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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ. Rai G, et al. Among authors: cheff dm. J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29120638 Free PMC article.
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.
Urban DJ, Martinez NJ, Davis MI, Brimacombe KR, Cheff DM, Lee TD, Henderson MJ, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall MD. Urban DJ, et al. Among authors: cheff dm. Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x. Sci Rep. 2017. PMID: 28986582 Free PMC article.
Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.
Yang SM, Martinez NJ, Yasgar A, Danchik C, Johansson C, Wang Y, Baljinnyam B, Wang AQ, Xu X, Shah P, Cheff D, Wang XS, Roth J, Lal-Nag M, Dunford JE, Oppermann U, Vasiliou V, Simeonov A, Jadhav A, Maloney DJ. Yang SM, et al. J Med Chem. 2018 Jun 14;61(11):4883-4903. doi: 10.1021/acs.jmedchem.8b00270. Epub 2018 May 31. J Med Chem. 2018. PMID: 29767973 Free PMC article.
High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2.
Coussens NP, Kales SC, Henderson MJ, Lee OW, Horiuchi KY, Wang Y, Chen Q, Kuznetsova E, Wu J, Chakka S, Cheff DM, Cheng KC, Shinn P, Brimacombe KR, Shen M, Simeonov A, Lal-Nag M, Ma H, Jadhav A, Hall MD. Coussens NP, et al. Among authors: cheff dm. J Biol Chem. 2018 Aug 31;293(35):13750-13765. doi: 10.1074/jbc.RA118.004274. Epub 2018 Jun 26. J Biol Chem. 2018. PMID: 29945974 Free PMC article.
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
Kearney SE, Zahoránszky-Kőhalmi G, Brimacombe KR, Henderson MJ, Lynch C, Zhao T, Wan KK, Itkin Z, Dillon C, Shen M, Cheff DM, Lee TD, Bougie D, Cheng K, Coussens NP, Dorjsuren D, Eastman RT, Huang R, Iannotti MJ, Karavadhi S, Klumpp-Thomas C, Roth JS, Sakamuru S, Sun W, Titus SA, Yasgar A, Zhang YQ, Zhao J, Andrade RB, Brown MK, Burns NZ, Cha JK, Mevers EE, Clardy J, Clement JA, Crooks PA, Cuny GD, Ganor J, Moreno J, Morrill LA, Picazo E, Susick RB, Garg NK, Goess BC, Grossman RB, Hughes CC, Johnston JN, Joullie MM, Kinghorn AD, Kingston DGI, Krische MJ, Kwon O, Maimone TJ, Majumdar S, Maloney KN, Mohamed E, Murphy BT, Nagorny P, Olson DE, Overman LE, Brown LE, Snyder JK, Porco JA Jr, Rivas F, Ross SA, Sarpong R, Sharma I, Shaw JT, Xu Z, Shen B, Shi W, Stephenson CRJ, Verano AL, Tan DS, Tang Y, Taylor RE, Thomson RJ, Vosburg DA, Wu J, Wuest WM, Zakarian A, Zhang Y, Ren T, Zuo Z, Inglese J, Michael S, Simeonov A, Zheng W, Shinn P, Jadhav A, Boxer MB, Hall MD, Xia M, Guha R, Rohde JM. Kearney SE, et al. Among authors: cheff dm. ACS Cent Sci. 2018 Dec 26;4(12):1727-1741. doi: 10.1021/acscentsci.8b00747. Epub 2018 Dec 5. ACS Cent Sci. 2018. PMID: 30648156 Free PMC article.
19 results