Update of P2Y receptor pharmacology: IUPHAR Review 27

doi:10.1111/bph.1500510.1111/bph.15005

	Update of P2Y receptor pharmacology: IUPHAR Review 27
	Jacobson, Kenneth A.2; Delicado, Esmerilda G.3; Gachet, Christian 4; Kennedy, Charles 5; von Kuegelgen, Ivar 6; Li, Beibei 7; Miras-Portugal, M. Teresa 3; Novak, Ivana 8; Schoeneberg, Torsten 9; Perez-Sen, Raquel 3
刊名	BRITISH JOURNAL OF PHARMACOLOGY
	2020-06-01
卷号	177 期号:11 页码:2413-2433
ISSN号	0007-1188
DOI	10.1111/bph.1500510.1111/bph.15005
通讯作者	Jacobson, Kenneth A.(kennethj@niddk.nih.gov)
英文摘要	Eight G protein-coupled P2Y receptor subtypes respond to extracellular adenine and uracil mononucleotides and dinucleotides. P2Y receptors belong to the delta group of rhodopsin-like GPCRs and contain two structurally distinct subfamilies: P2Y(1), P2Y(2), P2Y(4), P2Y(6), and P2Y(11) (principally G(q) protein-coupled P2Y(1)-like) and P2Y(12-14) (principally G(i) protein-coupled P2Y(12)-like) receptors. Brain P2Y receptors occur in neurons, glial cells, and vasculature. Endothelial P2Y(1), P2Y(2), P2Y(4), and P2Y(6) receptors induce vasodilation, while smooth muscle P2Y(2), P2Y(4), and P2Y(6) receptor activation leads to vasoconstriction. Pancreatic P2Y(1) and P2Y(6) receptors stimulate while P2Y(13) receptors inhibits insulin secretion. Antagonists of P2Y(12) receptors, and potentially P2Y(1) receptors, are anti-thrombotic agents, and a P2Y(2)/P2Y(4) receptor agonist treats dry eye syndrome in Asia. P2Y receptor agonists are generally pro-inflammatory, and antagonists may eventually treat inflammatory conditions. This article reviews recent developments in P2Y receptor pharmacology (using synthetic agonists and antagonists), structure and biophysical properties (using X-ray crystallography, mutagenesis and modelling), physiological and pathophysiological roles, and present and potentially future therapeutic targeting.
资助项目	NIDDK[ZIADK31116] ; Independent Research Fund Denmark[DFF-4002-00162] ; State of Saxony, Germany ; Integrated Research and Treatment Center (IFB) AdiposityDiseases (BMBF) ; German Research Foundation[FOR2372] ; German Research Foundation[GRK1873] ; German Research Foundation[SFB 1052]
WOS关键词	SMOOTH-MUSCLE-CELLS ; P2Y(12) RECEPTOR ; NUCLEOTIDE RECEPTORS ; CONCISE GUIDE ; ACTIVE METABOLITE ; PURINERGIC REGULATION ; SELECTIVE AGONISTS ; EXTRACELLULAR ATP ; PLATELET P2Y(1) ; ANTAGONIST
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	WILEY
WOS记录号	WOS:000530811400001
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/280070]
专题	中国科学院上海药物研究所
通讯作者	Jacobson, Kenneth A.
作者单位	1.Univ Leipzig, IFB AdiposityDis, Med Ctr, Leipzig, Germany 2.NIDDK, Lab Bioorgan Chem, NIH, 9000 Rockville Pike, Bethesda, MD 20892 USA 3.Univ Complutense Madrid, Dept Bioquim & Biol Mol, Madrid, Spain 4.Univ Strasbourg, INSERM, EFS Grand Est, BPPS,UMR S 1255,FMTS, Strasbourg, France 5.Univ Strathclyde, Strathclyde Inst Pharm & Biomed Sci, Glasgow, Lanark, Scotland 6.Univ Bonn, Dept Pharmacol & Toxicol, Biomed Res Ctr, Bonn, Germany 7.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai, Peoples R China 8.Univ Copenhagen, Sect Cell Biol & Physiol, Dept Biol, Copenhagen, Denmark 9.Univ Leipzig, Rudolf Schonheimer Inst Biochem, Med Fac, Mol Biochem, Leipzig, Germany 10.Univ Bonn, Pharmaceut Inst, Dept Pharmaceut & Med Chem, Bonn, Germany
推荐引用方式 GB/T 7714	Jacobson, Kenneth A.,Delicado, Esmerilda G.,Gachet, Christian,et al. Update of P2Y receptor pharmacology: IUPHAR Review 27[J]. BRITISH JOURNAL OF PHARMACOLOGY,2020,177(11):2413-2433.
APA	Jacobson, Kenneth A..,Delicado, Esmerilda G..,Gachet, Christian.,Kennedy, Charles.,von Kuegelgen, Ivar.,...&Mueller, Christa E..(2020).Update of P2Y receptor pharmacology: IUPHAR Review 27.BRITISH JOURNAL OF PHARMACOLOGY,177(11),2413-2433.
MLA	Jacobson, Kenneth A.,et al."Update of P2Y receptor pharmacology: IUPHAR Review 27".BRITISH JOURNAL OF PHARMACOLOGY 177.11(2020):2413-2433.