Jove
Visualize
联系我们
JoVE
x logofacebook logolinkedin logoyoutube logo
关于 JoVE
概览领导团队博客JoVE 帮助中心
作者
出版流程编辑委员会范围与政策同行评审常见问题投稿
图书馆员
用户评价订阅访问资源图书馆顾问委员会常见问题
研究
JoVE JournalMethods CollectionsJoVE Encyclopedia of Experiments存档
教育
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab Manual教师资源中心教师网站
使用条款与条件
隐私政策
政策

相关概念视频

Acid Suppressive Drugs for Peptic Ulcer Disease: Proton Pump Inhibitors01:13

Acid Suppressive Drugs for Peptic Ulcer Disease: Proton Pump Inhibitors

463
Peptic ulcers, often induced by H. pylori infections or NSAID usage, arise from disruptions in the delicate balance of gastric acid production. Peptic ulcers stem from heightened gastric acid levels due to H. pylori infections or NSAID use. The protective mucus layer diminishes in the presence of these factors, allowing gastric acid to erode the stomach lining and form ulcers.
Gastric acid, a potent cocktail of hydrogen and chloride ions, is produced in specialized parietal cells within the...
463
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

764
Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
764
Acid Suppressive Drugs for Peptic Ulcer Disease: Histamine H2-Receptor Antagonists01:28

Acid Suppressive Drugs for Peptic Ulcer Disease: Histamine H2-Receptor Antagonists

511
Histamine H2 receptors, which are intricately located on the basolateral membrane of parietal cells, play a crucial role in modulating gastric acid secretion. When released from enterochromaffin-like cells, histamine engages H2 receptors, initiating the cyclic AMP (cAMP) pathway. In this pathway, adenylyl cyclase converts ATP into cAMP, elevating intracellular cAMP levels. The activation of protein kinase A follows, stimulating the proton pump. This stimulation prompts the secretion of hydrogen...
511
Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents01:20

Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents

488
The gastric mucosa produces prostaglandins E2 (PGE2) and prostacyclin (PGI2), crucial in maintaining gastric health. They exert cytoprotective effects, including increasing bicarbonate secretion, releasing protective mucin, reducing gastric acid output, and preventing harmful vasoconstriction. These effects are mediated through various receptors, such as EP1, EP2, EP3, and EP4.
Non-steroidal anti-inflammatory drugs (NSAIDs) can induce peptic ulcers by inhibiting cyclooxygenase, decreasing...
488
Peptic Ulcer Disease IV: Management01:26

Peptic Ulcer Disease IV: Management

110
Medical treatment strategies for peptic ulcers encompass various methods. The primary goal of treatment is to diminish gastric acidity and strengthen mucosal defense mechanisms.
The therapeutic approach involves ensuring adequate rest, implementing drug therapy, promoting smoking cessation, making dietary modifications, and emphasizing long-term follow-up care.
Pharmacological management
The prevailing therapy for peptic ulcers involves a combination of managing the patient's current...
110
Drug Discovery: Overview01:26

Drug Discovery: Overview

8.0K
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...
8.0K

您也可能阅读

相关文章

通过共同作者、期刊和引用图与本文相关的文章。

排序
Same author

Integrative Molecular Scaffold Generation of PI3K/mTOR Inhibitors Using DeepSARM and Ligand-Based Virtual Screening Approaches.

ChemMedChem·2026
Same author

A planar dimer of bovine ATP synthase.

Cell death and differentiation·2026
Same author

On the mechanism of hypomagnesemia with treatment-resistant seizures caused by variants of the Na+,K+-ATPase α1 subunit (ATP1A1).

The Journal of general physiology·2026
Same author

Total Synthesis of Scandine.

JACS Au·2026
Same author

Water, water, every where-the advent of hydrated pili structure.

The FEBS journal·2026
Same author

Synthesis of Multisubstituted Diazatricyclic Molecules Via Intramolecular Cycloaddition of Cyclic Azomethine Ylides.

Organic letters·2026

相关实验视频

Updated: Jul 16, 2025

Author Spotlight: Gastric Epithelial Cell Responses in Helicobacter pylori infection
08:24

Author Spotlight: Gastric Epithelial Cell Responses in Helicobacter pylori infection

Published on: July 5, 2024

670

深度学习驱动的de novo药物设计基于胃质子结构.

Kazuhiro Abe1,2,3, Mami Ozako4, Miki Inukai4

  • 1Cellular and Structural Physiology Institute, Nagoya University, Nagoya, Aichi, 464-8601, Japan. kabe@cespi.nagoya-u.ac.jp.

Communications biology
|September 19, 2023
PubMed
概括

研究人员使用人工智能驱动的药物设计和冷EM开发了针对胃质子的新型化合物. 最强效的化合物,DQ-18,对新药开发具有强大的抑制潜力.

更多相关视频

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.4K
Author Spotlight: A Computational Approach to Decipher Amino Acid Preferences in Multispecific Protein-Protein Interactions
06:50

Author Spotlight: A Computational Approach to Decipher Amino Acid Preferences in Multispecific Protein-Protein Interactions

Published on: January 26, 2024

1.9K

相关实验视频

Last Updated: Jul 16, 2025

Author Spotlight: Gastric Epithelial Cell Responses in Helicobacter pylori infection
08:24

Author Spotlight: Gastric Epithelial Cell Responses in Helicobacter pylori infection

Published on: July 5, 2024

670
Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.4K
Author Spotlight: A Computational Approach to Decipher Amino Acid Preferences in Multispecific Protein-Protein Interactions
06:50

Author Spotlight: A Computational Approach to Decipher Amino Acid Preferences in Multispecific Protein-Protein Interactions

Published on: January 26, 2024

1.9K

科学领域:

  • 药用化学 医学化学
  • 结构生物学 结构生物学
  • 计算机化药物发现技术

背景情况:

  • 现有的药物面临着诸如副作用和较差的结合亲和力等局限性.
  • 针对胃质子对于治疗的发展至关重要.

研究的目的:

  • 设计新型化合物,对胃质子具有很高的抑制作用.
  • 通过基于结构的de novo设计,克服现有药物的局限性.

主要方法:

  • 使用深度生成模型进行新药设计 (深度四重奏工作流).
  • 使用有机合成和冷电子显微镜 (cryo-EM) 进行结构分析.
  • 集成的in silico设计与体外查和结构验证.

主要成果:

  • 设计和合成基于与药物结合的质子药的候选化合物.
  • 确定了DQ-18 (N-甲基-4-((2-(基)-5-基) 氧) 胺) 作为最强效的化合物.
  • 获得DQ-18的Ki值为47.6nM,绑定姿势由2.08 Å的冷EM确定.

结论:

  • 综合方法使得基于结构的新药开发成为可能.
  • 高分辨率的冷EM可方便代化合物设计和优化.
  • 证明了一个成功的框架,用于创建针对特定蛋白质结构的强效药物候选物.