Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer Activities (Articolo in rivista)

Type
Label
  • Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer Activities (Articolo in rivista) (literal)
Anno
  • 2014-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/jm4012802 (literal)
Alternative label
  • Rotili, Dante; Tomassi, Stefano; Conte, Mariarosaria; Benedetti, Rosaria; Tortorici, Marcello; Ciossani, Giuseppe; Valente, Sergio; Marrocco, Biagina; Labella, Donatella; Novellino, Ettore; Mattevi, Andrea; Altucci, Lucia; Tumber, Anthony; Yapp, Clarence; King, Oliver N. F.; Hopkinson, Richard J.; Kawamura, Akane; Schofield, Christopher J.; Mai, Antonello (2014)
    Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer Activities
    in Journal of medicinal chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Rotili, Dante; Tomassi, Stefano; Conte, Mariarosaria; Benedetti, Rosaria; Tortorici, Marcello; Ciossani, Giuseppe; Valente, Sergio; Marrocco, Biagina; Labella, Donatella; Novellino, Ettore; Mattevi, Andrea; Altucci, Lucia; Tumber, Anthony; Yapp, Clarence; King, Oliver N. F.; Hopkinson, Richard J.; Kawamura, Akane; Schofield, Christopher J.; Mai, Antonello (literal)
Pagina inizio
  • 42 (literal)
Pagina fine
  • 55 (literal)
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  • 57 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 14 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 1 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy Department of Pharmacy, University of Naples \"Federico II\", Via D. Montesano 49, 80131 Naples, Italy Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, Vico L. De Crecchio 7, 80138 Naples, Italy Department of Biology and Biotechnology, University of Pavia, Via Ferrata 9, 27100 Pavia, Italy Institute of Genetics and Biophysics, Consiglio Nazionale delle Ricerche, Via P. Castellino, 80100 Naples, Italy Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosvelt Drive, Headington OX3 7DU, United Kingdom Chemistry Research Laboratory University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, United Kingdo (literal)
Titolo
  • Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer Activities (literal)
Abstract
  • In prostate cancer, two different types of histone lysine demethylases (KDM), LSD1/KDM1 and JMJD2/KDM4, are coexpressed and colocalize with the androgen receptor. We designed and synthesized hybrid LSD1/JmjC or \"pan-KDM\" inhibitors 1-6 by coupling the skeleton of tranylcypromine 7, a known LSD1 inhibitor, with 4-carboxy-4'-carbomethoxy-2,2'-bipyridine 8 or 5-carboxy-8-hydroxyquinoline 9, two 2-oxoglutarate competitive templates developed for JmjC inhibition. Hybrid compounds 1-6 are able to simultaneously target both KDM families and have been validated as potential antitumor agents in cells. Among them, 2 and 3 increase H3K4 and H3K9 methylation levels in cells and cause growth arrest and substantial apoptosis in LNCaP prostate and HCT116 colon cancer cells. When tested in noncancer mesenchymal progenitor (MePR) cells, 2 and 3 induced little and no apoptosis, respectively, thus showing cancer-selective inhibiting action. (literal)
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