab O, Smith PG, Buonamici S. Seiler M, et al. Nat Med. 2018 May;24(4):497-504. doi: 10.1038/nm.4493. Epub 2018 Feb 19. Nat Med. 2018. PMID: 29457796 Free PMC article.
187 results