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Corrigendum: 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 MR, 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, Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. Pacold ME, et al. Among authors: brimacombe kr. Nat Chem Biol. 2016 Jul 19;12(8):656. doi: 10.1038/nchembio0816-656. Nat Chem Biol. 2016. PMID: 27434767 No abstract available.
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.
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: brimacombe kr. 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.
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: brimacombe kr. Nat Chem Biol. 2012 Oct;8(10):839-47. doi: 10.1038/nchembio.1060. Nat Chem Biol. 2012. PMID: 22922757 Free PMC article.
Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo.
Najm FJ, Madhavan M, Zaremba A, Shick E, Karl RT, Factor DC, Miller TE, Nevin ZS, Kantor C, Sargent A, Quick KL, Schlatzer DM, Tang H, Papoian R, Brimacombe KR, Shen M, Boxer MB, Jadhav A, Robinson AP, Podojil JR, Miller SD, Miller RH, Tesar PJ. Najm FJ, et al. Among authors: brimacombe kr. Nature. 2015 Jun 11;522(7555):216-20. doi: 10.1038/nature14335. Epub 2015 Apr 20. Nature. 2015. PMID: 25896324 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.
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
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.
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.
106 results