Rediocide A, an Insecticide, Induces G-Protein-Coupled Receptor Desensitization via Activation of Conventional Protein Kinase C

doi:10.1021/np3000359

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	Rediocide A, an Insecticide, Induces G-Protein-Coupled Receptor Desensitization via Activation of Conventional Protein Kinase C
	Cui, Lixin; Li, Jing; Xie, Xin
刊名	JOURNAL OF NATURAL PRODUCTS
	2012-06
卷号	75 期号:6 页码:1058-1062
ISSN号	0163-3864
DOI	10.1021/np3000359
文献子类	Article
英文摘要	In order to identify small-molecule antagonists of Methuselah (Mth), a Drosophila G-protein-coupled receptor (GPCR) involved in life-span control, a library of natural compounds was screened, and it was found that rediocide A (1), a daphnane ester from the roots of Trigonostemon reidioides and used currently for flea control, potently inhibited calcium mobilization mediated by this receptor. Compound 1 inhibited calcium mobilization in GPCRs other than Mth, indicating that the inhibitory effect was not due to receptor antagonism but rather to a more general mechanism. It was found that 1 can induce GPCR desensitization and internalization, and such effects were mediated by the activation of conventional protein kinase C.
资助项目	Ministry of Science and Technology of China[2009CB940900] ; Ministry of Science and Technology of China[2009ZX09302-001] ; Chinese Academy of Sciences[XDA01040301] ; National Natural Sciences Foundation of China[81100963] ; Shanghai Commission of Science and Technology[11DZ2292200]
WOS关键词	TRIGONOSTEMON-REIDIOIDES ; LIFE-SPAN ; DOWN-REGULATION ; DROSOPHILA ; PHOSPHORYLATION ; TRAFFICKING ; MECHANISMS ; METHUSELAH ; DAPHNANE ; GENOME
WOS研究方向	Plant Sciences ; Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000305503500008
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278055]
专题	国家新药筛选中心中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Xie, Xin
作者单位	Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Cui, Lixin,Li, Jing,Xie, Xin. Rediocide A, an Insecticide, Induces G-Protein-Coupled Receptor Desensitization via Activation of Conventional Protein Kinase C[J]. JOURNAL OF NATURAL PRODUCTS,2012,75(6):1058-1062.
APA	Cui, Lixin,Li, Jing,&Xie, Xin.(2012).Rediocide A, an Insecticide, Induces G-Protein-Coupled Receptor Desensitization via Activation of Conventional Protein Kinase C.JOURNAL OF NATURAL PRODUCTS,75(6),1058-1062.
MLA	Cui, Lixin,et al."Rediocide A, an Insecticide, Induces G-Protein-Coupled Receptor Desensitization via Activation of Conventional Protein Kinase C".JOURNAL OF NATURAL PRODUCTS 75.6(2012):1058-1062.