最近 ALKBH 1-8 抑制剂的发现取得了进展
Claudia Silva1, Valentina Zuliani1, Gabriella Nicolini2
1Food and Drug Department, University of Parma, Parma, Italy.
Expert opinion on drug discovery
|October 28, 2025
概括
向AlkB家族二氧化原酶 (ALKBH18) 的抑制剂对于表观遗传调节和癌症治疗至关重要. 开发具有良好的药理动力学的选择性抑制剂具有挑战性,但具有显著的治疗潜力.
科学领域:
- 生物化学 生物化学
- 药用化学 医学化学
- 表观遗传学 在表观遗传学中,表观遗传学是指表观遗传学.
背景情况:
- AlkB家族包括Fe (II) 和α-甲酸依赖的二氧化基酶,参与核基脱基化.
- 这些酶在DNA修复和表观遗传调节中发挥作用,有九种人类同类 (ALKBH18和FTO).
研究的目的:
- 本综述侧重于ALKBH18.8的抑制剂的发现和开发.
- 它考察了药物化学的角度,包括结构-活性关系.
主要方法:
- 在2021年至2025年期间使用PubMed.Med发表的研究文献综述.
- 对抑制剂发现和发展途径的分析.
主要成果:
- 由于ALKBH酶在病理,特别是癌症中的作用,因此对ALKBH酶的抑制越来越感兴趣.
- 挑战包括实现亚型选择性和优化药物动力学概况以治疗用途.
结论:
- ALKBH 抑制剂对各种疾病具有显著的治疗机会.
- 进一步了解ALKBH家族结构和机制对于有针对性的药物开发至关重要.
更多相关视频
05:55Identifying Inhibitors of the HBx-DDB1 Interaction Using a Split Luciferase Assay System
Published on: December 21, 2019
7.1K
10:33Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
Published on: October 26, 2015
11.8K
相关概念视频
Drug Discovery: Overview
10.9K
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...
10.9K
Alkynes to Aldehydes and Ketones: Hydroboration-Oxidation
20.7K
Introduction
One of the convenient methods for the preparation of aldehydes and ketones is via hydration of alkynes. Hydroboration-oxidation of alkynes is an indirect hydration reaction in which an alkyne is treated with borane followed by oxidation with alkaline peroxide to form an enol that rapidly converts into an aldehyde or a ketone. Terminal alkynes form aldehydes, whereas internal alkynes give ketones as the final product.
One of the convenient methods for the preparation of aldehydes and ketones is via hydration of alkynes. Hydroboration-oxidation of alkynes is an indirect hydration reaction in which an alkyne is treated with borane followed by oxidation with alkaline peroxide to form an enol that rapidly converts into an aldehyde or a ketone. Terminal alkynes form aldehydes, whereas internal alkynes give ketones as the final product.
20.7K
Targeted Cancer Therapies
8.6K
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...
8.6K
Cooperative Allosteric Transitions
8.6K
Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
8.6K
