메뉴 건너뛰기




Volumn 13, Issue 4, 2014, Pages 842-854

Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; EPZ 6438; HISTONE H3; LYSINE; TRANSCRIPTION FACTOR EZH2; UNCLASSIFIED DRUG; BENZAMIDE DERIVATIVE; EPZ-6438; POLYCOMB REPRESSIVE COMPLEX 2; PYRIDONE DERIVATIVE;

EID: 84921318899     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-13-0773     Document Type: Article
Times cited : (466)

References (32)
  • 1
    • 84875424617 scopus 로고    scopus 로고
    • Emerging roles for chromatin as a signal integration and storage platform
    • Badeaux AI, Shi Y. Emerging roles for chromatin as a signal integration and storage platform. Nat Rev Mol Cell Biol 2013;14:211-24.
    • (2013) Nat Rev Mol Cell Biol , vol.14 , pp. 211-224
    • Badeaux, A.I.1    Shi, Y.2
  • 2
    • 69949148388 scopus 로고    scopus 로고
    • Protein methyltransferases as a target class for drug discovery
    • Copeland RA, Solomon ME, Richon VM. Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov 2009;8:724-32.
    • (2009) Nat Rev Drug Discov , vol.8 , pp. 724-732
    • Copeland, R.A.1    Solomon, M.E.2    Richon, V.M.3
  • 3
    • 84874789539 scopus 로고    scopus 로고
    • Targeting genetic alterations in protein methyltransferases for personalized cancer therapeutics
    • Copeland RA, Moyer MP, Richon VM. Targeting genetic alterations in protein methyltransferases for personalized cancer therapeutics. Oncogene 2013;32:939-46.
    • (2013) Oncogene , vol.32 , pp. 939-946
    • Copeland, R.A.1    Moyer, M.P.2    Richon, V.M.3
  • 4
    • 78751662908 scopus 로고    scopus 로고
    • The polycomb complex PRC2 and its mark in life
    • Margueron R, Reinberg D. The polycomb complex PRC2 and its mark in life. Nature 2011;469:343-9.
    • (2011) Nature , vol.469 , pp. 343-349
    • Margueron, R.1    Reinberg, D.2
  • 5
    • 84864876023 scopus 로고    scopus 로고
    • Inner workings and regulatory inputs that control polycomb repressive complex 2
    • O'Meara MM, Simon JA. Inner workings and regulatory inputs that control polycomb repressive complex 2. Chromosoma 2012;121:221-34.
    • (2012) Chromosoma , vol.121 , pp. 221-234
    • O'Meara, M.M.1    Simon, J.A.2
  • 6
    • 79955513100 scopus 로고    scopus 로고
    • Aberrations of EZH2 in cancer
    • Chase A, Cross NC. Aberrations of EZH2 in cancer. Clin Cancer Res 2011;17:2613-8.
    • (2011) Clin Cancer Res , vol.17 , pp. 2613-2618
    • Chase, A.1    Cross, N.C.2
  • 7
    • 84857942952 scopus 로고    scopus 로고
    • Discovery and prioritization of somatic mutations in diffuse large B-cell lymphoma (DLBCL) by whole-exome sequencing
    • Lohr JG, Stojanov P, Lawrence MS, Auclair D, Chapuy B, Sougnez C, et al. Discovery and prioritization of somatic mutations in diffuse large B-cell lymphoma (DLBCL) by whole-exome sequencing. Proc Natl Acad Sci U S A 2012;109:3879-84.
    • (2012) Proc Natl Acad Sci U S a , vol.109 , pp. 3879-3884
    • Lohr, J.G.1    Stojanov, P.2    Lawrence, M.S.3    Auclair, D.4    Chapuy, B.5    Sougnez, C.6
  • 8
    • 75749124332 scopus 로고    scopus 로고
    • Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin
    • Morin RD, Johnson NA, Severson TM, Mungall AJ, An J, Goya R, et al. Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin. Nat Genet 2010;42:181-5.
    • (2010) Nat Genet , vol.42 , pp. 181-185
    • Morin, R.D.1    Johnson, N.A.2    Severson, T.M.3    Mungall, A.J.4    An, J.5    Goya, R.6
  • 10
    • 0034598746 scopus 로고    scopus 로고
    • Distinct types of diffuse large B-cell lymphoma identified by gene expression profiling
    • Alizadeh AA, Eisen MB, Davis RE, Ma C, Lossos IS, Rosenwald A, et al. Distinct types of diffuse large B-cell lymphoma identified by gene expression profiling. Nature 2000;403:503-11.
    • (2000) Nature , vol.403 , pp. 503-511
    • Alizadeh, A.A.1    Eisen, M.B.2    Davis, R.E.3    Ma, C.4    Lossos, I.S.5    Rosenwald, A.6
  • 11
    • 84877815031 scopus 로고    scopus 로고
    • EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation
    • Beguelin W, Popovic R, Teater M, Jiang Y, Bunting KL, Rosen M, et al. EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation. Cancer Cell 2013;23:677-92.
    • (2013) Cancer Cell , vol.23 , pp. 677-692
    • Beguelin, W.1    Popovic, R.2    Teater, M.3    Jiang, Y.4    Bunting, K.L.5    Rosen, M.6
  • 13
    • 84863165348 scopus 로고    scopus 로고
    • Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)
    • McCabe MT, Graves AP, Ganji G, Diaz E, Halsey WS, Jiang Y, et al. Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27). Proc Natl Acad Sci 2012;109:2989-94.
    • (2012) Proc Natl Acad Sci , vol.109 , pp. 2989-2994
    • McCabe, M.T.1    Graves, A.P.2    Ganji, G.3    Diaz, E.4    Halsey, W.S.5    Jiang, Y.6
  • 14
    • 78650454078 scopus 로고    scopus 로고
    • Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas
    • Sneeringer CJ, Scott MP, Kuntz KW, Knutson SK, Pollock RM, Richon VM, et al. Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas. Proc Natl Acad Sci 2010;107:20980-5.
    • (2010) Proc Natl Acad Sci , vol.107 , pp. 20980-20985
    • Sneeringer, C.J.1    Scott, M.P.2    Kuntz, K.W.3    Knutson, S.K.4    Pollock, R.M.5    Richon, V.M.6
  • 15
    • 80053279825 scopus 로고    scopus 로고
    • The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states
    • Wigle TJ, Knutson SK, Jin L, Kuntz KW, Pollock RM, Richon VM, et al. The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states. FEBS Lett 2011;585:3011-4.
    • (2011) FEBS Lett , vol.585 , pp. 3011-3014
    • Wigle, T.J.1    Knutson, S.K.2    Jin, L.3    Kuntz, K.W.4    Pollock, R.M.5    Richon, V.M.6
  • 16
    • 79952167230 scopus 로고    scopus 로고
    • Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation
    • Yap DB, Chu J, Berg T, Schapira M, Cheng SW, Moradian A, et al. Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation. Blood 2011;117:2451-9.
    • (2011) Blood , vol.117 , pp. 2451-2459
    • Yap, D.B.1    Chu, J.2    Berg, T.3    Schapira, M.4    Cheng, S.W.5    Moradian, A.6
  • 18
    • 84879750981 scopus 로고    scopus 로고
    • An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1
    • Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, et al. An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1. ACS Chem Biol 2013;8:1324-34.
    • (2013) ACS Chem Biol , vol.8 , pp. 1324-1334
    • Konze, K.D.1    Ma, A.2    Li, F.3    Barsyte-Lovejoy, D.4    Parton, T.5    Macnevin, C.J.6
  • 19
    • 84870573126 scopus 로고    scopus 로고
    • EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations
    • McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature 2012;492:108-12.
    • (2012) Nature , vol.492 , pp. 108-112
    • McCabe, M.T.1    Ott, H.M.2    Ganji, G.3    Korenchuk, S.4    Thompson, C.5    Van Aller, G.S.6
  • 20
    • 84871841675 scopus 로고    scopus 로고
    • Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation
    • Qi W, Chan H, Teng L, Li L, Chuai S, Zhang R, et al. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci U S A 2012;109:21360-5.
    • (2012) Proc Natl Acad Sci U S a , vol.109 , pp. 21360-21365
    • Qi, W.1    Chan, H.2    Teng, L.3    Li, L.4    Chuai, S.5    Zhang, R.6
  • 21
    • 84877324084 scopus 로고    scopus 로고
    • Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2
    • Knutson SK, Warholic NM, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A 2013;110:7922-7.
    • (2013) Proc Natl Acad Sci U S a , vol.110 , pp. 7922-7927
    • Knutson, S.K.1    Warholic, N.M.2    Wigle, T.J.3    Klaus, C.R.4    Allain, C.J.5    Raimondi, A.6
  • 22
    • 42649112047 scopus 로고    scopus 로고
    • An embryonic stem cell-like gene expression signature in poorly differentiated aggressive human tumors
    • Ben-Porath I, Thomson MW, Carey VJ, Ge R, Bell GW, Regev A, et al. An embryonic stem cell-like gene expression signature in poorly differentiated aggressive human tumors. Nat Genet 2008;40:499-507.
    • (2008) Nat Genet , vol.40 , pp. 499-507
    • Ben-Porath, I.1    Thomson, M.W.2    Carey, V.J.3    Ge, R.4    Bell, G.W.5    Regev, A.6
  • 23
    • 78650062951 scopus 로고    scopus 로고
    • EZH2-mediated epigenetic silencing in germinal center B cells contributes to proliferation and lymphomagenesis
    • Velichutina I, Shaknovich R, Geng H, Johnson NA, Gascoyne RD, Melnick AM, et al. EZH2-mediated epigenetic silencing in germinal center B cells contributes to proliferation and lymphomagenesis. Blood 2010;116:5247-55.
    • (2010) Blood , vol.116 , pp. 5247-5255
    • Velichutina, I.1    Shaknovich, R.2    Geng, H.3    Johnson, N.A.4    Gascoyne, R.D.5    Melnick, A.M.6
  • 24
    • 84877278637 scopus 로고    scopus 로고
    • Implementing personalized cancer genomics in clinical trials
    • Simon R, Roychowdhury S. Implementing personalized cancer genomics in clinical trials. Nat Rev Drug Discov 2013;12:358-69.
    • (2013) Nat Rev Drug Discov , vol.12 , pp. 358-369
    • Simon, R.1    Roychowdhury, S.2
  • 27
    • 84881086323 scopus 로고    scopus 로고
    • Cancer as a dysregulated epigenome allowing cellular growth advantage at the expense of the host
    • Timp W, Feinberg AP. Cancer as a dysregulated epigenome allowing cellular growth advantage at the expense of the host. Nat Rev Cancer 2013;13:497-510.
    • (2013) Nat Rev Cancer , vol.13 , pp. 497-510
    • Timp, W.1    Feinberg, A.P.2
  • 29
    • 84869003466 scopus 로고    scopus 로고
    • Epigenetic therapy leaps ahead with specific targeting of EZH2
    • Melnick A. Epigenetic therapy leaps ahead with specific targeting of EZH2. Cancer Cell 2012;22:569-70.
    • (2012) Cancer Cell , vol.22 , pp. 569-570
    • Melnick, A.1
  • 30
    • 84879000598 scopus 로고    scopus 로고
    • Phosphorylation of EZH2 activates STAT3 signaling via STAT3 methylation and promotes tumorigenicity of glioblastoma stem-like cells
    • Kim E, Kim M, Woo DH, Shin Y, Shin J, Chang N, et al. Phosphorylation of EZH2 activates STAT3 signaling via STAT3 methylation and promotes tumorigenicity of glioblastoma stem-like cells. Cancer Cell 2013;23:839-52.
    • (2013) Cancer Cell , vol.23 , pp. 839-852
    • Kim, E.1    Kim, M.2    Woo, D.H.3    Shin, Y.4    Shin, J.5    Chang, N.6
  • 31
    • 84871052080 scopus 로고    scopus 로고
    • EZH2 oncogenic activity in castration-resistant prostate cancer cells is polycomb-independent
    • Xu K, Wu ZJ, Groner AC, He HH, Cai C, Lis RT, et al. EZH2 oncogenic activity in castration-resistant prostate cancer cells is polycomb-independent. Science 2012;338:1465-9.
    • (2012) Science , vol.338 , pp. 1465-1469
    • Xu, K.1    Wu, Z.J.2    Groner, A.C.3    He, H.H.4    Cai, C.5    Lis, R.T.6
  • 32
    • 0142105414 scopus 로고    scopus 로고
    • EZH2 is downstream of the pRB-E2F pathway, essential for proliferation and amplified in cancer
    • Bracken AP, Pasini D, Capra M, Prosperini E, Colli E, Helin K. EZH2 is downstream of the pRB-E2F pathway, essential for proliferation and amplified in cancer. EMBO J 2003;22:5323-35.
    • (2003) EMBO J , vol.22 , pp. 5323-5335
    • Bracken, A.P.1    Pasini, D.2    Capra, M.3    Prosperini, E.4    Colli, E.5    Helin, K.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.