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

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

268
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
268
Factors Affecting Solubility04:01

Factors Affecting Solubility

33.9K
Compared with pure water, the solubility of an ionic compound is less in aqueous solutions containing a common ion (one also produced by dissolution of the ionic compound). This is an example of a phenomenon known as the common ion effect, which is a consequence of the law of mass action that may be explained using Le Chȃtelier’s principle. Consider the dissolution of silver iodide:
33.9K
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

2.0K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
2.0K
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

1.0K
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
1.0K
Physical Properties Affecting Solubility02:19

Physical Properties Affecting Solubility

23.6K
Solutions of Gases in Liquids
As for any solution, the solubility of a gas in a liquid is affected by the attractive intermolecular forces between solute and solvent species. Unlike solid and liquid solutes, however, there is no solute-solute intermolecular attraction to overcome when a gaseous solute dissolves in a liquid solvent since the atoms or molecules comprising a gas are far separated and experience negligible interactions. Consequently, solute-solvent interactions are the sole...
23.6K
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

195
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
195

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

Targeting Histone Acetyltransferases EP300/CBP by Novel Proline-Based PROTAC Degraders.

ACS medicinal chemistry letters·2026
Same author

Fluorinated Aminopiperidones as Non-Glutarimide Thalidomide Analogs: Stereodivergent Synthesis and Validation.

ChemMedChem·2026
Same author

Author Correction: Teclistamab-based induction treatment in transplant-eligible, newly diagnosed multiple myeloma: a phase 2 trial.

Nature medicine·2026
Same author

Teclistamab-based induction treatment in transplant-eligible, newly diagnosed multiple myeloma: a phase 2 trial.

Nature medicine·2026
Same author

Teclistamab for treatment-refractory autoimmune diseases: a multicentre case series.

Annals of the rheumatic diseases·2026
Same author

Teclistamab induces rapid clinical response and deep tissue depletion in refractory systemic sclerosis-a case series.

Annals of the rheumatic diseases·2026

相关实验视频

Updated: Sep 15, 2025

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
05:08

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

17.0K

在基于VHL的PROTAC中提高溶解性:优化USP7降解器以提高可开发性.

Sophie Wittenburg1, Maximilian R Zuleeg2, Kirsten Peter2

  • 1Pharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, DE-53121 Bonn, Germany.

Journal of medicinal chemistry
|July 17, 2025
PubMed
概括

研究人员通过修改它们的结构,提高了基于VHL的蛋白质溶解向嵌合体 (PROTACs) 的溶解度. 这项工作加强了用于潜在的体内应用的PROTACs的开发.

更多相关视频

A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
09:57

A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles

Published on: December 23, 2016

9.0K
Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

13.4K

相关实验视频

Last Updated: Sep 15, 2025

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
05:08

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

17.0K
A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
09:57

A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles

Published on: December 23, 2016

9.0K
Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

13.4K

科学领域:

  • 药用化学 医学化学
  • 药物发现 药物发现 药物发现
  • 分子生物学分子生物学

背景情况:

  • 基于VHL的蛋白质溶解向嵌合体 (PROTACs) 面临开发挑战,原因是其物理化学性能差,例如水溶性低.
  • 高的极地总表面积 (TPSA) 和键供体 (HBD) 数量有助于这些限制.

研究的目的:

  • 为了增强VHL-招募USP7降解剂的物理化学特性.
  • 开发具有提高溶解性的PROTAC,同时保持目标降解效率.

主要方法:

  • 在VHL招募PROTAC中对脂友性,HBD计数和TPSA进行系统调整.
  • VHL连接体的结构修改,包括支架约束和溶解组的添加.
  • 评估USP7降解能力和目标选择性.

主要成果:

  • 在基于VHL的新型PROTAC中取得显著改善的水溶性.
  • 与其前身相比,PROTAC 40具有二基皮佩拉,可溶性增加了170倍.
  • 在结构修改后保持了强大的USP7降解和目标选择性.

结论:

  • 合理的脚手架设计是有效的,用于创建可溶性增强的基于VHL的PROTAC.
  • 开发的PROTAC显示了药物开发和体内应用的广泛潜力.
  • 该方法可能适用于开发针对其他E3链酶的PROTACs.