Pregled bibliografske jedinice broj: 1083548
Rational design, synthesis and biological profiling of new KDM4C inhibitors
Rational design, synthesis and biological profiling of new KDM4C inhibitors // Bioorganic & medicinal chemistry, 28 (2020), 115128, 13 doi:10.1016/j.bmc.2019.115128 (međunarodna recenzija, članak, znanstveni)
CROSBI ID: 1083548 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Rational design, synthesis and biological profiling of new KDM4C
inhibitors
Autori
Letfus, Vatroslav ; Jelić, Dubravko ; Bokulić, Ana ; Petrinić Grba Adriana ; Koštrun, Sanja
Izvornik
Bioorganic & medicinal chemistry (0968-0896) 28
(2020);
115128, 13
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni
Ključne riječi
Epigenetics, KDM4C enzyme, Inhibitor, Drug design, Computational chemistry
Sažetak
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.
Izvorni jezik
Engleski
Citiraj ovu publikaciju:
Časopis indeksira:
- Current Contents Connect (CCC)
- Web of Science Core Collection (WoSCC)
- Science Citation Index Expanded (SCI-EXP)
- SCI-EXP, SSCI i/ili A&HCI
- Scopus
- MEDLINE
