有多少激酶是可以服用药物的? 这是一个对我们目前的理解的回顾
Brian Anderson1, Peter Rosston1,2, Han Wee Ong1
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, U.S.A.
The Biochemical journal
|August 29, 2023
概括
为每一个人体酶开发一种药物是可以实现的. 分析显示,许多激酶研究不足,但存在工具化合物,突出显示药物发现和激酶选择性策略的未开发潜力.
科学领域:
- 生物化学 生物化学
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
背景情况:
- 现存的500多种人体激酶具有不同程度的研究兴趣.
- 基因酶在疾病发病过程中至关重要,并且是有吸引力的药物标.
研究的目的:
- 评估当前可使用药物的人类激酶的现状.
- 确定未经研究的激酶,并探索开发新型激酶抑制剂的机会.
主要方法:
- 关于人体激酶的全面数据收集:引用数量,化学探针,药物批准,PDB结构和测试可用性.
- 分析数据以确定研究重点和基因组内的知识差距.
- 对实现酶选择性的策略的审查.
主要成果:
- 一个不成比例的研究重点存在于具有良好的特征的激酶,留下了大部分的基因组研究不足.
- 已经开发了对未经研究的激酶的工具化合物,这表明了大量尚未开发的潜力.
- 在过去二十年中,酶向药物发现的进展显而易见.
结论:
- 开发一个工具化合物对每一个人体酶都是可行的.
- 本综述可以作为未来酶向药物发现工作的资源和灵感.
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