中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 大连化学物理研究所
  3. 中国科学院大连化学物理研究所
Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products

文献类型：期刊论文

作者Xu, Fangfang3,4; Zhou, Han3; Liu, Xiumei3; Zhang, Xiuli1,3; Wang, Zhiwei5; Hou, Tao3; Wang, Jixia3; Qu, Lala3,4; Zhang, Pengyu2; Piao, Hailong3
刊名RSC ADVANCES
出版日期2019
卷号9期号:26页码:15073-15083
ISSN号2046-2069
DOI10.1039/c9ra02142f
通讯作者Zhang, Xiuli(zhangxiuli@dicp.ac.cn) ; Liang, Xinmiao()
英文摘要In this article, pharmacological studies of the free fatty acid receptor (FFA) 4 and FFA1 were conducted in transfected CHO cells (FFA4&FFA1) and HT29 cells with application of a label-free dynamic mass redistribution (DMR) assay. Commercially available compounds including -linolenic acid (ALA), GW9508, TUG891, GSK137647A, TAK875, MEDICA16, AH7614 and GW1100, were used to validate the assay; real-time tracing of ligand-induced cell responses elucidated pharmacological properties of ligand-receptor interactions. A pool of 140 natural compounds was screened using the CHO-FFA4 cells. Three new FFA4 agonists with novel skeletons were discovered and they were dihydrotanshinone, emodin and acetylshikonin (EC50 values were 32.88, 38.18 and 10.17 M, respectively). Ligand selectivity was compared between FFA4 and FFA1; dihydrotanshinone and emodin displayed FFA4 selectivity, while acetylshikonin shared FFA1 and FFA4 agonist activities with EC50 values comparable to the endogenous ligand ALA. The three novel FFA4 agonists provide a promising chemical starting point for identification and optimization of drugs used for treating metabolic and inflammatory diseases. Besides, this work will help to explain the mechanism of actions of natural products.
WOS关键词DIETARY FATTY-ACIDS ; INSULIN-SECRETION ; RECEPTOR ; GPR120 ; POTENT ; IDENTIFICATION ; TAK-875 ; PHARMACOLOGY ; FFA4/GPR120 ; DRUGS
资助项目State Key Program of National Natural Science of China[U1508221] ; National Science Foundation of China[81403100] ; DICP, CAS[DICP TMSR201601] ; DICP, CAS[ZZBS201803]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000468641300057
出版者ROYAL SOC CHEMISTRY
资助机构State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; National Science Foundation of China ; National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; National Science Foundation of China ; National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; National Science Foundation of China ; National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; National Science Foundation of China ; National Science Foundation of China ; DICP, CAS ; DICP, CAS
源URL[http://cas-ir.dicp.ac.cn/handle/321008/172105]  
专题大连化学物理研究所_中国科学院大连化学物理研究所
通讯作者Zhang, Xiuli; Liang, Xinmiao
作者单位1.Nantong Univ, Coinnovat Ctr Neuroregenerat, Nantong 226019, Peoples R China
2.Dalian Med Univ, Liaoning Prov Core Lab Med Mol Biol, Dalian 116044, Peoples R China
3.Chinese Acad Sci, Dalian Inst Chem Phys, Key Lab Separat Sci Analyt Chem, Dalian 116023, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
5.DICP CMC Innovat Inst Med, Taizhou 225300, Peoples R China
推荐引用方式
GB/T 7714		 Xu, Fangfang,Zhou, Han,Liu, Xiumei,et al. Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products[J]. RSC ADVANCES,2019,9(26):15073-15083.
APA Xu, Fangfang.,Zhou, Han.,Liu, Xiumei.,Zhang, Xiuli.,Wang, Zhiwei.,...&Liang, Xinmiao.(2019).Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products.RSC ADVANCES,9(26),15073-15083.
MLA Xu, Fangfang,et al."Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products".RSC ADVANCES 9.26(2019):15073-15083.

入库方式： OAI收割

来源：大连化学物理研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。