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

Zhangshuang Deng; Nai-Kei Wong; Zhiyong Guo; Kun Zou; Youli Xiao; Yiqing Zhou

doi:10.1039/c9cc00256a

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

Chem Commun (Camb). 2019 Apr 4;55(29):4194-4197. doi: 10.1039/c9cc00256a.

Authors

Zhangshuang Deng¹, Nai-Kei Wong, Zhiyong Guo, Kun Zou, Youli Xiao, Yiqing Zhou

Affiliation

¹ School of Biotechnology and Food Engineering, Changshu Institute of Technology, Changshu, Jiangsu 215500, China. [email protected].

PMID: 30895984
DOI: 10.1039/c9cc00256a

Abstract

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.

MeSH terms

ATP Citrate (pro-S)-Lyase / antagonists & inhibitors*
ATP Citrate (pro-S)-Lyase / metabolism
Antineoplastic Agents / pharmacology*
Cell Proliferation / drug effects
Enzyme Inhibitors / pharmacology*
HeLa Cells
Humans
Proteomics*
Zearalenone / analogs & derivatives*
Zearalenone / pharmacology

Substances

Antineoplastic Agents
Enzyme Inhibitors
dehydrocurvularin
Zearalenone
ATP Citrate (pro-S)-Lyase