Rational design, synthesis and biological profiling of new KDM4C inhibitors (CROSBI ID 283979)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Letfus, Vatroslav ; Jelić, Dubravko ; Bokulić, Ana ; Petrinić Grba Adriana ; Koštrun, Sanja
engleski
Rational design, synthesis and biological profiling of new KDM4C inhibitors
The human histone demethylases of the KDM4 family have been related to diseases such as prostate and breast cancer. Majority of currently known inhibitors suffer from the low permeability and low selectivity between the enzyme isoforms. In this study, toxoflavin motif was used to design and synthesize new KDM4C inhibitors with improved biological activity and in vitro ADME properties. Inhibitors displayed good passive cellular perme- ability and metabolic stability. However, diminishing of redox liability and consequently non-specific influence on cell viability still remains a challenge.
Epigenetics, KDM4C enzyme, Inhibitor, Drug design, Computational chemistry
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
Podaci o izdanju
28
2020.
115128
13
objavljeno
0968-0896
1464-3391
10.1016/j.bmc.2019.115128