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相关概念视频

Genetic Screens02:46

Genetic Screens

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Genetic screens are tools used to identify genes and mutations responsible for phenotypes of interest. Genetic screens help identify individuals or a group of people at risk of developing  genetic diseases and help them with early intervention, targeted therapy, and reproductive options.
Forward genetic screens
Forward or “classical” genetic screens involve creating random mutations in an organism’s DNA using radiation, mutagens, or insertion of additional bases, which...
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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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...
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GPCR Desensitization01:12

GPCR Desensitization

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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...
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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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GPCRVS - - 一个基于人工智能的决策支持系统,用于GPCR虚拟选.

Dorota Latek1, Khushil Prajapati1, Paulina Dragan1

  • 1University of Warsaw, Faculty of Chemistry, 1 Pasteur St, 02-093 Warsaw, Poland.

International journal of molecular sciences
|March 13, 2025
PubMed
概括

GPCRVS是一种新的机器学习系统,可以预测G蛋白结合受体 (GPCRs) 的药物活性. 它评估化合物的活性,药理作用和结合方式,有助于设计向治疗药物.

关键词:
与G蛋白结合的受体是G蛋白结合的受体.决策支持系统 决策支持系统深度学习是一种深度学习.药物选择性的药物选择性梯度增强机器 梯度增强机器机器学习是机器学习.分子对接的分子对接.神经网络的神经网络的神经网络虚拟选 虚拟选 虚拟选

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相关实验视频

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科学领域:

  • 药理学 药理学是指药理学的学科.
  • 计算化学的计算化学
  • 生物信息学是一种生物信息学.

背景情况:

  • G蛋白结合受体 (GPCR) 是最大的药物点类,因为它们的可访问性和明确的信号传递.
  • 由于GPCR对化学结构的敏感性,可以精确设计药物.
  • 结构生物学最近的进展为GPCR药物发现中的机器学习应用提供了足够的数据.

研究的目的:

  • 引入GPCRVS,这是一个高效的机器学习系统,用于预测针对GPCR目标的化合物活性.
  • 为了使候选药物的在线评估,包括具有挑战性的和蛋白质结合GPCRs.
  • 通过评估活性范围,药理效应和约束模式来支持药物设计中的决策.

主要方法:

  • 开发GPCRVS,一种使用多类分类的机器学习系统.
  • 处理不完整和模糊的生物数据,以进行可靠的预测.
  • 使用ChEMBL和谷歌专利数据集对B类GPCR和化学因子受体进行验证.

主要成果:

  • GPCRVS有效地评估了各种GPCR的化合物活性,药理作用和潜在的结合模式.
  • 该系统处理不同类型的化合物,从小分子到短.
  • 为了准确性,预测与已知的活性配体进行了基准测试.

结论:

  • GPCRVS为虚拟查和针对GPCRs的药物设计提供了一个强大的工具.
  • 该系统能够处理复杂的GPCR和多样化的数据,提高了它的效用.
  • 通过预测化合物行为,GPCRVS促进了选择性和特定药物的开发.