Computer- and structure-based lead design for epigenetic targets |
| |
Authors: | Heinke Ralf Carlino Luca Kannan Srinivasaraghavan Jung Manfred Sippl Wolfgang |
| |
Affiliation: | Department of Pharmaceutical Chemistry, Martin-Luther University of Halle-Wittenberg, 06120 Halle/Saale, Germany. |
| |
Abstract: | The term epigenetics is defined as inheritable changes that influence the outcome of a phenotype without changes in the genome. Epigenetics is based upon DNA methylation and posttranslational histone modifications. While there is much known about reversible acetylation as a posttranslational modification, research on reversible histone methylation is still emerging, especially with regard to drug discovery. As aberrant epigenetic modifications have been linked to many diseases, inhibitors of histone modifying enzymes are very much in demand. This article will summarize the progress on small molecule epigenetic inhibitors identified by structure- and computer-based approaches. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|