The role of histone demethylases in cancer therapy.
Reversible histone methylation has emerged in the last few years as an important mechanism of epigenetic regulation. Histone methyltransferases and demethylases have been identified as contributing factors in the development of several diseases, especially cancer. Therefore, they have been postulated to be new drug targets with high therapeutic potential. Here, we review histone demethylases with a special focus on their potential role in oncology drug discovery. We present an overview over the different classes of enzymes, their biochemistry, selected data on their role in physiology and already available inhibitors.
Institute of Pharmaceutical Sciences, Albert-Ludwigs-University of Freiburg, Albertstr. 25, 79104 Freiburg, Germany.
Inga
I
Hoffmann
Martin
M
Roatsch
Martin L
ML
Schmitt
Luca
L
Carlino
Martin
M
Pippel
Wolfgang
W
Sippl
Manfred
M
Jung
D000595:Amino Acid Sequence; D000818:Animals; D019175:DNA Methylation / Q000187:drug effects; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D044127:Epigenesis, Genetic / Q000187:drug effects; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D006657:Histones / Q000235:genetics / Q000378:metabolism; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology* / Q000235:genetics / Q000378:metabolism
D004791:Enzyme Inhibitors; D006657:Histones; D056466:Histone Demethylases