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Drug Discovery


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107 Pertega-Gomes, N et al. Monocarboxylate transporter 4 (MCT4) and CD147 overexpression is associated with poor prognosis in prostate cancer. BMC Cancer. 11: p. 312. 108 Pinheiro, C et al. Monocarboxylate transporter 1 is up-regulated in basal-like breast carcinoma. Histopathology. 56(7): p. 860-7. 109 Pinheiro, C et al. Increasing expression of monocarboxylate transporters 1 and 4 along progression to invasive cervical carcinoma. Int J Gynecol Pathol, 2008. 27(4): p. 568-74. 110 Pinheiro, C et al. Increased expression of monocarboxylate transporters 1, 2, and 4 in colorectal carcinomas. Virchows Arch, 2008. 452(2): p. 139-46. 111 Kennedy, KM and Dewhirst, MW. Tumor metabolism of lactate: the influence and therapeutic potential for MCT and CD147 regulation. Future Oncol. 6(1): p. 127-48. 112 David, CJ et al. HnRNP proteins controlled by c-Myc deregulate pyruvate kinase mRNA splicing in cancer. Nature. 463(7279): p. 364-8. 113 Bluemlein, K et al. No evidence for a shift in pyruvate kinase PKM1 to PKM2 expression during tumorigenesis. Oncotarget. 2(5): p. 393-400. 114 Dang, CV. PKM2 tyrosine phosphorylation and glutamine metabolism signal a different view of the Warburg effect. Sci Signal, 2009. 2(97): p. pe75. 115 Lv, L et al. Acetylation targets the M2 isoform of pyruvate kinase for degradation through chaperone-mediated autophagy and promotes tumor growth. Mol Cell. 42(6): p. 719-30. 116 Locasale, JW. Vander Heiden, MG and Cantley, LC. Rewiring of glycolysis in cancer cell metabolism. Cell Cycle. 9(21): p. 4253. 117Vander Heiden, MG et al. Identification of small molecule inhibitors of pyruvate kinase M2. Biochem Pharmacol. 79(8): p. 1118-24. 118 Boxer, MB et al. Identification of activators for the M2 isoform of human pyruvate kinase Version 3. 119 Frezza, C, Tennant, DA and Gottlieb, E. IDH1 mutations in gliomas: when an enzyme loses its grip. Cancer Cell. 17(1): p. 7-9. 120 Gross, S et al. Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations. J Exp Med. 207(2): p. 339-44. 121Ward, PS et al. The common feature of leukemia-associated IDH1 and IDH2 mutations is a neomorphic enzyme activity converting alpha-ketoglutarate to 2-hydroxyglutarate. Cancer Cell. 17(3): p. 225-34. 122 Dang, L et al. Cancer-associated IDH1 mutations produce 2-hydroxyglutarate. Nature, 2009. 462(7274): p. 739-44. 123 Zhao, S et al. Glioma-derived mutations in IDH1 dominantly inhibit IDH1 catalytic activity and induce HIF-1. Science, 2009. 324(5924): p. 261-5.


Drug Discovery World Fall 2011


124 Christensen, BC et al. DNA methylation, isocitrate dehydrogenase mutation, and survival in glioma. J Natl Cancer Inst. 103(2): p. 143-53. 125 Colombo, SL et al. Anaphase-promoting complex/cyclosome-Cdh1 coordinates glycolysis and glutaminolysis with transition to S phase in human T lymphocytes. Proc Natl Acad Sci U S A. 107(44): p. 18868-73. 126 Herrero-Mendez, A et al. The bioenergetic and antioxidant status of neurons is controlled by continuous degradation of a key glycolytic enzyme by APC/C-Cdh1. Nat Cell Biol, 2009. 11(6): p. 747-52. 127 Almeida, A, Bolanos, JP and Moncada, S. E3 ubiquitin ligase APC/C-Cdh1 accounts for the Warburg effect by linking glycolysis to cell proliferation. Proc Natl Acad Sci U S A. 107(2): p. 738-41. 128 Bolanos, JP, Almeida, A and Moncada, S. Glycolysis: a bioenergetic or a survival pathway? Trends Biochem Sci. 35(3): p. 145-9.


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