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Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors.
Singh A, Venkannagari S, Oh KH, Zhang YQ, Rohde JM, Liu L, Nimmagadda S, Sudini K, Brimacombe KR, Gajghate S, Ma J, Wang A, Xu X, Shahane SA, Xia M, Woo J, Mensah GA, Wang Z, Ferrer M, Gabrielson E, Li Z, Rastinejad F, Shen M, Boxer MB, Biswal S. Singh A, et al. Among authors: boxer mb. ACS Chem Biol. 2016 Nov 18;11(11):3214-3225. doi: 10.1021/acschembio.6b00651. Epub 2016 Oct 17. ACS Chem Biol. 2016. PMID: 27552339 Free PMC article.
Synthesis and structure-activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein.
Hall MD, Brimacombe KR, Varonka MS, Pluchino KM, Monda JK, Li J, Walsh MJ, Boxer MB, Warren TH, Fales HM, Gottesman MM. Hall MD, et al. Among authors: boxer mb. J Med Chem. 2011 Aug 25;54(16):5878-89. doi: 10.1021/jm2006047. Epub 2011 Aug 1. J Med Chem. 2011. PMID: 21721528 Free PMC article.
2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M, Auld DS, Thomas CJ, Boxer MB. Walsh MJ, et al. Among authors: boxer mb. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6322-7. doi: 10.1016/j.bmcl.2011.08.114. Epub 2011 Sep 14. Bioorg Med Chem Lett. 2011. PMID: 21958545 Free PMC article.
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park HW, Cantley LC, Thomas CJ, Vander Heiden MG. Anastasiou D, et al. Among authors: boxer mb. Nat Chem Biol. 2012 Oct;8(10):839-47. doi: 10.1038/nchembio.1060. Nat Chem Biol. 2012. PMID: 22922757 Free PMC article.
Biochemical, cellular, and biophysical characterization of a potent inhibitor of mutant isocitrate dehydrogenase IDH1.
Davis MI, Gross S, Shen M, Straley KS, Pragani R, Lea WA, Popovici-Muller J, DeLaBarre B, Artin E, Thorne N, Auld DS, Li Z, Dang L, Boxer MB, Simeonov A. Davis MI, et al. Among authors: boxer mb. J Biol Chem. 2014 May 16;289(20):13717-25. doi: 10.1074/jbc.M113.511030. Epub 2014 Mar 25. J Biol Chem. 2014. PMID: 24668804 Free PMC article.
Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.
Brimacombe KR, Walsh MJ, Liu L, Vásquez-Valdivieso MG, Morgan HP, McNae I, Fothergill-Gilmore LA, Michels PA, Auld DS, Simeonov A, Walkinshaw MD, Shen M, Boxer MB. Brimacombe KR, et al. Among authors: boxer mb. ACS Med Chem Lett. 2013 Oct 30;5(1):12-7. doi: 10.1021/ml400259d. eCollection 2014 Jan 9. ACS Med Chem Lett. 2013. PMID: 24900769 Free PMC article.
Structure activity relationships of human galactokinase inhibitors.
Liu L, Tang M, Walsh MJ, Brimacombe KR, Pragani R, Tanega C, Rohde JM, Baker HL, Fernandez E, Blackman B, Bougie JM, Leister WH, Auld DS, Shen M, Lai K, Boxer MB. Liu L, et al. Among authors: boxer mb. Bioorg Med Chem Lett. 2015 Feb 1;25(3):721-7. doi: 10.1016/j.bmcl.2014.11.061. Epub 2014 Dec 13. Bioorg Med Chem Lett. 2015. PMID: 25553891
75 results