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Cyclopropanamine Compounds and Use Thereof

Author:
Blass, Benjamin  


Journal:
ACS MEDICINAL CHEMISTRY LETTERS


Issue Date:
2016


Abstract(summary):

Packaging of DNA into nucleosomes in eukaryotic cells is dependent upon the proper utilization of histones. These highly basic proteins are the primary component of chromatin, act as spool for DNA winding, and are regulated via methylation and demethylation processes. Lysine-specific demethylase 1 (LSD1) is an FAD dependent enzyme that demethylates mono- and dimethylated lysines in histone 3. Inhibition of this enzyme causes an increase in histone 3 methylation. Further, changes in methylation content of histone 3 have been linked to alterations in gene expression. LSD1 inhibitors are currently being examined as novel therapeutic agent for the treatment of a number of disease states including schizophrenia, Rett's syndrome, fragile X syndrome, Alzheimer's disease, epilepsy, and drug addiction. The present disclosure describes a series of functionalized cyclopropanamine inhibitors of LSD I and their method use in treating the aforementioned conditions.


Page:
10---11


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