title: Specific inhibition of DNMT1/CFP1 reduces cancer phenotypes and enhances chemotherapy effectiveness.
abstract: OBJECTIVE
  DNA methylation is a fundamental biologic process of genomes and is a candidate for pharmacological manipulation that might have important therapeutic advantages. Thus, DNA methyltransferases (DNMTs) appear to be ideal targets for drug intervention.
  
  
  METHODS
  To develop a new generation of DNMT inhibitor, we analyzed the ability of peptides to selectively inhibit certain DNMT1-incuding complexes.
  
  
  RESULTS
  Our study demonstrates that the disruption of DNMT1/CFP1-including complexes increases the efficiency of chemotherapeutic treatment on established tumors in mice.
  
  
  CONCLUSIONS
  Our data opens a promising and innovative alternative to the development of DNMT inhibitors.
authors.affiliation: UMR 892 INSERM, 6299 CNRS, Nantes, France.
authors.forename: Mathilde
authors.initials: M
authors.lastname: Cheray
authors.forename: Arulraj
authors.initials: A
authors.lastname: Nadaradjane
authors.forename: Pascal
authors.initials: P
authors.lastname: Bonnet
authors.forename: Sylvain
authors.initials: S
authors.lastname: Routier
authors.forename: François M
authors.initials: FM
authors.lastname: Vallette
authors.forename: Pierre-François
authors.initials: PF
authors.lastname: Cartron
mesh_terms: D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D000076123:DNA (Cytosine-5-)-Methyltransferase 1; D004248:DNA (Cytosine-5-)-Methyltransferases / Q000037:antagonists & inhibitors*; D003606:Dacarbazine / Q000031:analogs & derivatives / Q000627:therapeutic use; D004357:Drug Synergism; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D044127:Epigenesis, Genetic; D005260:Female; D015972:Gene Expression Regulation, Neoplastic; D005910:Glioma / Q000188:drug therapy / Q000473:pathology*; D051379:Mice; D009368:Neoplasm Transplantation; D010455:Peptides / Q000494:pharmacology*; D000077204:Temozolomide; D015534:Trans-Activators / Q000037:antagonists & inhibitors*
chemical_list: C501971:Cxxc1 protein, mouse; D004791:Enzyme Inhibitors; D010455:Peptides; D015534:Trans-Activators; D003606:Dacarbazine; D000076123:DNA (Cytosine-5-)-Methyltransferase 1; D004248:DNA (Cytosine-5-)-Methyltransferases; C000619381:Dnmt1 protein, mouse; D000077204:Temozolomide
keywords: DNA methylation; DNMT inhibitor; DNMT1; cell death; epigenetic; glioblastoma; glioma