• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

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

Agonist-receptor efficacy. II. Agonist trafficking of receptor signals.

作者信息

Kenakin T

机构信息

Department of Cellular Biochemistry, Glaxo Research Institute, Research Triangle Park, NC 27709, USA.

出版信息

Trends Pharmacol Sci. 1995 Jul;16(7):232-8. doi: 10.1016/s0165-6147(00)89032-x.

DOI:10.1016/s0165-6147(00)89032-x
PMID:7667897
Abstract

There is evidence to suggest that receptors with seven transmembrane domains can exist in G protein-activating conformations. It is not known how many activated receptor forms exist for each receptor. Furthermore, if there are multiple forms, does the chemical structure of the agonist determine which form dominates, and therefore, which response pathway is activated? This latter scheme is referred to as agonist-receptor trafficking, and is discussed in this, the second of two articles by Terry Kenakin. One way to approach these questions is to study receptors that couple to more than one G protein and, in essence, to try to allow the G protein to indicate the receptor state.

摘要

相似文献

1
Agonist-receptor efficacy. II. Agonist trafficking of receptor signals.
Trends Pharmacol Sci. 1995 Jul;16(7):232-8. doi: 10.1016/s0165-6147(00)89032-x.
2
G-protein coupled receptors: conformations and states.G蛋白偶联受体:构象与状态
Biochem Pharmacol. 1999 Oct 1;58(7):1081-8. doi: 10.1016/s0006-2952(99)00144-6.
3
Modelling of signalling via G-protein coupled receptors: pathway-dependent agonist potency and efficacy.G蛋白偶联受体信号转导的建模:依赖途径的激动剂效力和效能
Bull Math Biol. 2003 Sep;65(5):933-58. doi: 10.1016/S0092-8240(03)00055-7.
4
Agonist induction and conformational selection during activation of a G-protein-coupled receptor.G蛋白偶联受体激活过程中的激动剂诱导与构象选择
Trends Pharmacol Sci. 2003 Feb;24(2):81-6. doi: 10.1016/S0165-6147(02)00050-0.
5
Functional differences between full and partial agonists: evidence for ligand-specific receptor conformations.完全激动剂与部分激动剂之间的功能差异:配体特异性受体构象的证据
J Pharmacol Exp Ther. 2001 Jun;297(3):1218-26.
6
Morphological and biochemical strategies for monitoring trafficking of epitope-tagged G protein-coupled receptors in agonist-naive and agonist-occupied states.
Methods Enzymol. 2002;343:530-44. doi: 10.1016/s0076-6879(02)43156-4.
7
Role of endocytosis in signalling and regulation of G-protein-coupled receptors.内吞作用在G蛋白偶联受体信号传导及调控中的作用
Biochem Soc Trans. 2001 Aug;29(Pt 4):500-4. doi: 10.1042/bst0290500.
8
A three-state receptor model: predictions of multiple agonist pharmacology for the same receptor type.一种三态受体模型:对同一受体类型多种激动剂药理学的预测。
Ann N Y Acad Sci. 1998 Dec 15;861:97-103. doi: 10.1111/j.1749-6632.1998.tb10179.x.
9
Diversity and selectivity of receptor-G protein interaction.受体-G蛋白相互作用的多样性和选择性。
Annu Rev Pharmacol Toxicol. 1996;36:429-59. doi: 10.1146/annurev.pa.36.040196.002241.
10
A higher plant seven-transmembrane receptor that influences sensitivity to cytokinins.一种影响对细胞分裂素敏感性的高等植物七跨膜受体。
Curr Biol. 1998 Mar 12;8(6):315-24. doi: 10.1016/s0960-9822(98)70131-9.

引用本文的文献

1
Molecular Pathways Potentially Involved in Hallucinatory Experiences During Sleep Paralysis: The Emerging Role of β-Arrestin-2.睡眠麻痹期间幻觉体验可能涉及的分子途径:β-抑制蛋白2的新作用。
Int J Mol Sci. 2025 Jul 26;26(15):7233. doi: 10.3390/ijms26157233.
2
Lysophospholipid stereoisomers exert distinct GPR55-mediated functions via different Gα subunits.溶血磷脂立体异构体通过不同的Gα亚基发挥独特的GPR55介导的功能。
J Biol Chem. 2025 May 30;301(7):110324. doi: 10.1016/j.jbc.2025.110324.
3
Biased Opioid Receptor Agonists: Balancing Analgesic Efficacy and Side-Effect Profiles.
偏向性阿片受体激动剂:平衡镇痛疗效与副作用特征
Int J Mol Sci. 2025 Feb 21;26(5):1862. doi: 10.3390/ijms26051862.
4
Ligand-Induced Biased Activation of GPCRs: Recent Advances and New Directions from In Silico Approaches.G蛋白偶联受体的配体诱导偏向性激活:计算机模拟方法的最新进展与新方向
Molecules. 2025 Feb 25;30(5):1047. doi: 10.3390/molecules30051047.
5
Molecular Glues: A New Approach to Modulating GPCR Signaling Bias.分子胶:调节G蛋白偶联受体信号偏向性的新方法。
Biochemistry. 2025 Feb 18;64(4):749-759. doi: 10.1021/acs.biochem.4c00734. Epub 2025 Feb 3.
6
A narrative review of chemokine receptors CXCR1 and CXCR2 and their role in acute respiratory distress syndrome.趋化因子受体 CXCR1 和 CXCR2 的综述及其在急性呼吸窘迫综合征中的作用。
Eur Respir Rev. 2024 Jul 24;33(173). doi: 10.1183/16000617.0172-2023. Print 2024 Jul.
7
Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition.了解你的分子:候选药物的药理学特征,以提高疗效并减少后期损耗。
Nat Rev Drug Discov. 2024 Aug;23(8):626-644. doi: 10.1038/s41573-024-00958-9. Epub 2024 Jun 18.
8
Quantitative receptor model for responses that are left- or right-shifted versus occupancy (are more or less concentration sensitive): the SABRE approach.针对左移或右移反应与占有率(浓度敏感性或多或少)的定量受体模型:SABRE方法。
Front Pharmacol. 2023 Dec 15;14:1274065. doi: 10.3389/fphar.2023.1274065. eCollection 2023.
9
How New Developments in Pharmacology Receptor Theory Are Changing (Our Understanding of) Hypertension Therapy.药理学受体理论的新进展如何改变(我们对)高血压治疗的理解。
Am J Hypertens. 2024 Mar 15;37(4):248-260. doi: 10.1093/ajh/hpad121.
10
The G protein biased serotonin 5-HT2A receptor agonist lisuride exerts anti-depressant drug-like activities in mice.G蛋白偏向性5-羟色胺5-HT2A受体激动剂利苏立肽在小鼠中发挥出类抗抑郁药物活性。
Front Mol Biosci. 2023 Oct 10;10:1233743. doi: 10.3389/fmolb.2023.1233743. eCollection 2023.