Dehydrocurvularin is a potent antineoplastic agent irreversibly blocking ATP-citrate lyase: evidence from chemoproteomics

Natural-product macrolide 10,11-dehydrocurvularin ( DCV ) was revealed to be a potent irreversible inhibitor of ATP-citrate lyase (ACLY) via classical chemoproteomic profiling, which mechanistically illuminates the anti-cancer mode of action of DCV and its analogues. Dehydrocurvularin irreversibly i...

Full description

Saved in:
Bibliographic Details
Published inChemical communications (Cambridge, England) Vol. 55; no. 29; pp. 4194 - 4197
Main Authors Deng, Zhangshuang, Wong, Nai-Kei, Guo, Zhiyong, Zou, Kun, Xiao, Youli, Zhou, Yiqing
Format Journal Article
LanguageEnglish
Published England Royal Society of Chemistry 04.04.2019
Subjects
antineoplastic agents
Antineoplastic Agents - pharmacology
ATP Citrate (pro-S)-Lyase - antagonists & inhibitors
ATP Citrate (pro-S)-Lyase - metabolism
ATP citrate synthase
Cell Proliferation - drug effects
chemical reactions
dehydrocurvularin
Enzyme Inhibitors - pharmacology
HeLa Cells
Humans
mechanism of action
Proteomics
Zearalenone - analogs & derivatives
Zearalenone - pharmacology
Online AccessGet full text

Cover

More Information
Summary:Natural-product macrolide 10,11-dehydrocurvularin ( DCV ) was revealed to be a potent irreversible inhibitor of ATP-citrate lyase (ACLY) via classical chemoproteomic profiling, which mechanistically illuminates the anti-cancer mode of action of DCV and its analogues. Dehydrocurvularin irreversibly inhibits human ATP-citrate lyase.
Bibliography:10.1039/c9cc00256a
Electronic supplementary information (ESI) available. See DOI
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 14
content type line 23
ISSN:1359-7345
1364-548X
1364-548X
DOI:10.1039/c9cc00256a