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关于甘丙肽受体3突变体的数据集,这些突变体可改善重组受体在激动剂和拮抗剂结合形式下的表达和稳定性。

Dataset on Galanin Receptor 3 mutants that improve recombinant receptor expression and stability in an agonist and antagonist bound form.

作者信息

Ho Thao T, Nguyen Jasmine T, Liu Juping, Stanczak Pawel, Thompson Aaron A, Yan Yingzhuo G, Chen Jasmine, Allerston Charles K, Dillard Charles L, Xu Hao, Shoger Nicholas J, Cameron Jill S, Massari Mark E, Aertgeerts Kathleen

机构信息

Department of Structural Biology, Dart Neuroscience, 12278 Scripps Summit Drive, San Diego, CA 92131, USA.

Department of Preclinical Development, Dart Neuroscience, 12278 Scripps Summit Drive, San Diego, CA 92131, USA.

出版信息

Data Brief. 2017 May 4;12:603-607. doi: 10.1016/j.dib.2017.04.057. eCollection 2017 Jun.

Abstract

Galanin Receptor 3 (GALR3) is a G-protein-coupled receptor with a widespread distribution in the brain and plays a role in a variety of physiologic processes including cognition/memory, sensory/pain processing, hormone secretion, and feeding behavior. Therefore, GALR3 is considered an attractive CNS drug target (Freimann et al., 2015) [1]. This dataset contains GALR3 point mutants that improve recombinant protein expression and thermal stability of the receptor contained in virus-like particles (VLPs) or obtained by detergent-purification of baculovirus-infected insect cells. The mutations listed can be grouped in those that improve the stability of the agonist-bound and the antagonist-bound form of the receptor. Protein characteristics in terms of protein expression and thermal stability were comparable between GPCR-VLP and GPCR overexpressing Sf9 cultures. The further analysis and detailed results of these mutants as well as their impact on biophysical assay development for drug discovery can be found in "Method for Rapid Optimization of Recombinant GPCR Protein Expression and Stability using Virus-Like Particles" (Ho et al., 2017) [2].

摘要

甘丙肽受体3(GALR3)是一种G蛋白偶联受体,在大脑中广泛分布,在包括认知/记忆、感觉/疼痛处理、激素分泌和进食行为等多种生理过程中发挥作用。因此,GALR3被认为是一个有吸引力的中枢神经系统药物靶点(Freimann等人,2015年)[1]。该数据集包含GALR3点突变体,这些突变体可提高病毒样颗粒(VLP)中所含受体或通过去污剂纯化杆状病毒感染的昆虫细胞获得的受体的重组蛋白表达和热稳定性。列出的突变可分为提高受体激动剂结合形式和拮抗剂结合形式稳定性的突变。在GPCR-VLP和过表达GPCR的Sf9培养物之间,蛋白质表达和热稳定性方面的蛋白质特性具有可比性。这些突变体的进一步分析和详细结果以及它们对药物发现的生物物理测定开发的影响可在“使用病毒样颗粒快速优化重组GPCR蛋白表达和稳定性的方法”(Ho等人,2017年)[2]中找到。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73dd/5430141/43bfbfb61eec/gr1.jpg

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