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Future Medicinal Chemistry Volume 6, 2014 - Issue 11
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Editorial

Challenges in Developing Novel DNA Methyltransferases Inhibitors for Cancer Therapy

Dominique Guianvarc’ha Laboratoire des BioMolécules, Sorbonne Universités, UPMC Univ Paris 06, CNRS, UMR 7203, Ecole Normale Supérieure, 4, place Jussieu, F-75005, Paris, France Tel.: +33 144 275 [email protected]Correspondence[email protected]
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&
Paola Barbara Arimondob USR CNRS-Pierre Fabre n°3388ETaC, CRDPF BP 13562, 3 avenue Hubert Curien, F-31100Toulouse, FranceView further author information
Pages 1237-1240 | Published online: 27 Aug 2014

References

  • Jurkowska RZ , JurkowskiTP, JeltschA. Structure and function of mammalian DNA methyltransferases. Chembiochem.12 (2), 206–222 (2011).
  • Weber M , HellmannI, StadlerMBet al. Distribution, silencing potential and evolutionary impact of promoter DNA methylation in the human genome. Nat. Genet.39 (4), 457–466 (2007).
  • Baylin SB , JonesPA. A decade of exploring the cancer epigenome – biological and translational implications. Nat. Rev. Cancer11 (10), 726–734 (2011).
  • Mai A , AltucciL. Epi-drugs to fight cancer: from chemistry to cancer treatment, the road ahead. Int. J. Biochem. Cell Biol.41 (1), 199–213 (2009).
  • Issa J-PJ , KantarjianHM. Targeting DNA methylation. Clin. Cancer Res.15 (12), 3938–3946 (2009).
  • Stresemann C , LykoF. Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine. Int. J. Cancer.123 (1), 8–13 (2008).
  • Juergens RA , WrangleJ, VendettiFPet al. Combination epigenetic therapy has efficacy in patients with refractory advanced non-small cell lung cancer. Cancer Discovery1 (7), 598–607 (2011).
  • ClinicalTrials.gov . www.clinicaltrials.gov
  • Boumber Y , KantarjianH, JorgensenJet al. A randomized study of decitabine versus conventional care for maintenance therapy in patients with acute myeloid leukemia in complete remission. Leukemia.26 (11), 2428–2431 (2012).
  • Chuang JC , WarnerSL, VollmerDet al. S110, a 5-aza-2’-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth. Mol. Cancer Ther.9 (5), 1443–1450 (2010).
  • Fang MZ , ChenD, SunY, JinZ, ChristmanJK, YangCS. Reversal of hypermethylation and reactivation of p16INK4a, RARβ, and MGMT genes by genistein and other isoflavones from soy. Clin. Cancer Res.11 (19), 7033–7041 (2005).
  • Ceccaldi A , RajaveluA, ChampionCet al. C5-DNA methyltransferase inhibitors: from screening to effects on zebrafish embryo development. Chembiochem.12 (9), 1337–1345 (2011).
  • Brueckner B , BoyRG, SiedleckiPet al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res.65 (14), 6305–6311 (2005).
  • Datta J , GhoshalK, DennyWAet al. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res.69 (10), 4277–4285 (2009).
  • Ceccaldi A , RajaveluA, RagozinSet al. Identification of novel inhibitors of DNA methylation by screening of a chemical library. ACS Chem. Biol.8 (3), 543–548 (2013).
  • Fagan RL , WuM, ChédinF, BrennerC. An ultrasensitive high throughput screen for DNA methyltransferase 1-targeted molecular probes. PLoS ONE8 (11), e78752 (2013).
  • Kilgore JA , DuX, MelitoLet al. Identification of DNMT1 selective antagonists using a novel scintillation proximity assay. J. Biol. Chem.288 (27), 19673–19684 (2013).
  • Gros C , ChauvignéL, PouletAet al. Development of a universal radioactive DNA methyltransferase inhibition test for high-throughput screening and mechanistic studies. Nucleic Acids Res.41 (19), e185 (2013).
  • Song J , RechkoblitO, BestorTH, PatelDJ. Structure of DNMT1–DNA complex reveals a role for auto inhibition in maintenance DNA methylation. Science331 (6020), 1036–1040 (2011).
  • Song J , TeplovaM, Ishibe-MurakamiS, PatelDJ. Structure-based mechanistic insights into DNMT1-mediated maintenance DNA methylation. Science335 (6069), 709–712 (2012).
  • Takeshita K , SuetakeI, YamashitaEet al. Structural insight into maintenance methylation by mouse DNA methyltransferase 1 (Dnmt1). Proc. Natl Acad. Sci. USA108 (22), 9055–9059 (2011).
  • Jia D , JurkowskaRZ, ZhangX, JeltschA, ChengX. Structure of Dnmt3a bound to Dnmt3L suggests a model for de novo DNA methylation. Nature449 (7159),  248–251  (2007).
  • Yoo J , Medina-FrancoJL. Homology modeling, docking and structure-based pharmacophore of inhibitors of DNA methyltransferase. J. Comput. Aided Mol. Des.25 (6), 555–567 (2011).
  • Asgatay S , ChampionC, MarloieGet al. Synthesis and evaluation of analogues of N-phthaloyl-l-tryptophan (RG108) as inhibitors of DNA methyltransferase 1. J. Med. Chem.57 (2), 421–434 (2014).
  • Yu W , ChoryEJ, WernimontAKet al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat. Commun.3, 1288 (2012).
  • Filippakopoulos P , QiJ, PicaudSet al. Selective inhibition of BET bromodomains. Nature468 (7327), 1067–1073 (2010).

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