메뉴 건너뛰기




Volumn 6, Issue 9, 2011, Pages

Structure-based development of small molecule PFKFB3 inhibitors: A framework for potential cancer therapeutic agents targeting the Warburg effect

Author keywords

[No Author keywords available]

Indexed keywords

5,6,7,8 TETRAHYDROXY 2 (4 HYDROXYPHENYL)CHROMEN 4 ONE; 6 PHOSPHOFRUCTO 2 KINASE FRUCTOSE 2,6 BISPHOSPHATASE INHIBITOR; 7,8 DIHYDROXY 3 (4 HYDROXYPHENYL)CHROMEN 4 ONE; ANTINEOPLASTIC AGENT; BISPHOSPHONIC ACID DERIVATIVE; ETHYL 7 HYDROXY 2 OXOCHROMENE 3 CARBOXYLIC ACID; FRUCTOSE 2,6 BISPHOSPHONATE; UNCLASSIFIED DRUG; YN 1; YZ 9; 6 PHOSPHOFRUCTO 2 KINASE; BENZOPYRAN DERIVATIVE; ENZYME INHIBITOR; FRUCTOSE 6 PHOSPHATE; FRUCTOSE PHOSPHATE; FRUCTOSE-6-PHOSPHATE; PFKFB3 PROTEIN, HUMAN;

EID: 80052988662     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0024179     Document Type: Article
Times cited : (59)

References (40)
  • 1
    • 61849135453 scopus 로고    scopus 로고
    • Tumor suppressors and cell metabolism: a recipe for cancer growth
    • Jones RG, Thompson CB, (2009) Tumor suppressors and cell metabolism: a recipe for cancer growth. Genes Dev 23: 537-548.
    • (2009) Genes Dev , vol.23 , pp. 537-548
    • Jones, R.G.1    Thompson, C.B.2
  • 2
    • 12444279265 scopus 로고
    • On the origin of cancer cells
    • Warburg O, (1956) On the origin of cancer cells. Science 123: 309-314.
    • (1956) Science , vol.123 , pp. 309-314
    • Warburg, O.1
  • 3
    • 66249108601 scopus 로고    scopus 로고
    • Understanding the Warburg effect: the metabolic requirements of cell proliferation
    • Vander Heiden MG, Cantley LC, Thompson CB, (2009) Understanding the Warburg effect: the metabolic requirements of cell proliferation. Science 324: 1029-1033.
    • (2009) Science , vol.324 , pp. 1029-1033
    • Vander Heiden, M.G.1    Cantley, L.C.2    Thompson, C.B.3
  • 4
    • 33744969828 scopus 로고    scopus 로고
    • Energy deregulation: licensing tumors to grow
    • Garber K, (2006) Energy deregulation: licensing tumors to grow. Science 312: 1158-1159.
    • (2006) Science , vol.312 , pp. 1158-1159
    • Garber, K.1
  • 5
    • 52649107626 scopus 로고    scopus 로고
    • Cancer cell metabolism: Warburg and beyond
    • Hsu PP, Sabatini DM, (2008) Cancer cell metabolism: Warburg and beyond. Cell 134: 703-707.
    • (2008) Cell , vol.134 , pp. 703-707
    • Hsu, P.P.1    Sabatini, D.M.2
  • 6
    • 0031736203 scopus 로고    scopus 로고
    • Somatic mutations of the mitochondrial genome in human colorectal tumours
    • Polyak K, Li Y, Zhu H, Lengauer C, Willson JK, et al. (1998) Somatic mutations of the mitochondrial genome in human colorectal tumours. Nat Genet 20: 291-293.
    • (1998) Nat Genet , vol.20 , pp. 291-293
    • Polyak, K.1    Li, Y.2    Zhu, H.3    Lengauer, C.4    Willson, J.K.5
  • 7
    • 28544446058 scopus 로고    scopus 로고
    • Mitochondrial tumour suppressors: a genetic and biochemical update
    • Gottlieb E, Tomlinson IP, (2005) Mitochondrial tumour suppressors: a genetic and biochemical update. Nat Rev Cancer 5: 857-866.
    • (2005) Nat Rev Cancer , vol.5 , pp. 857-866
    • Gottlieb, E.1    Tomlinson, I.P.2
  • 8
    • 33745303045 scopus 로고    scopus 로고
    • Hypoxia signalling in cancer and approaches to enforce tumour regression
    • Pouyssegur J, Dayan F, Mazure NM, (2006) Hypoxia signalling in cancer and approaches to enforce tumour regression. Nature 441: 437-443.
    • (2006) Nature , vol.441 , pp. 437-443
    • Pouyssegur, J.1    Dayan, F.2    Mazure, N.M.3
  • 9
    • 37449024702 scopus 로고    scopus 로고
    • The biology of cancer: metabolic reprogramming fuels cell growth and proliferation
    • DeBerardinis RJ, Lum JJ, Hatzivassiliou G, Thompson CB, (2008) The biology of cancer: metabolic reprogramming fuels cell growth and proliferation. Cell Metab 7: 11-20.
    • (2008) Cell Metab , vol.7 , pp. 11-20
    • DeBerardinis, R.J.1    Lum, J.J.2    Hatzivassiliou, G.3    Thompson, C.B.4
  • 10
    • 33746879141 scopus 로고    scopus 로고
    • Glycolysis inhibition for anticancer treatment
    • Pelicano H, Martin DS, Xu RH, Huang P, (2006) Glycolysis inhibition for anticancer treatment. Oncogene 25: 4633-4646.
    • (2006) Oncogene , vol.25 , pp. 4633-4646
    • Pelicano, H.1    Martin, D.S.2    Xu, R.H.3    Huang, P.4
  • 11
    • 12544256565 scopus 로고    scopus 로고
    • Inhibition of glycolysis in cancer cells: a novel strategy to overcome drug resistance associated with mitochondrial respiratory defect and hypoxia
    • Xu RH, Pelicano H, Zhou Y, Carew JS, Feng L, et al. (2005) Inhibition of glycolysis in cancer cells: a novel strategy to overcome drug resistance associated with mitochondrial respiratory defect and hypoxia. Cancer Res 65: 613-621.
    • (2005) Cancer Res , vol.65 , pp. 613-621
    • Xu, R.H.1    Pelicano, H.2    Zhou, Y.3    Carew, J.S.4    Feng, L.5
  • 12
    • 77949967131 scopus 로고    scopus 로고
    • Targeting metabolic transformation for cancer therapy
    • Tennant DA, Duran RV, Gottlieb E, (2010) Targeting metabolic transformation for cancer therapy. Nat Rev Cancer 10: 267-277.
    • (2010) Nat Rev Cancer , vol.10 , pp. 267-277
    • Tennant, D.A.1    Duran, R.V.2    Gottlieb, E.3
  • 13
    • 0029043852 scopus 로고
    • 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase: a metabolic signaling enzyme
    • Pilkis SJ, Claus TH, Kurland IJ, Lange AJ, (1995) 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase: a metabolic signaling enzyme. Annu Rev Biochem 64: 799-835.
    • (1995) Annu Rev Biochem , vol.64 , pp. 799-835
    • Pilkis, S.J.1    Claus, T.H.2    Kurland, I.J.3    Lange, A.J.4
  • 14
    • 0035744596 scopus 로고    scopus 로고
    • 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase: suiting structure to need, in a family of tissue-specific enzymes
    • El-Maghrabi MR, Noto F, Wu N, Manes N, (2001) 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase: suiting structure to need, in a family of tissue-specific enzymes. Curr Opin Clin Nutr Metab Care 4: 411-418.
    • (2001) Curr Opin Clin Nutr Metab Care , vol.4 , pp. 411-418
    • El-Maghrabi, M.R.1    Noto, F.2    Wu, N.3    Manes, N.4
  • 15
    • 0342919888 scopus 로고
    • Control of liver 6-phosphofructokinase by fructose 2,6-bisphosphate and other effectors
    • Van Schaftingen E, Jett MF, Hue L, Hers HG, (1981) Control of liver 6-phosphofructokinase by fructose 2,6-bisphosphate and other effectors. Proc Natl Acad Sci U S A 78: 3483-3486.
    • (1981) Proc Natl Acad Sci U S A , vol.78 , pp. 3483-3486
    • van Schaftingen, E.1    Jett, M.F.2    Hue, L.3    Hers, H.G.4
  • 16
    • 0028804088 scopus 로고
    • Fructose 2,6-bisphosphate metabolism in Ehrlich ascites tumour cells
    • Nissler K, Petermann H, Wenz I, Brox D, (1995) Fructose 2,6-bisphosphate metabolism in Ehrlich ascites tumour cells. J Cancer Res Clin Oncol 121: 739-745.
    • (1995) J Cancer Res Clin Oncol , vol.121 , pp. 739-745
    • Nissler, K.1    Petermann, H.2    Wenz, I.3    Brox, D.4
  • 17
    • 0027479937 scopus 로고
    • Fructose 2,6-bisphosphate and the control of glycolysis by growth factors, tumor promoters and oncogenes
    • Hue L, Rousseau GG, (1993) Fructose 2,6-bisphosphate and the control of glycolysis by growth factors, tumor promoters and oncogenes. Adv Enzyme Regul 33: 97-110.
    • (1993) Adv Enzyme Regul , vol.33 , pp. 97-110
    • Hue, L.1    Rousseau, G.G.2
  • 18
    • 33747487110 scopus 로고    scopus 로고
    • Ras transformation requires metabolic control by 6-phosphofructo-2-kinase
    • Telang S, Yalcin A, Clem AL, Bucala R, Lane AN, et al. (2006) Ras transformation requires metabolic control by 6-phosphofructo-2-kinase. Oncogene 25: 7225-7234.
    • (2006) Oncogene , vol.25 , pp. 7225-7234
    • Telang, S.1    Yalcin, A.2    Clem, A.L.3    Bucala, R.4    Lane, A.N.5
  • 19
    • 4344618856 scopus 로고    scopus 로고
    • 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase: head-to-head with a bifunctional enzyme that controls glycolysis
    • Rider MH, Bertrand L, Vertommen D, Michels PA, Rousseau GG, et al. (2004) 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase: head-to-head with a bifunctional enzyme that controls glycolysis. Biochem J 381: 561-579.
    • (2004) Biochem J , vol.381 , pp. 561-579
    • Rider, M.H.1    Bertrand, L.2    Vertommen, D.3    Michels, P.A.4    Rousseau, G.G.5
  • 20
    • 0242710750 scopus 로고    scopus 로고
    • Hypoxic regulation of the 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase gene family (PFKFB-1-4) expression in vivo
    • Minchenko O, Opentanova I, Caro J, (2003) Hypoxic regulation of the 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase gene family (PFKFB-1-4) expression in vivo. FEBS Lett 554: 264-270.
    • (2003) FEBS Lett , vol.554 , pp. 264-270
    • Minchenko, O.1    Opentanova, I.2    Caro, J.3
  • 21
    • 0037108709 scopus 로고    scopus 로고
    • High expression of inducible 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (iPFK-2; PFKFB3) in human cancers
    • Atsumi T, Chesney J, Metz C, Leng L, Donnelly S, et al. (2002) High expression of inducible 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (iPFK-2; PFKFB3) in human cancers. Cancer Res 62: 5881-5887.
    • (2002) Cancer Res , vol.62 , pp. 5881-5887
    • Atsumi, T.1    Chesney, J.2    Metz, C.3    Leng, L.4    Donnelly, S.5
  • 22
    • 33746037631 scopus 로고    scopus 로고
    • PFKFB3 gene silencing decreases glycolysis, induces cell-cycle delay and inhibits anchorage-independent growth in HeLa cells
    • Calvo MN, Bartrons R, Castano E, Perales JC, Navarro-Sabate A, et al. (2006) PFKFB3 gene silencing decreases glycolysis, induces cell-cycle delay and inhibits anchorage-independent growth in HeLa cells. FEBS Lett 580: 3308-3314.
    • (2006) FEBS Lett , vol.580 , pp. 3308-3314
    • Calvo, M.N.1    Bartrons, R.2    Castano, E.3    Perales, J.C.4    Navarro-Sabate, A.5
  • 23
    • 0037155247 scopus 로고    scopus 로고
    • Hypoxia-inducible factor-1-mediated expression of the 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase-3 (PFKFB3) gene. Its possible role in the Warburg effect
    • Minchenko A, Leshchinsky I, Opentanova I, Sang N, Srinivas V, et al. (2002) Hypoxia-inducible factor-1-mediated expression of the 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase-3 (PFKFB3) gene. Its possible role in the Warburg effect. J Biol Chem 277: 6183-6187.
    • (2002) J Biol Chem , vol.277 , pp. 6183-6187
    • Minchenko, A.1    Leshchinsky, I.2    Opentanova, I.3    Sang, N.4    Srinivas, V.5
  • 24
    • 38349183620 scopus 로고    scopus 로고
    • Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth
    • Clem B, Telang S, Clem A, Yalcin A, Meier J, et al. (2008) Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth. Mol Cancer Ther 7: 110-120.
    • (2008) Mol Cancer Ther , vol.7 , pp. 110-120
    • Clem, B.1    Telang, S.2    Clem, A.3    Yalcin, A.4    Meier, J.5
  • 25
    • 33646352483 scopus 로고    scopus 로고
    • Crystal structure of the hypoxia-inducible form of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFKFB3): a possible new target for cancer therapy
    • Kim SG, Manes NP, El-Maghrabi MR, Lee YH, (2006) Crystal structure of the hypoxia-inducible form of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFKFB3): a possible new target for cancer therapy. J Biol Chem 281: 2939-2944.
    • (2006) J Biol Chem , vol.281 , pp. 2939-2944
    • Kim, S.G.1    Manes, N.P.2    El-Maghrabi, M.R.3    Lee, Y.H.4
  • 26
    • 0034645763 scopus 로고    scopus 로고
    • Knowledge-based scoring function to predict protein-ligand interactions
    • Gohlke H, Hendlich M, Klebe G, (2000) Knowledge-based scoring function to predict protein-ligand interactions. J Mol Biol 295: 337-356.
    • (2000) J Mol Biol , vol.295 , pp. 337-356
    • Gohlke, H.1    Hendlich, M.2    Klebe, G.3
  • 27
    • 0031736004 scopus 로고    scopus 로고
    • Biochemical determinants of apoptosis and necrosis
    • McConkey DJ, (1998) Biochemical determinants of apoptosis and necrosis. Toxicol Lett 99: 157-168.
    • (1998) Toxicol Lett , vol.99 , pp. 157-168
    • McConkey, D.J.1
  • 29
    • 34249335028 scopus 로고    scopus 로고
    • A direct substrate-substrate interaction found in the kinase domain of the bifunctional enzyme, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase
    • Kim SG, Cavalier M, El-Maghrabi MR, Lee YH, (2007) A direct substrate-substrate interaction found in the kinase domain of the bifunctional enzyme, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase. J Mol Biol 370: 14-26.
    • (2007) J Mol Biol , vol.370 , pp. 14-26
    • Kim, S.G.1    Cavalier, M.2    El-Maghrabi, M.R.3    Lee, Y.H.4
  • 30
    • 14644431061 scopus 로고    scopus 로고
    • Managing molecular diversity
    • Perez JJ, (2005) Managing molecular diversity. Chem Soc Rev 34: 143-152.
    • (2005) Chem Soc Rev , vol.34 , pp. 143-152
    • Perez, J.J.1
  • 31
    • 0037072311 scopus 로고    scopus 로고
    • Cation-pi interactions in ligand recognition by serotonergic (5-HT3A) and nicotinic acetylcholine receptors: the anomalous binding properties of nicotine
    • Beene DL, Brandt GS, Zhong W, Zacharias NM, Lester HA, et al. (2002) Cation-pi interactions in ligand recognition by serotonergic (5-HT3A) and nicotinic acetylcholine receptors: the anomalous binding properties of nicotine. Biochemistry 41: 10262-10269.
    • (2002) Biochemistry , vol.41 , pp. 10262-10269
    • Beene, D.L.1    Brandt, G.S.2    Zhong, W.3    Zacharias, N.M.4    Lester, H.A.5
  • 32
    • 0026730489 scopus 로고
    • Structure-based strategies for drug design and discovery
    • Kuntz ID, (1992) Structure-based strategies for drug design and discovery. Science 257: 1078-1082.
    • (1992) Science , vol.257 , pp. 1078-1082
    • Kuntz, I.D.1
  • 33
    • 0036051992 scopus 로고    scopus 로고
    • High-throughput crystallography for lead discovery in drug design
    • Blundell TL, Jhoti H, Abell C, (2002) High-throughput crystallography for lead discovery in drug design. Nat Rev Drug Discov 1: 45-54.
    • (2002) Nat Rev Drug Discov , vol.1 , pp. 45-54
    • Blundell, T.L.1    Jhoti, H.2    Abell, C.3
  • 34
    • 0034306450 scopus 로고    scopus 로고
    • Specificity and mechanism of action of some commonly used protein kinase inhibitors
    • Davies SP, Reddy H, Caivano M, Cohen P, (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 351: 95-105.
    • (2000) Biochem J , vol.351 , pp. 95-105
    • Davies, S.P.1    Reddy, H.2    Caivano, M.3    Cohen, P.4
  • 35
    • 0023885305 scopus 로고
    • The protein kinase family: conserved features and deduced phylogeny of the catalytic domains
    • Hanks SK, Quinn AM, Hunter T, (1988) The protein kinase family: conserved features and deduced phylogeny of the catalytic domains. Science 241: 42-52.
    • (1988) Science , vol.241 , pp. 42-52
    • Hanks, S.K.1    Quinn, A.M.2    Hunter, T.3
  • 36
    • 0020438908 scopus 로고
    • A kinetic study of pyrophosphate: fructose-6-phosphate phosphotransferase from potato tubers. Application to a microassay of fructose 2,6-bisphosphate
    • Van Schaftingen E, Lederer B, Bartrons R, Hers HG, (1982) A kinetic study of pyrophosphate: fructose-6-phosphate phosphotransferase from potato tubers. Application to a microassay of fructose 2,6-bisphosphate. Eur J Biochem 129: 191-195.
    • (1982) Eur J Biochem , vol.129 , pp. 191-195
    • van Schaftingen, E.1    Lederer, B.2    Bartrons, R.3    Hers, H.G.4
  • 37
    • 0018735516 scopus 로고
    • Statistical analysis of enzyme kinetic data
    • Cleland WW, (1979) Statistical analysis of enzyme kinetic data. Methods Enzymol 63: 103-138.
    • (1979) Methods Enzymol , vol.63 , pp. 103-138
    • Cleland, W.W.1
  • 38
    • 0031985647 scopus 로고    scopus 로고
    • Annexin V-affinity assay: a review on an apoptosis detection system based on phosphatidylserine exposure
    • van Engeland M, Nieland LJ, Ramaekers FC, Schutte B, Reutelingsperger CP, (1998) Annexin V-affinity assay: a review on an apoptosis detection system based on phosphatidylserine exposure. Cytometry 31: 1-9.
    • (1998) Cytometry , vol.31 , pp. 1-9
    • van Engeland, M.1    Nieland, L.J.2    Ramaekers, F.C.3    Schutte, B.4    Reutelingsperger, C.P.5
  • 40
    • 0028103275 scopus 로고
    • The CCP4 suite: programs for protein crystallography
    • Collaborative Computational Project
    • Collaborative Computational Project (1994) The CCP4 suite: programs for protein crystallography. Acta Crystallogr D Biol Crystallogr 50: 760-763.
    • (1994) Acta Crystallogr D Biol Crystallogr , vol.50 , pp. 760-763


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.