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Volumn 7, Issue 5, 2017, Pages 478-493

AG-221, a first-in-class therapy targeting acute myeloid leukemia harboring oncogenic IDH2 mutations

(41)  Yen, Katharine a   Travins, Jeremy a   Wang, Fang a   David, Muriel D b,c,d   Artin, Erin a   Straley, Kimberly a,i   Padyana, Anil a   Gross, Stefan a   Delabarre, Byron a,j   Tobin, Erica a   Chen, Yue a   Nagaraja, Raj a   Choe, Sung a   Jin, Lei a   Konteatis, Zenon a   Cianchetta, Giovanni a   Saunders, Jeffrey O a,k   Salituro, Francesco G a,l   Quivoron, Cyril b,c,d   Opolon, Paule c   more..


Author keywords

[No Author keywords available]

Indexed keywords

2 HYDROXYGLUTARIC ACID; CD11 ANTIGEN; CD11B ANTIGEN; CD14 ANTIGEN; CD15 ANTIGEN; CD24 ANTIGEN; CYTARABINE; ENASIDENIB; ERYTHROPOIETIN; HEMOGLOBIN A; ISOCITRATE DEHYDROGENASE 2; KRUPPEL LIKE FACTOR; TRANSCRIPTION FACTOR RUNX1; TRANSCRIPTION FACTOR RUNX3; AG-221; AMINOPYRIDINE DERIVATIVE; ANTINEOPLASTIC AGENT; ISOCITRATE DEHYDROGENASE; ISOCITRATE DEHYDROGENASE 2, HUMAN; TRIAZINE DERIVATIVE;

EID: 85018387546     PISSN: 21598274     EISSN: 21598290     Source Type: Journal    
DOI: 10.1158/2159-8290.CD-16-1034     Document Type: Article
Times cited : (364)

References (50)
  • 1
    • 84955326448 scopus 로고    scopus 로고
    • The emerging hallmarks of cancer metabolism
    • Pavlova NN, Thompson CB. The emerging hallmarks of cancer metabolism. Cell Metab 2016;23:27–47.
    • (2016) Cell Metab , vol.23 , pp. 27-47
    • Pavlova, N.N.1    Thompson, C.B.2
  • 2
    • 79952284127 scopus 로고    scopus 로고
    • Hallmarks of cancer: The next generation
    • Hanahan D, Weinberg RA. Hallmarks of cancer: The next generation. Cell 2011;144:646–74.
    • (2011) Cell , vol.144 , pp. 646-674
    • Hanahan, D.1    Weinberg, R.A.2
  • 6
    • 77952426827 scopus 로고    scopus 로고
    • Mutations of IDH1 and IDH2 genes in early and accelerated phases of myelodysplastic syndromes and MDS/myeloproliferative neoplasms
    • Kosmider O, Gelsi-Boyer V, Slama L, Dreyfus F, Beyne-Rauzy O, Quesnel B, et al. Mutations of IDH1 and IDH2 genes in early and accelerated phases of myelodysplastic syndromes and MDS/myeloproliferative neoplasms. Leukemia 2010;24:1094–6.
    • (2010) Leukemia , vol.24 , pp. 1094-1096
    • Kosmider, O.1    Gelsi-Boyer, V.2    Slama, L.3    Dreyfus, F.4    Beyne-Rauzy, O.5    Quesnel, B.6
  • 7
    • 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
  • 8
    • 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
  • 9
    • 77149134353 scopus 로고    scopus 로고
    • Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations
    • Gross S, Cairns RA, Minden MD, Driggers EM, Bittinger MA, Jang HG, et al. Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations. J Exp Med 2010;207:339–44.
    • (2010) J Exp Med , vol.207 , pp. 339-344
    • Gross, S.1    Cairns, R.A.2    Minden, M.D.3    Driggers, E.M.4    Bittinger, M.A.5    Jang, H.G.6
  • 11
    • 77649305610 scopus 로고    scopus 로고
    • The common feature of leukemia-associated IDH1 and IDH2 mutations is a neomorphic enzyme activity converting alpha-ketoglutarate to 2-hydroxyglutarate
    • Ward PS, Patel J, Wise DR, Abdel-Wahab O, Bennett BD, Coller HA, 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 2010;17:225–34.
    • (2010) Cancer Cell , vol.17 , pp. 225-234
    • Ward, P.S.1    Patel, J.2    Wise, D.R.3    Abdel-Wahab, O.4    Bennett, B.D.5    Coller, H.A.6
  • 13
    • 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
  • 14
    • 78651463452 scopus 로고    scopus 로고
    • Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutaratedependent dioxygenases
    • Xu W, Yang H, Liu Y, Yang Y, Wang P, Kim SH, et al. Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-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
  • 15
    • 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
  • 16
    • 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
  • 17
    • 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
  • 18
    • 84858796263 scopus 로고    scopus 로고
    • IDH1 mutation is sufficient to establish the glioma hypermethylator phenotype
    • Turcan S, Rohle D, Goenka A, Walsh LA, Fang F, Yilmaz E, et al. IDH1 mutation is sufficient to establish the glioma hypermethylator phenotype. Nature 2012;483:479–83.
    • (2012) Nature , vol.483 , pp. 479-483
    • Turcan, S.1    Rohle, D.2    Goenka, A.3    Walsh, L.A.4    Fang, F.5    Yilmaz, E.6
  • 19
    • 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
  • 20
    • 84907033777 scopus 로고    scopus 로고
    • Mutant IDH inhibits HNF-4α to block hepatocyte differentiation and promote biliary cancer
    • Saha SK, Parachoniak CA, Ghanta KS, Fitamant J, Ross KN, Najem MS, et al. Mutant IDH inhibits HNF-4α to block hepatocyte differentiation and promote biliary cancer. Nature 2014;513:110–4.
    • (2014) Nature , vol.513 , pp. 110-114
    • Saha, S.K.1    Parachoniak, C.A.2    Ghanta, K.S.3    Fitamant, J.4    Ross, K.N.5    Najem, M.S.6
  • 23
    • 84884575080 scopus 로고    scopus 로고
    • Cancerassociated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition
    • Chen C, Liu Y, Lu C, Cross JR, Morris 4th JP, Shroff AS, et al. Cancerassociated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition. Genes Dev 2013;27:1974–85.
    • (2013) Genes Dev , vol.27 , pp. 1974-1985
    • Chen, C.1    Liu, Y.2    Lu, C.3    Cross, J.R.4    Morris, J.P.5    Shroff, A.S.6
  • 25
    • 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
  • 26
    • 84894245627 scopus 로고    scopus 로고
    • Identification of pre-leukaemic haematopoietic stem cells in acute leukaemia
    • Shlush LI, Zandi S, Mitchell A, Chen WC, Brandwein JM, Gupta V, et al. Identification of pre-leukaemic haematopoietic stem cells in acute leukaemia. Nature 2014;506:328–33.
    • (2014) Nature , vol.506 , pp. 328-333
    • Shlush, L.I.1    Zandi, S.2    Mitchell, A.3    Chen, W.C.4    Brandwein, J.M.5    Gupta, V.6
  • 27
    • 84894304555 scopus 로고    scopus 로고
    • Preleukemic mutations in human acute myeloid leukemia affect epigenetic regulators and persist in remission
    • Corces-Zimmerman MR, Hong WJ, Weissman IL, Medeiros BC, Majeti R. Preleukemic mutations in human acute myeloid leukemia affect epigenetic regulators and persist in remission. Proc Natl Acad Sci U S A 2014;111:2548–53.
    • (2014) Proc Natl Acad Sci U S A , vol.111 , pp. 2548-2553
    • Corces-Zimmerman, M.R.1    Hong, W.J.2    Weissman, I.L.3    Medeiros, B.C.4    Majeti, R.5
  • 28
    • 84961391278 scopus 로고    scopus 로고
    • Clonal evolution of preleukemic hematopoietic stem cells in acute myeloid leukemia
    • Sykes SM, Kokkaliaris KD, Milsom MD, Levine RL, Majeti R. Clonal evolution of preleukemic hematopoietic stem cells in acute myeloid leukemia. Exp Hematol 2015;43:989–92.
    • (2015) Exp Hematol , vol.43 , pp. 989-992
    • Sykes, S.M.1    Kokkaliaris, K.D.2    Milsom, M.D.3    Levine, R.L.4    Majeti, R.5
  • 29
    • 77952536841 scopus 로고    scopus 로고
    • IDH1 and IDH2 gene mutations identify novel molecular subsets within de novo cytogenetically normal acute myeloid leukemia: A Cancer and Leukemia Group B study
    • Marcucci G, Maharry K, Wu YZ, Radmacher MD, Mrozek K, Margeson D, et al. IDH1 and IDH2 gene mutations identify novel molecular subsets within de novo cytogenetically normal acute myeloid leukemia: A Cancer and Leukemia Group B study. J Clin Oncol 2010;28:2348–55.
    • (2010) J Clin Oncol , vol.28 , pp. 2348-2355
    • Marcucci, G.1    Maharry, K.2    Wu, Y.Z.3    Radmacher, M.D.4    Mrozek, K.5    Margeson, D.6
  • 30
    • 79960534917 scopus 로고    scopus 로고
    • The prognostic significance of IDH2 mutations in AML depends on the location of the mutation
    • Green CL, Evans CM, Zhao L, Hills RK, Burnett AK, Linch DC, et al. The prognostic significance of IDH2 mutations in AML depends on the location of the mutation. Blood 2011;118:409–12.
    • (2011) Blood , vol.118 , pp. 409-412
    • Green, C.L.1    Evans, C.M.2    Zhao, L.3    Hills, R.K.4    Burnett, A.K.5    Linch, D.C.6
  • 31
    • 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, W.G.2
  • 32
    • 79958126696 scopus 로고    scopus 로고
    • A tale of two subunits: How the neomorphic R132H IDH1 mutation enhances production of αHG
    • Pietrak B, Zhao H, Qi H, Quinn C, Gao E, Boyer JG, et al. A tale of two subunits: How the neomorphic R132H IDH1 mutation enhances production of αHG. Biochemistry 2011;50:4804–12.
    • (2011) Biochemistry , vol.50 , pp. 4804-4812
    • Pietrak, B.1    Zhao, H.2    Qi, H.3    Quinn, C.4    Gao, E.5    Boyer, J.G.6
  • 33
    • 78049480082 scopus 로고    scopus 로고
    • Molecular mechanisms of “off-on switch” of activities of human IDH1 by tumor-associated mutation R132H
    • Yang B, Zhong C, Peng Y, Lai Z, Ding J. Molecular mechanisms of “off-on switch” of activities of human IDH1 by tumor-associated mutation R132H. Cell Res 2010;20:1188–200.
    • (2010) Cell Res , vol.20 , pp. 1188-1200
    • Yang, B.1    Zhong, C.2    Peng, Y.3    Lai, Z.4    Ding, J.5
  • 34
    • 84870557152 scopus 로고    scopus 로고
    • Prospective serial evaluation of 2-hydroxyglutarate, during treatment of newly diagnosed acute myeloid leukemia, to assess disease activity and therapeutic response
    • Fathi AT, Sadrzadeh H, Borger DR, Ballen KK, Amrein PC, Attar EC, et al. Prospective serial evaluation of 2-hydroxyglutarate, during treatment of newly diagnosed acute myeloid leukemia, to assess disease activity and therapeutic response. Blood 2012;120:4649–52.
    • (2012) Blood , vol.120 , pp. 4649-4652
    • Fathi, A.T.1    Sadrzadeh, H.2    Borger, D.R.3    Ballen, K.K.4    Amrein, P.C.5    Attar, E.C.6
  • 35
    • 84983549729 scopus 로고    scopus 로고
    • Granulopoiesis and granules of human neutrophils
    • Cowland JB, Borregaard N. Granulopoiesis and granules of human neutrophils. Immunol Rev 2016;273:11–28.
    • (2016) Immunol Rev , vol.273 , pp. 11-28
    • Cowland, J.B.1    Borregaard, N.2
  • 36
    • 77449159028 scopus 로고    scopus 로고
    • Diagnosis and management of acute myeloid leukemia in adults: Recommendations from an international expert panel, on behalf of the European LeukemiaNet
    • Döhner H, Estey EH, Amadori S, Appelbaum FR, Buchner T, Burnett AK, et al. Diagnosis and management of acute myeloid leukemia in adults: Recommendations from an international expert panel, on behalf of the European LeukemiaNet. Blood 2010;115:453–74.
    • (2010) Blood , vol.115 , pp. 453-474
    • Döhner, H.1    Estey, E.H.2    Amadori, S.3    Appelbaum, F.R.4    Buchner, T.5    Burnett, A.K.6
  • 37
  • 38
    • 84939558433 scopus 로고    scopus 로고
    • IDH1 and IDH2 mutations in myelodysplastic syndromes and role in disease progression
    • DiNardo CD, Jabbour E, Ravandi F, Takahashi K, Daver N, Routbort M, et al. IDH1 and IDH2 mutations in myelodysplastic syndromes and role in disease progression. Leukemia 2015;30:980–4.
    • (2015) Leukemia , vol.30 , pp. 980-984
    • Dinardo, C.D.1    Jabbour, E.2    Ravandi, F.3    Takahashi, K.4    Daver, N.5    Routbort, M.6
  • 39
    • 84920971376 scopus 로고    scopus 로고
    • IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition
    • Kernytsky A, Wang F, Hansen E, Schalm S, Straley K, Gliser C, et al. IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition. Blood 2015;125:296–303.
    • (2015) Blood , vol.125 , pp. 296-303
    • Kernytsky, A.1    Wang, F.2    Hansen, E.3    Schalm, S.4    Straley, K.5    Gliser, C.6
  • 40
    • 41949111045 scopus 로고    scopus 로고
    • Acute promyelocytic leukemia: From highly fatal to highly curable
    • Wang ZY, Chen Z. Acute promyelocytic leukemia: From highly fatal to highly curable. Blood 2008;111:2505–15.
    • (2008) Blood , vol.111 , pp. 2505-2515
    • Wang, Z.Y.1    Chen, Z.2
  • 41
    • 84954246999 scopus 로고    scopus 로고
    • Safety and efficacy of AG-221, a potent inhibitor of mutant IDH2 that promotes differentiation of myeloid cells in patients with advanced hematologic malignancies: Results of a phase 1/2 trial
    • Stein EM, DiNardo C, Altman JK, Collins R, DeAngelo DJ, Kantarjian HM, et al. Safety and efficacy of AG-221, a potent inhibitor of mutant IDH2 that promotes differentiation of myeloid cells in patients with advanced hematologic malignancies: Results of a phase 1/2 trial. Blood 2015;126:323.
    • (2015) Blood , vol.126 , pp. 323
    • Stein, E.M.1    Dinardo, C.2    Altman, J.K.3    Collins, R.4    Deangelo, D.J.5    Kantarjian, H.M.6
  • 42
    • 0031059866 scopus 로고    scopus 로고
    • Processing of X-ray diffraction data collected in oscillation mode
    • Otwinowski Z, Minor W. Processing of X-ray diffraction data collected in oscillation mode. Methods Enzymol 1997;276:307–26.
    • (1997) Methods Enzymol , vol.276 , pp. 307-326
    • Otwinowski, Z.1    Minor, W.2
  • 46
    • 77957286222 scopus 로고    scopus 로고
    • Prognostic impact of isocitrate dehydrogenase enzyme isoforms 1 and 2 mutations in acute myeloid leukemia: A study by the Acute Leukemia French Association group
    • Boissel N, Nibourel O, Renneville A, Gardin C, Reman O, Contentin N, et al. Prognostic impact of isocitrate dehydrogenase enzyme isoforms 1 and 2 mutations in acute myeloid leukemia: A study by the Acute Leukemia French Association group. J Clin Oncol 2010;28:3717–23.
    • (2010) J Clin Oncol , vol.28 , pp. 3717-3723
    • Boissel, N.1    Nibourel, O.2    Renneville, A.3    Gardin, C.4    Reman, O.5    Contentin, N.6
  • 47
    • 84959419471 scopus 로고    scopus 로고
    • Mutation allele burden remains unchanged in chronic myelomonocytic leukaemia responding to hypomethylating agents
    • Merlevede J, Droin N, Qin T, Meldi K, Yoshida K, Morabito M, et al. Mutation allele burden remains unchanged in chronic myelomonocytic leukaemia responding to hypomethylating agents. Nat Commun 2016;7:10767.
    • (2016) Nat Commun , vol.7 , pp. 10767
    • Merlevede, J.1    Droin, N.2    Qin, T.3    Meldi, K.4    Yoshida, K.5    Morabito, M.6
  • 48
    • 84964461711 scopus 로고    scopus 로고
    • Quantitation of isocitrate dehydrogenase (IDH)- induced D and L enantiomers of 2-hydroxyglutaric acid in biological fluids by a fully validated liquid tandem mass spectrometry method, suitable for clinical applications
    • Poinsignon V, Mercier L, Nakabayashi K, David MD, Lalli A, Penard- Lacronique V, et al. Quantitation of isocitrate dehydrogenase (IDH)- induced D and L enantiomers of 2-hydroxyglutaric acid in biological fluids by a fully validated liquid tandem mass spectrometry method, suitable for clinical applications. J Chromatogr B Analyt Technol Biomed Life Sci 2016;1022:290–7.
    • (2016) J Chromatogr B Analyt Technol Biomed Life Sci , vol.1022 , pp. 290-297
    • Poinsignon, V.1    Mercier, L.2    Nakabayashi, K.3    David, M.D.4    Lalli, A.5    Penard- Lacronique, V.6
  • 50
    • 79958789936 scopus 로고    scopus 로고
    • Activity of the multikinase inhibitor sorafenib in combination with cytarabine in acute myeloid leukemia
    • Hu S, Niu H, Inaba H, Orwick S, Rose C, Panetta JC, et al. Activity of the multikinase inhibitor sorafenib in combination with cytarabine in acute myeloid leukemia. J Natl Cancer Inst 2011;103:893–905.
    • (2011) J Natl Cancer Inst , vol.103 , pp. 893-905
    • Hu, S.1    Niu, H.2    Inaba, H.3    Orwick, S.4    Rose, C.5    Panetta, J.C.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.