Naphthoquinone-mediated Inhibition of Lysine Acetyltransferase KAT3B/p300, Basis for Non-toxic Inhibitor Synthesis

Hydroxynaphthoquinone-based inhibitors of the lysine acetyltransferase KAT3B (p300), such as plumbagin, are relatively toxic. Here, we report that free thiol reactivity and redox cycling properties greatly contribute to the toxicity of plumbagin. A reactive 3rd position in the naphthoquinone derivat...

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Autori principali: Vasudevarao, Mohankrishna Dalvoy, Mizar, Pushpak, Kumari, Sujata, Mandal, Somnath, Siddhanta, Soumik, Swamy, Mahadeva MM, Kaypee, Stephanie, Kodihalli, Ravindra C, Banerjee, Amrita, Naryana, Chandrabhas, Dasgupta, Dipak, Kundu, Tapas K.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Society for Biochemistry and Molecular Biology 2014
Soggetti:
Enzymology
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC3953281/
https://ncbi.nlm.nih.gov/pubmed/24469461
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.M113.486522
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