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Transducer Mechanism: G Protein–Coupled Receptors

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...

G Protein-coupled Receptors

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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...

GPCR Desensitization

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...

Conservative Site-specific Recombination and Phase Variation

Conservative Site-specific Recombination and Phase Variation

Because the DNA segments are cut and reorganized in a direction-specific manner, site-specific recombination has emerged as an efficient genetic engineering technique. Flippase and Cyclization recombinases or Flp and Cre, respectively, are two members of the tyrosine recombinase family derived from bacteriophages, that are used to mediate site-specific DNA insertions, deletions, and targeted expression of proteins in mammalian cell lines.
The recognition sites for Cre recombinase called LoxP...

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Updated: Jun 11, 2025

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

一个机器学习算法建议重新定位针对选定的GPCR的机会.

Shayma El-Atawneh¹, Amiram Goldblum¹

¹Molecular Modelling and Drug Design Lab, Institute for Drug Research and Fraunhofer Project Center for Drug Discovery and Delivery, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 9112001, Israel.

International journal of molecular sciences

|September 28, 2024

概括

此摘要是机器生成的。

这项研究使用了机器学习算法来选现有药物的新治疗用途. 计算方法为各种G蛋白结合受体识别了5982种潜在的药物重定位候选者.

关键词:

在GPCRs中,GPCRs是指GPCR.这就是ISE.大麻素2受体的受体多巴胺受体的多巴胺受体发现药物的发现.基因素受体基因素受体基因素受体机器学习是机器学习.重新调整使用目的.

更多相关视频

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Published on: April 9, 2018

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

相关实验视频

Last Updated: Jun 11, 2025

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Published on: April 9, 2018

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

科学领域:

计算化学是一种计算化学.
药理学药理学是指药理学的学科.
药物发现药物发现

背景情况:

药物重定向通过利用具有既定的安全性概况的药物来加速新疗法的发现.
计算方法通过提供合理的框架和降低失败率来增强药物重新用途.

研究的目的:

利用计算方法来识别新药重定向的机会.
在DrugBank数据库中选G蛋白结合受体 (GPCRs) 的潜在激素和对抗剂.

主要方法:

利用代随机淘汰 (ISE) 算法,一种机器学习工具,来构建基于连接体的模型.
开发了六个GPCR家族的agonist和antagonist模型,使用物理化学性质和发表的生物活性数据 (IC50,Ki,EC50).
将DrugBank数据库与这些模型对比,以确定得分最高的药物候选人.

主要成果:

确定了5982种潜在的新分子作用 (激动剂和对抗剂).
创建了针对大麻素2 (CB2),组胺素 (H1,H3,H4) 和多巴胺3 (D3) 受体的药物重新定位候选者的列表.
这些候选药物显示出治疗疾病的潜力,包括神经炎症,肥胖,过敏性皮肤炎和药物滥用.

结论:

计算选成功识别了许多药物重定向候选人.
已识别的候选药物值得对新型治疗应用进行实验验证.
这种方法显著增加了发现用于未满足医疗需求的高度生物活性分子的可能性.