P2Y受体亚型的药理学表征 - 一个更新
1Department of Pharmacology and Toxicology, Pharma Center, University of Bonn, D-53127, Bonn, Germany. kugelgen@uni-bonn.de.
药理学工具有助于识别参与生理和病理过程的P2Y受体亚型. 本综述详细介绍了P2Y1,P2Y2,P2Y4,P2Y6,P2Y11,P2Y12,P2Y13和P2Y14受体的选择性对抗剂.
科学领域:
- 药理学 药理学是指药理学的学科.
- 分子生物学分子生物学
- 生物化学 生物化学
背景情况:
- P2Y受体是G蛋白合受体 (GPCRs),由细胞外核酸激活.
- 哺乳动物P2Y受体的八个亚型 (P2Y1,P2Y2,P2Y4,P2Y6,P2Y11,P2Y12,P2Y13和P2Y14) 被广泛表达,并在生理学和病理生理学中发挥关键作用.
研究的目的:
- 本综述旨在总结使用药理工具来表征参与各种生物反应的P2Y受体亚型的药理工具.
- 提供对选择性抗剂及其在研究P2Y受体功能中的应用的概述.
主要方法:
- 对使用药理学药物来研究P2Y受体亚型的研究的文献综述.
- 对每个P2Y受体亚型的选择性抗剂的鉴定和分类.
主要成果:
- 对于各种P2Y受体,已确定了特定的抗剂:MRS2500 (P2Y1),AR-C118925 (P2Y2),PSB16133 (P2Y4),MRS2578 (P2Y6),NF157/NF340 (P2Y11),PSB0739 (P2Y12),MRS2211/MRS2603 (P2Y13),以及PPTN (P2Y14),这些都是P2Y受体中的一种.
- P2Y1和P2Y12受体调解ADP诱导的血小板聚合,其中包括克洛皮多格雷尔,普拉苏格雷尔,蒂卡格雷尔和坎格雷尔等多种化合物作为P2Y12对手.
结论:
- 药理学工具对于剖析单个P2Y受体亚型在生物系统中的作用至关重要.
- 选择性抗剂的可用性促进了对P2Y受体介导的信号通路和治疗标识的进一步研究.
更多相关视频
11:47Real-time Live-cell Flow Cytometry to Investigate Calcium Influx, Pore Formation, and Phagocytosis by P2X7 Receptors in Adult Neural Progenitor Cells
Published on: April 3, 2019
08:33Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time
Published on: March 11, 2021
相关概念视频
Adrenergic Receptors: ɑ Subtype
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical,...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline...
