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Rational design, synthesis and biological profiling of new KDM4C inhibitors (CROSBI ID 283979)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

Letfus, Vatroslav ; Jelić, Dubravko ; Bokulić, Ana ; Petrinić Grba Adriana ; Koštrun, Sanja Rational design, synthesis and biological profiling of new KDM4C inhibitors // Bioorganic & medicinal chemistry, 28 (2020), 115128, 13. doi: 10.1016/j.bmc.2019.115128

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

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Podaci o izdanju

28

2020.

115128

13

objavljeno

0968-0896

1464-3391

10.1016/j.bmc.2019.115128

Povezanost rada

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Poveznice
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