Epigenetics meets GPCR: inhibition of histone H3 methyltransferase (G9a) and histamine H₃ receptor for Prader-Willi Syndrome.

ABSTRACT: The role of epigenetic regulation is in large parts connected to cancer, but additionally, its therapeutic claim in neurological disorders has emerged. Inhibition of histone H3 lysine N-methyltransferase, especially G9a, has been recently shown to restore candidate genes from silenced parental chromosomes in the imprinting disorder Prader-Willi syndrome (PWS). In addition to this epigenetic approach, pitolisant as G-protein coupled histamine H₃ receptor (H₃R) antagonist has demonstrated promising therapeutic effects for Prader-Willi syndrome. To combine these pioneering principles of drug action, we aimed to identify compounds that combine both activities, guided by the pharmacophore blueprint for both targets. However, pitolisant as selective H₃R inverse a

SUBMITTER: Reiner D 

PROVIDER: S-EPMC7419559 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature