Discovery and characterization of novel ATP citrate lyase inhibitors from natural products by a luminescence-based assay

Autor:	Pan Wang, Xingrong Peng, Tao Hou, Fangfang Xu, Han Zhou, Yancheng Yu, Minghua Qiu, Yanfang Liu, Yaopeng Zhao, Zhimou Guo, Jixia Wang, Xinmiao Liang
Rok vydání:	2022
Předmět:	Adenosine Diphosphate Biological Products Luminescence ATP Citrate (pro-S)-Lyase Coenzyme A Serum Albumin Bovine General Medicine Toxicology
Zdroj:	Chemico-biological interactions. 367
ISSN:	1872-7786
Popis:	ATP citrate lyase (ACLY) is a key enzyme in glucolipid metabolism with therapeutic prospect for treating hyperlipidemia and various cancers. Much effort has been put into discovering ACLY inhibitors. However, current screening approaches have limitations in sensitivity, portability and high-throughput. To develop a general screening assay, we investigated series of conditions affecting the enzymatic reaction based on the ADP-Glo luminescence assay. Bovine serum albumin (0.001%) added triggered strong and stable fluorescence signal. The optimized assay was validated and applied to screen our natural product library. Two novel inhibitors were identified with IC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6957e472ec3d7a5bde5e4fc4c40bdea0 https://pubmed.ncbi.nlm.nih.gov/36174740 Zobrazit plný text záznamu Full Text from ScienceDirect