Targeting histone demethylases in cancer therapy.
A novel oligoamine analog inhibitor of histone demethylases blocks colon tumor cell growth in association with histone methylation and gene re-expression. It also markedly potentiates the activity of hypomethylating agents in vitro and in vivo, suggesting that histone demethylase inhibitors may represent a valuable addition to the armamentarium of epigenetic agents.
Grant
Steven
S
Department of Medicine, Virginia Commonwealth University/Massey Cancer Center, Richmond, Virginia 23298-0035, USA. stgrant@vcu.edu
D000588:Amines / Q000737:chemistry; D000970:Antineoplastic Agents / Q000494:pharmacology*; D019175:DNA Methylation; D044127:Epigenesis, Genetic; D020868:Gene Silencing; D056466:Histone Demethylases / Q000378:metabolism*; D006657:Histones / Q000378:metabolism; D006801:Humans; D008954:Models, Biological; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism*; D015398:Signal Transduction
D000588:Amines; D000970:Antineoplastic Agents; D006657:Histones; D056466:Histone Demethylases