Institute of Pharmaceutical Sciences, Albert-Ludwigs-University of Freiburg, Albertstr. 25, 79104 Freiburg, Germany.
Mol Oncol. 2012 Dec;6(6):683-703. doi: 10.1016/j.molonc.2012.07.004. Epub 2012 Aug 7.
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.
近年来,可逆组蛋白甲基化已成为表观遗传调控的一个重要机制。组蛋白甲基转移酶和去甲基化酶已被确定为多种疾病(尤其是癌症)发展的促成因素。因此,它们被认为是具有高治疗潜力的新型药物靶点。在这里,我们重点介绍组蛋白去甲基酶,并特别探讨它们在肿瘤药物发现中的潜在作用。我们概述了不同类别的酶、它们的生物化学特性、在生理学中的作用以及已有的抑制剂方面的相关数据。