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相关概念视频

The Two-State Receptor Model01:29

The Two-State Receptor Model

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
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相关实验视频

Updated: Jun 29, 2025

Parallel Interrogation of &#946;-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

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使用基于高通量测试的活性模型优化雄激素受体优先级.

Ronnie Joe Bever1, Stephen W Edwards2, Todor Antonijevic3

  • 1U.S. Environmental Protection Agency, Washington, DC, United States.

Frontiers in toxicology
|March 26, 2024
PubMed
概括
此摘要是机器生成的。

这项研究开发了一种数据驱动的方法来优化化学选试验,减少了52%的资源需求,同时保持了对内分泌干扰物检测的高灵敏度.

关键词:
受体受体是受体的受体.计算毒理学计算毒理学内分泌干扰 干扰内分泌系统高通量选的高通量选阶段性测试阶段性测试是指分层测试.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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科学领域:

  • 环境毒理学环境毒理学
  • 计算毒理学计算毒理学
  • 化学选 化学选 化学选

背景情况:

  • 计算模型有助于为美国环保署的内分泌干扰物查计划 (EDSP) 确定化学物质优先级.
  • 现有的雄激素受体 (AR) 途径模型需要优化,以提高效率和成本效益.
  • 测试可用性和化学多样性对当前选模型构成挑战.

研究的目的:

  • 展示一种数据处理方法,以确定最佳的最小测试电池.
  • 建立一个统一的评估方法,以对抗AR路径模型对最小测试电池进行评估.
  • 将化学集群分析纳入测试电池性能评估中.

主要方法:

  • 对比了两种先前发表的AR途径模型 (11-和14-试验).
  • 调查了测试子集,以优化测试策略的成本和灵敏度.
  • 在多阶段测试工作流程中包含基于化学结构的聚类.

主要成果:

  • 一个扩展的14个试验模型显示对对抗剂的敏感性更高;11个试验模型偏好了对抗剂.
  • 确定了关键测定:对抗性3种,对抗性2种.
  • 至少需要9个测试以达到95%的对激动性和对抗性的敏感性.
  • 在多阶段工作流程中,化学聚类将每种化学物质所需的平均检测量减少了52%.
  • 在形预测进一步降低了资源需求.

结论:

  • 使用化学聚类和多机制考虑的数据驱动方法提高了化学选效率.
  • 本案例研究验证了在EDSP下优化测试电池的概念验证.
  • 高效的选最大限度地提高了化学品的吞吐量,并使数据驱动的优先级能够用于进一步的测试.