Suppr超能文献

从血管紧张素AT1受体和多巴胺D2受体角度看G蛋白偶联受体中的寡聚化与协同性

Oligomerization and cooperativity in GPCRs from the perspective of the angiotensin AT1 and dopamine D2 receptors.

作者信息

Durdagi Serdar, Erol Ismail, Salmas Ramin Ekhteiari, Aksoydan Busecan, Kantarcioglu Isik

机构信息

Computational Biology and Molecular Simulations Laboratory, Department of Biophysics, School of Medicine, Bahcesehir University (BAU), Istanbul, Turkey; Neuroscience Program, Graduate School of Health Sciences, Bahcesehir University, Istanbul, Turkey.

Computational Biology and Molecular Simulations Laboratory, Department of Biophysics, School of Medicine, Bahcesehir University (BAU), Istanbul, Turkey; Department of Chemistry, Gebze Technical University, Kocaeli, Turkey.

出版信息

Neurosci Lett. 2019 May 1;700:30-37. doi: 10.1016/j.neulet.2018.04.028. Epub 2018 Apr 20.

Abstract

G Protein-Coupled Receptors (GPCRs) can form homo- and heterodimers or constitute higher oligomeric clusters with other heptahelical GPCRs. In this article, multiscale molecular modeling approaches as well as experimental techniques which are used to study oligomerization of GPCRs are reviewed. In particular, the effect of dimerization/oligomerization to the ligand binding affinity of individual protomers and also on the efficacy of the oligomer are discussed by including diverse examples from the literature. In addition, possible allosteric effects that may emerge upon interaction of GPCRs with membrane components, like cholesterol, is also discussed. Investigation of these above-mentioned interactions may greatly contribute to the candidate molecule screening studies and development of novel therapeutics with fewer adverse effects.

摘要

G蛋白偶联受体(GPCRs)可形成同二聚体和异二聚体,或与其他七螺旋GPCRs构成更高阶的寡聚簇。本文综述了用于研究GPCRs寡聚化的多尺度分子建模方法以及实验技术。特别地,通过纳入文献中的各种实例,讨论了二聚化/寡聚化对单个原聚体配体结合亲和力以及寡聚体功效的影响。此外,还讨论了GPCRs与膜成分(如胆固醇)相互作用时可能出现的变构效应。对上述相互作用的研究可能会极大地促进候选分子筛选研究以及开发副作用更少的新型疗法。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验