DICP OpenIR
Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products
Xu, Fangfang1,2; Zhou, Han1; Liu, Xiumei1; Zhang, Xiuli1,3; Wang, Zhiwei4; Hou, Tao1; Wang, Jixia1; Qu, Lala1,2; Zhang, Pengyu5; Piao, Hailong1; Liang, Xinmiao1,3
Corresponding AuthorZhang, Xiuli(zhangxiuli@dicp.ac.cn) ; Liang, Xinmiao()
Source PublicationRSC ADVANCES
2019
ISSN2046-2069
DOI10.1039/c9ra02142f
Volume9Issue:26Pages:15073-15083
Funding ProjectState Key Program of National Natural Science of China[U1508221] ; National Science Foundation of China[81403100] ; DICP, CAS[DICP TMSR201601] ; DICP, CAS[ZZBS201803]
Funding OrganizationState 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
WOS SubjectChemistry, Multidisciplinary
WOS Research AreaChemistry
WOS KeywordDIETARY FATTY-ACIDS ; INSULIN-SECRETION ; RECEPTOR ; GPR120 ; POTENT ; IDENTIFICATION ; TAK-875 ; PHARMACOLOGY ; FFA4/GPR120 ; DRUGS
AbstractIn 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.
Language英语
Funding OrganizationState 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
WOS IDWOS:000468641300057
PublisherROYAL SOC CHEMISTRY
Citation statistics
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/172106
Collection中国科学院大连化学物理研究所
Corresponding AuthorZhang, Xiuli; Liang, Xinmiao
Affiliation1.Chinese Acad Sci, Dalian Inst Chem Phys, Key Lab Separat Sci Analyt Chem, Dalian 116023, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Nantong Univ, Coinnovat Ctr Neuroregenerat, Nantong 226019, Peoples R China
4.DICP CMC Innovat Inst Med, Taizhou 225300, Peoples R China
5.Dalian Med Univ, Liaoning Prov Core Lab Med Mol Biol, Dalian 116044, Peoples R China
Recommended Citation
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.
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