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Volumn 4, Issue 7, 2014, Pages 828-839

A high-throughput fluorimetric assay for 2-Hydroxyglutarate Identifies Zaprinast as a Glutaminase Inhibitor

Author keywords

[No Author keywords available]

Indexed keywords

2 HYDROXYGLUTARIC ACID; AGAR; CYCLIC GMP; ENZYME INHIBITOR; GLUTAMINASE; GLUTAMINASE INHIBITOR; HISTONE; ISOCITRATE DEHYDROGENASE 1; REACTIVE OXYGEN METABOLITE; SILDENAFIL; TADALAFIL; UNCLASSIFIED DRUG; ZAPRINAST; ALPHA-HYDROXYGLUTARATE; GLUTARIC ACID DERIVATIVE; ISOCITRATE DEHYDROGENASE; PURINE DERIVATIVE;

EID: 84904042360     PISSN: 21598274     EISSN: 21598290     Source Type: Journal    
DOI: 10.1158/2159-8290.CD-13-0572     Document Type: Article
Times cited : (70)

References (34)
  • 1
    • 75149148563 scopus 로고    scopus 로고
    • Q's next: The diverse functions of glutamine in metabolism, cell biology and cancer
    • DeBerardinis RJ, Cheng T. Q's next: the diverse functions of glutamine in metabolism, cell biology and cancer. Oncogene 2010; 29: 313-24.
    • (2010) Oncogene , vol.29 , pp. 313-324
    • DeBerardinis, R.J.1    Cheng, T.2
  • 2
    • 57749088701 scopus 로고    scopus 로고
    • Myc regulates a transcriptional program that stimulates mitochondrial glutaminolysis and leads to glutamine addiction
    • Wise DR, DeBerardinis RJ, Mancuso A, Sayed N, Zhang XY, Pfeiffer HK, et al. Myc regulates a transcriptional program that stimulates mitochondrial glutaminolysis and leads to glutamine addiction. Proc Natl Acad Sci U S A 2008; 105: 18782-7.
    • (2008) Proc Natl Acad Sci U S A , vol.105 , pp. 18782-18787
    • Wise, D.R.1    DeBerardinis, R.J.2    Mancuso, A.3    Sayed, N.4    Zhang, X.Y.5    Pfeiffer, H.K.6
  • 3
    • 64749116346 scopus 로고    scopus 로고
    • c-Myc suppression of miR-23a/b enhances mitochondrial glutaminase expression and glutamine metabolism
    • Gao P, Tchernyshyov I, Chang TC, Lee YS, Kita K, Ochi T, et al. c-Myc suppression of miR-23a/b enhances mitochondrial glutaminase expression and glutamine metabolism. Nature 2009; 458: 762-5.
    • (2009) Nature , vol.458 , pp. 762-765
    • Gao, P.1    Tchernyshyov, I.2    Chang, T.C.3    Lee, Y.S.4    Kita, K.5    Ochi, T.6
  • 4
    • 84875894714 scopus 로고    scopus 로고
    • Glutamine supports pancreatic cancer growth through a KRASregulated metabolic pathway
    • Son J, Lyssiotis CA, Ying H, Wang X, Hua S, Ligorio M, et al. Glutamine supports pancreatic cancer growth through a KRASregulated metabolic pathway. Nature 2013; 496: 101-5.
    • (2013) Nature , vol.496 , pp. 101-105
    • Son, J.1    Lyssiotis, C.A.2    Ying, H.3    Wang, X.4    Hua, S.5    Ligorio, M.6
  • 9
    • 79958226901 scopus 로고    scopus 로고
    • IDH1 and IDH2 mutations are frequent events in central chondrosarcoma and central and periosteal chondromas but not in other mesenchymal tumours
    • Amary MF, Bacsi K, Maggiani F, Damato S, Halai D, Berisha F, et al. IDH1 and IDH2 mutations are frequent events in central chondrosarcoma and central and periosteal chondromas but not in other mesenchymal tumours. J Pathol 2011; 224: 334-43.
    • (2011) J Pathol , vol.224 , pp. 334-343
    • Amary, M.F.1    Bacsi, K.2    Maggiani, F.3    Damato, S.4    Halai, D.5    Berisha, F.6
  • 10
    • 84856298658 scopus 로고    scopus 로고
    • Frequent mutation of isocitrate dehydrogenase (IDH)1 and IDH2 in cholangiocarcinoma identified through broad-based tumor genotyping
    • Borger DR, Tanabe KK, Fan KC, Lopez HU, Fantin VR, Straley KS, et al. Frequent mutation of isocitrate dehydrogenase (IDH)1 and IDH2 in cholangiocarcinoma identified through broad-based tumor genotyping. Oncologist 2012; 17: 72-9.
    • (2012) Oncologist , vol.17 , pp. 72-79
    • Borger, D.R.1    Tanabe, K.K.2    Fan, K.C.3    Lopez, H.U.4    Fantin, V.R.5    Straley, K.S.6
  • 11
    • 84876889621 scopus 로고    scopus 로고
    • What a difference a hydroxyl makes: Mutant IDH, (R)-2-hydroxyglutarate, and cancer
    • Losman JA, Kaelin WG Jr. What a difference a hydroxyl makes: mutant IDH, (R)-2-hydroxyglutarate, and cancer. Genes Dev 2013; 27: 836-52.
    • (2013) Genes Dev , vol.27 , pp. 836-852
    • Losman, J.A.1    Kaelin Jr., W.G.2
  • 12
    • 78651463452 scopus 로고    scopus 로고
    • Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of alpha-ketoglutaratedependent dioxygenases
    • Xu W, Yang H, Liu Y, Yang Y, Wang P, Kim SH, et al. Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of alpha-ketoglutaratedependent dioxygenases. Cancer Cell 2011; 19: 17-30.
    • (2011) Cancer Cell , vol.19 , pp. 17-30
    • Xu, W.1    Yang, H.2    Liu, Y.3    Yang, Y.4    Wang, P.5    Kim, S.H.6
  • 13
    • 78650019179 scopus 로고    scopus 로고
    • Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation
    • Figueroa ME, Abdel-Wahab O, Lu C, Ward PS, Patel J, Shih A, et al. Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation. Cancer Cell 2010; 18: 553-67.
    • (2010) Cancer Cell , vol.18 , pp. 553-567
    • Figueroa, M.E.1    Abdel-Wahab, O.2    Lu, C.3    Ward, P.S.4    Patel, J.5    Shih, A.6
  • 14
    • 84862776918 scopus 로고    scopus 로고
    • Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation
    • Koivunen P, Lee S, Duncan CG, Lopez G, Lu G, Ramkissoon S, et al. Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation. Nature 2012; 483: 484-8.
    • (2012) Nature , vol.483 , pp. 484-488
    • Koivunen, P.1    Lee, S.2    Duncan, C.G.3    Lopez, G.4    Lu, G.5    Ramkissoon, S.6
  • 15
    • 84858796262 scopus 로고    scopus 로고
    • IDH mutation impairs histone demethylation and results in a block to cell differentiation
    • Lu C, Ward PS, Kapoor GS, Rohle D, Turcan S, Abdel-Wahab O, et al. IDH mutation impairs histone demethylation and results in a block to cell differentiation. Nature 2012; 483: 474-8.
    • (2012) Nature , vol.483 , pp. 474-478
    • Lu, C.1    Ward, P.S.2    Kapoor, G.S.3    Rohle, D.4    Turcan, S.5    Abdel-Wahab, O.6
  • 16
    • 84875496294 scopus 로고    scopus 로고
    • (R)-2-hydroxyglutarate is sufficient to promote leukemogenesis and its effects are reversible
    • Losman JA, Looper RE, Koivunen P, Lee S, Schneider RK, McMahon C, et al. (R)-2-hydroxyglutarate is sufficient to promote leukemogenesis and its effects are reversible. Science 2013; 339: 1621-5.
    • (2013) Science , vol.339 , pp. 1621-1625
    • Losman, J.A.1    Looper, R.E.2    Koivunen, P.3    Lee, S.4    Schneider, R.K.5    McMahon, C.6
  • 17
    • 84865520089 scopus 로고    scopus 로고
    • IDH1(R132H) mutation increases murine haematopoietic progenitors and alters epigenetics
    • Sasaki M, Knobbe CB, Munger JC, Lind EF, Brenner D, Brustle A, et al. IDH1(R132H) mutation increases murine haematopoietic progenitors and alters epigenetics. Nature 2012; 488: 656-9.
    • (2012) Nature , vol.488 , pp. 656-659
    • Sasaki, M.1    Knobbe, C.B.2    Munger, J.C.3    Lind, E.F.4    Brenner, D.5    Brustle, A.6
  • 18
    • 84877632013 scopus 로고    scopus 로고
    • An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells
    • Rohle D, Popovici-Muller J, Palaskas N, Turcan S, Grommes C, Campos C, et al. An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science 2013; 340: 626-30.
    • (2013) Science , vol.340 , pp. 626-630
    • Rohle, D.1    Popovici-Muller, J.2    Palaskas, N.3    Turcan, S.4    Grommes, C.5    Campos, C.6
  • 19
    • 84877620952 scopus 로고    scopus 로고
    • Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation
    • Wang F, Travins J, DeLaBarre B, Penard-Lacronique V, Schalm S, Hansen E, et al. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science 2013; 340: 622-6.
    • (2013) Science , vol.340 , pp. 622-626
    • Wang, F.1    Travins, J.2    DeLaBarre, B.3    Penard-Lacronique, V.4    Schalm, S.5    Hansen, E.6
  • 20
    • 0029671184 scopus 로고    scopus 로고
    • A novel alpha-ketoglutarate reductase activity of the serA-encoded 3-phosphoglycerate dehydrogenase of Escherichia coli K-12 and its possible implications for human 2-hydroxyglutaric aciduria
    • Zhao G, Winkler ME. A novel alpha-ketoglutarate reductase activity of the serA-encoded 3-phosphoglycerate dehydrogenase of Escherichia coli K-12 and its possible implications for human 2-hydroxyglutaric aciduria. J Bacteriol 1996; 178: 232-9.
    • (1996) J Bacteriol , vol.178 , pp. 232-239
    • Zhao, G.1    Winkler, M.E.2
  • 21
    • 63149156356 scopus 로고    scopus 로고
    • An enzymatic fluorimetric assay for glucose-6-phosphate: Application in an in vitro Warburg-like effect
    • Zhu A, Romero R, Petty HR. An enzymatic fluorimetric assay for glucose-6-phosphate: application in an in vitro Warburg-like effect. Anal Biochem 2009; 388: 97-101.
    • (2009) Anal Biochem , vol.388 , pp. 97-101
    • Zhu, A.1    Romero, R.2    Petty, H.R.3
  • 23
    • 0041422429 scopus 로고    scopus 로고
    • A constitutively activated mutant of human soluble guanylyl cyclase (sGC): Implication for the mechanism of sGC activation
    • Martin E, Sharina I, Kots A, Murad F. A constitutively activated mutant of human soluble guanylyl cyclase (sGC): implication for the mechanism of sGC activation. Proc Natl Acad Sci U S A 2003; 100: 9208-13.
    • (2003) Proc Natl Acad Sci U S A , vol.100 , pp. 9208-9213
    • Martin, E.1    Sharina, I.2    Kots, A.3    Murad, F.4
  • 24
    • 37449034854 scopus 로고    scopus 로고
    • Beyond aerobic glycolysis: Transformed cells can engage in glutamine metabolism that exceeds the requirement for protein and nucleotide synthesis
    • DeBerardinis RJ, Mancuso A, Daikhin E, Nissim I, Yudkoff M, Wehrli S, et al. Beyond aerobic glycolysis: transformed cells can engage in glutamine metabolism that exceeds the requirement for protein and nucleotide synthesis. Proc Natl Acad Sci U S A 2007; 104: 19345-50.
    • (2007) Proc Natl Acad Sci U S A , vol.104 , pp. 19345-19350
    • DeBerardinis, R.J.1    Mancuso, A.2    Daikhin, E.3    Nissim, I.4    Yudkoff, M.5    Wehrli, S.6
  • 27
    • 78549283855 scopus 로고    scopus 로고
    • Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1
    • Seltzer MJ, Bennett BD, Joshi AD, Gao P, Thomas AG, Ferraris DV, et al. Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1. Cancer Res 2010; 70: 8981-7.
    • (2010) Cancer Res , vol.70 , pp. 8981-8987
    • Seltzer, M.J.1    Bennett, B.D.2    Joshi, A.D.3    Gao, P.4    Thomas, A.G.5    Ferraris, D.V.6
  • 29
    • 84856374900 scopus 로고    scopus 로고
    • Mitochondrial localization and structure-based phosphate activation mechanism of Glutaminase C with implications for cancer metabolism
    • Cassago A, Ferreira AP, Ferreira IM, Fornezari C, Gomes ER, Greene KS, et al. Mitochondrial localization and structure-based phosphate activation mechanism of Glutaminase C with implications for cancer metabolism. Proc Natl Acad Sci U S A 2012; 109: 1092-7.
    • (2012) Proc Natl Acad Sci U S A , vol.109 , pp. 1092-1097
    • Cassago, A.1    Ferreira, A.P.2    Ferreira, I.M.3    Fornezari, C.4    Gomes, E.R.5    Greene, K.S.6
  • 31
    • 84870982915 scopus 로고    scopus 로고
    • Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors
    • Shukla K, Ferraris DV, Thomas AG, Stathis M, Duvall B, Delahanty G, et al. Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors. J Med Chem 2012; 55: 10551-63.
    • (2012) J Med Chem , vol.55 , pp. 10551-10563
    • Shukla, K.1    Ferraris, D.V.2    Thomas, A.G.3    Stathis, M.4    Duvall, B.5    Delahanty, G.6
  • 32
    • 0344146594 scopus 로고    scopus 로고
    • The relationship between effector binding and inhibition of activity in D-3-phosphoglycerate dehydrogenase
    • Grant GA, Xu XL, Hu Z. The relationship between effector binding and inhibition of activity in D-3-phosphoglycerate dehydrogenase. Protein Sci 1999; 8: 2501-5.
    • (1999) Protein Sci , vol.8 , pp. 2501-2505
    • Grant, G.A.1    Xu, X.L.2    Hu, Z.3
  • 33
    • 73349124764 scopus 로고    scopus 로고
    • Vascular endothelial growth factor receptor-1 is synthetic lethal to aberrant {beta}-catenin activation in colon cancer
    • Naik S, Dothager RS, Marasa J, Lewis CL, Piwnica-Worms D. Vascular endothelial growth factor receptor-1 is synthetic lethal to aberrant {beta}-catenin activation in colon cancer. Clin Cancer Res 2009; 15: 7529-37.
    • (2009) Clin Cancer Res , vol.15 , pp. 7529-7537
    • Naik, S.1    Dothager, R.S.2    Marasa, J.3    Lewis, C.L.4    Piwnica-Worms, D.5
  • 34
    • 0141762598 scopus 로고    scopus 로고
    • Bacterial expression, purification, and characterization of rat kidney-type mitochondrial glutaminase
    • Kenny J, Bao Y, Hamm B, Taylor L, Toth A, Wagers B, et al. Bacterial expression, purification, and characterization of rat kidney-type mitochondrial glutaminase. Protein Expr Purif 2003; 31: 140-8.
    • (2003) Protein Expr Purif , vol.31 , pp. 140-148
    • Kenny, J.1    Bao, Y.2    Hamm, B.3    Taylor, L.4    Toth, A.5    Wagers, B.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.