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Page 1
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: brimacombe kr. 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
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: brimacombe kr. 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.
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: brimacombe kr. 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.
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. 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.
Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Rohde JM, Karavadhi S, Pragani R, Liu L, Fang Y, Zhang W, McIver A, Zheng H, Liu Q, Davis MI, Urban DJ, Lee TD, Cheff DM, Hollingshead M, Henderson MJ, Martinez NJ, Brimacombe KR, Yasgar A, Zhao W, Klumpp-Thomas C, Michael S, Covey J, Moore WJ, Stott GM, Li Z, Simeonov A, Jadhav A, Frye S, Hall MD, Shen M, Wang X, Patnaik S, Boxer MB. Rohde JM, et al. Among authors: brimacombe kr. J Med Chem. 2021 Apr 22;64(8):4913-4946. doi: 10.1021/acs.jmedchem.1c00019. Epub 2021 Apr 6. J Med Chem. 2021. PMID: 33822623 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: brimacombe kr. Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x. Sci Rep. 2017. PMID: 28986582 Free PMC article.
A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.
Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Vander Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. Pacold ME, et al. Among authors: brimacombe kr. Nat Chem Biol. 2016 Jun;12(6):452-8. doi: 10.1038/nchembio.2070. Epub 2016 Apr 25. Nat Chem Biol. 2016. PMID: 27110680 Free PMC article.
Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.
Duveau DY, Yasgar A, Wang Y, Hu X, Kouznetsova J, Brimacombe KR, Jadhav A, Simeonov A, Thomas CJ, Maloney DJ. Duveau DY, et al. Among authors: brimacombe kr. Bioorg Med Chem Lett. 2014 Jan 15;24(2):630-5. doi: 10.1016/j.bmcl.2013.11.081. Epub 2013 Dec 4. Bioorg Med Chem Lett. 2014. PMID: 24360556 Free PMC article.
106 results