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β2 肾上腺素能受体β-arrestin2 募集:一种适应于药理学本科培训的荧光素酶互补测定法。

β-arrestin2 recruitment at the β2 adrenergic receptor: A luciferase complementation assay adapted for undergraduate training in pharmacology.

机构信息

Neuropharmacology Laboratory, Institute of Neuroscience, UCLouvain, Brussels, Belgium.

Faculty of Pharmacy and Biomedical Sciences, UCLouvain, Brussels, Belgium.

出版信息

Pharmacol Res Perspect. 2021 Feb;9(1):e00706. doi: 10.1002/prp2.706.

DOI:10.1002/prp2.706
PMID:33508174
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7842874/
Abstract

In the context of pharmacology teaching, hands-on activities constitute an essential complement to theoretical lectures. Frequently, these activities consist in exposing fresh animal tissues or even living animals to selected drugs and qualitatively or quantitatively evaluating functional responses. However, technological advancements in pharmacological research and the growing concerns for animal experimentation support the need for innovative and flexible in vitro assays adapted for teaching purposes. We herein report the implementation of a luciferase complementation assay (LCA) enabling to dynamically monitor β-arrestin2 recruitment at the β adrenergic receptor in the framework of pharmacological training at the faculty of Pharmacy and Biomedical Sciences. The assay allowed students to quantitatively characterize the competitive antagonism of propranolol, and to calculate pEC , pK , and pA values after a guided data analysis session. Moreover, the newly implemented workshop delivered highly reproducible results and were generally appreciated by students. As such, we report that the luciferase complementation-based assay proved to be a straightforward, robust, and cost-effective alternative to experiments performed on animal tissues, constituting a useful and flexible tool to enhance and update current hands-on training in the context of pharmacological teaching.

摘要

在药理学教学中,实践活动是理论讲座的重要补充。这些活动通常包括将新鲜的动物组织甚至活体动物暴露于选定的药物中,并定性或定量地评估功能反应。然而,药理学研究的技术进步和对动物实验的日益关注支持了创新和灵活的体外检测的需求,这些检测适用于教学目的。我们在此报告了一种荧光素酶互补测定法(LCA)的实施,该方法能够在药学院和生物医学科学系的药理学培训框架内动态监测β肾上腺素能受体的β-arrestin2 募集。该测定法允许学生定量表征普萘洛尔的竞争性拮抗作用,并在经过引导的数据分析会议后计算 pEC 、pK 和 pA 值。此外,新实施的研讨会提供了高度可重复的结果,并受到学生的普遍赞赏。因此,我们报告说,基于荧光素酶互补的测定法是一种简单、稳健且具有成本效益的替代动物组织实验的方法,是增强和更新药理学教学中当前实践培训的有用且灵活的工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/69d82abe0aa9/PRP2-9-e00706-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/dfbd0510425f/PRP2-9-e00706-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/2fc37620659b/PRP2-9-e00706-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/2138920710de/PRP2-9-e00706-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/ecb3f2083df7/PRP2-9-e00706-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/69d82abe0aa9/PRP2-9-e00706-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/dfbd0510425f/PRP2-9-e00706-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/2fc37620659b/PRP2-9-e00706-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/2138920710de/PRP2-9-e00706-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/ecb3f2083df7/PRP2-9-e00706-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cff0/7842874/69d82abe0aa9/PRP2-9-e00706-g005.jpg

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本文引用的文献

1
THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors.2019/20 年药理学简明指南:G 蛋白偶联受体。
Br J Pharmacol. 2019 Dec;176 Suppl 1(Suppl 1):S21-S141. doi: 10.1111/bph.14748.
2
Bioluminescence resonance energy transfer-based biosensors allow monitoring of ligand- and transducer-mediated GPCR conformational changes.基于生物发光共振能量转移的生物传感器可用于监测配体和转导介导的G蛋白偶联受体(GPCR)构象变化。
Commun Biol. 2018 Aug 7;1:106. doi: 10.1038/s42003-018-0101-z. eCollection 2018.
3
Pharmacology education: Reflections and challenges.
药理学教育:反思与挑战。
Eur J Pharmacol. 2018 Aug 15;833:392-395. doi: 10.1016/j.ejphar.2018.06.032. Epub 2018 Jun 20.
4
The IUPHAR/BPS Guide to PHARMACOLOGY in 2018: updates and expansion to encompass the new guide to IMMUNOPHARMACOLOGY.2018 年 IUPHAR/BPS 药理学指南:更新和扩展,以包含新的免疫药理学指南。
Nucleic Acids Res. 2018 Jan 4;46(D1):D1091-D1106. doi: 10.1093/nar/gkx1121.
5
Activation of the Orphan G Protein-Coupled Receptor GPR27 by Surrogate Ligands Promotes -Arrestin 2 Recruitment.替代配体激活孤儿G蛋白偶联受体GPR27可促进β-抑制蛋白2的募集。
Mol Pharmacol. 2017 Jun;91(6):595-608. doi: 10.1124/mol.116.107714. Epub 2017 Mar 17.
6
High-throughput live cell imaging and analysis for temporal reaction of G protein-coupled receptor based on split luciferase fragment complementation.基于分裂荧光素酶片段互补的G蛋白偶联受体时间反应的高通量活细胞成像与分析
Anal Sci. 2015;31(4):327-30. doi: 10.2116/analsci.31.327.
7
A review of computer assisted learning in medical undergraduates.医学本科生计算机辅助学习综述。
J Pharmacol Pharmacother. 2013 Apr;4(2):86-90. doi: 10.4103/0976-500X.110870.
8
Visualization and quantitative analysis of G protein-coupled receptor-β-arrestin interaction in single cells and specific organs of living mice using split luciferase complementation.使用荧光素酶互补技术在活鼠的单细胞和特定器官中可视化和定量分析 G 蛋白偶联受体-β-arrestin 相互作用。
ACS Chem Biol. 2012 May 18;7(5):901-10. doi: 10.1021/cb200360z. Epub 2012 Mar 12.
9
Principles of early drug discovery.早期药物发现的原则。
Br J Pharmacol. 2011 Mar;162(6):1239-49. doi: 10.1111/j.1476-5381.2010.01127.x.
10
The impact of introducing computer-based alternatives to the use of animals in the teaching of physiology and pharmacology at Balkan universities - a pilot study.在巴尔干地区的大学中,引入基于计算机的替代方法来替代动物在生理学和药理学教学中的应用的影响——一项试点研究。
Altern Lab Anim. 2009 Nov;37(5):547-56. doi: 10.1177/026119290903700511.