针对HSF1途径的小分子:化学策略和治疗潜力
Caiyiren Wen1,2, Yiqi Geng1,2, Jiayue Pei1,2
1State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Journal of medicinal chemistry
|September 3, 2025
概括
热冲击因子1 (HSF1) 是细胞压力和癌症的关键调节剂,但传统上是无法治疗的. 最近的药物化学进步提供了针对HSF1治疗的新型小分子战略.
科学领域:
- 生物化学
- 分子生物学
- 医学化学
背景情况:
- 热冲击因子1 (HSF1) 对细胞应激反应和癌症进展至关重要.
- 由于HSF1的结构和缺乏结合口袋使其成为一个具有挑战性的治疗目标.
- 现有研究强调HSF1在各种病理中的作用,包括癌症,神经退行和代谢疾病.
研究的目的:
- 对调节热冲击因子1 (HSF1) 活性药物化学的最新进展进行审查.
- 提供针对以前无法治疗的HSF1的创新化学策略的见解.
- 在瘤学,神经退行和代谢疾病中探索HSF1抑制剂的治疗机会.
主要方法:
- 审查最新的药物化学文献和药物发现方法.
- 针对HSF1的功能领域和调节网络的小分子调节器的分析.
- 探索化学策略来克服HSF1固有的药物挑战.
主要成果:
- 通过创新的化学策略开发了多种小分子调节器.
- 新的方法可以通过直接参与或间接调节网络来调节HSF1活动.
- 对于HSF1调节的化学空间已经显著扩大.
结论:
- 最近的药物化学进步提供了针对HSF1的可行策略,HSF1是一种"无毒"蛋白质.
- 这些发现为设计新型HSF1抑制剂提供了基础.
- 在治疗癌症,神经退行性和代谢性疾病方面,HSF1调节具有前景.
相关概念视频
Targets for Drug Action: Overview
7.4K
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...
7.4K
Targeted Cancer Therapies
7.8K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
7.8K
Drug Discovery: Overview
8.7K
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...
8.7K
siRNA - Small Interfering RNAs
17.0K
Small interfering RNAs, or siRNAs, are short regulatory RNA molecules that can silence genes post-transcriptionally, as well as the transcriptional level in some cases. siRNAs are important for protecting cells against viral infections and silencing transposable genetic elements.
In the cytoplasm, siRNA is processed from a double-stranded RNA, which comes from either endogenous DNA transcription or exogenous sources like a virus. This double-stranded RNA is then cleaved by the...
In the cytoplasm, siRNA is processed from a double-stranded RNA, which comes from either endogenous DNA transcription or exogenous sources like a virus. This double-stranded RNA is then cleaved by the...
17.0K


