揭开批准的非类宏循环的治疗景观
Zhonghua Li1, Zhenqiang Zhang1, Bin Yu2,3
1Academy of Chinese Medical Sciences, Collaborative Innovation Center of Research and Development on the Whole Industry Chain of Yu-Yao, Henan University of Chinese Medicine, Zhengzhou 450046, China.
Acta pharmaceutica Sinica. B
|July 23, 2025
概括
非类宏循环药物在向癌症等疾病方面具有结构优势. 本次审查强调了34种已批准的药物 (2000-2024年),重点关注自然,灵感和de novo宏观循环的优化策略.
科学领域:
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
- 有机化学 有机化学
背景情况:
- 非类宏环药物表现出独特的结构特征,有利于向生物分子.
- 这些化合物在各种疾病中显示出显著的治疗潜力,包括癌症和传染病.
研究的目的:
- 审查2000年至2024年间批准的34种非类宏循环药物.
- 专注于优化过程的自然,自然产品的灵感,和新的宏观循环药物.
- 阐明有助于有效性的结构特征,如形状刚性和目标特异性.
主要方法:
- 关于2000-2024年批准的宏环药物的综合文献综述.
- 对结构特征的分析和优化设计策略的分析.
- 案例研究说明了成功的宏观循环药物开发.
主要成果:
- 在指定期间批准的34种非类宏环药物.
- 突出了形状刚性和标特异性在药物疗效中的作用.
- 通过成功的例子展示了设计细节和优化见解.
结论:
- 宏循环药物,特别是非类药物,是一个有前途的治疗类.
- 对自然,灵感和de novo宏循环的优化策略对于药物开发至关重要.
- U型结构的宏循环化是 de novo宏循环设计中的一种新策略.
相关概念视频
Targets for Drug Action: Overview
7.5K
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
7.5K
Transducer Mechanism: Enzyme-Linked Receptors
2.8K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.8K
Principles of Drug Action
6.6K
Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
6.6K
Drug Administration and Therapy Phases: Overview
761
Drugs, the chemical agents used in diagnosing, treating, or preventing diseases, undergo a four-phase process of development: pharmaceutic, pharmacokinetics, pharmacodynamics, and therapeutic.
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...
761
Structure-Activity Relationships and Drug Design
1.1K
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...
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...
1.1K
Pharmacodynamics: Overview and Principles
2.1K
Pharmacodynamics is a scientific field that delves into drugs' intricate biochemical, cellular, and physiological effects on the human body. The study of pharmacodynamics helps us understand how drugs interact with the body and elicit various responses.
Most drugs' effects result from their interactions with drug receptors or targets within the body. These interactions trigger specific responses at the cellular or systemic level. Drug receptors can be found on the surfaces of cells or...
Most drugs' effects result from their interactions with drug receptors or targets within the body. These interactions trigger specific responses at the cellular or systemic level. Drug receptors can be found on the surfaces of cells or...
2.1K


