Now showing items 1-4 of 4
Design, synthesis and biological evaluation of new small-molecule modulators of proein lysine methyltransferases (PKMTs)
(Universita degli studi di Salerno, 2018-04-20)
Histone lysine methyltransferases have crucial roles in a number of biological processes and human diseases by controlling gene expression and chromatin state. Within this family, the lysine methyltransferase G9a has emerged ...
Design, synthesis, biological evaluation and binding studies of new small-molecule modulators of KDMs (lysine-specific demethylases)
(Universita degli studi di Salerno, 2017-03-27)
JHDMs (JmjC-domain-containing histone demethylases) are the largest class of demethylase enzymes, contain a Jumonji C (JmjC) domain and catalyze lysine demethylation of histones through an oxidative reaction that requires ...
Design, synthesis and biological evaluation of new non-nucleosidic inhibitors od DNA methyltransferases
(Universita degli studi di Salerno, 2013-04-03)
The inactivation of tumor suppressor genes, which often results from epigenetic silencing associated with DNA hypermethylation, plays a pivotal role in the development of most forms of human cancer. Moreover, there are ...
Biomolecular and biophysical approaches to interrogate epigenetic targets: a platform for drug discovery
(Universita degli studi di Salerno, 2016-04-20)
The term epigenetics refers to heritable changes in gene expression that do not involve changes in the DNA sequence. A large number of enzymes, which act mainly on histone tails and DNA, carries out epigenetic modifications, ...