2013-10-29 12:00:57 - Histone methyltransferases are promising epigenetic drug targets. Several drugs that inhibit histone methyltransferases have been developed for anticancer therapy.
DOT1L histone H3 methyltransferase is an evolutionarily conserved enzyme involved in the regulation of heterochromatin structure through methylation of histone H3 lysine 79 (H3K79). Mammalian DOT1L participates in the regulation of transcription, development, erythropoiesis, differentiation, and proliferation of normal cells. It was also shown that DOT1L plays an essential role in the development of several malignancies. DOT1L has been found to be a drug target of mixed lineage leukemia (MLL) gene translocated acute leukemia. Therefore, inhibitors of DOT1L could be used for anticancer therapy. Very potent and selective inhibitors of DOT1L have been identified. Several of these compounds were found to have antileukemic activity in cell-based assays and in animal models, with the most advanced compound being in clinical trials.
Ltd. has developed new DOT1L Targeted Library containing 1,625 compounds. The DOT1L Focused Library has been designed with receptor-based approach that included docking of Drug-like Green Collection in the active site of human DOT1L (PDB ID: 4EQZ) and filtering by score values and hydrogen bonds formed between ligand and key residues of the DOT1L active site. The library comprises drug-like compounds only.
More information about this library you can find at the web-site: www.otavachemicals.com.