抗寄生素的发现:从基因型到表型到化合物
Richard J Marhöfer1, Sandra Noack1, Paul M Selzer1
1Boehringer Ingelheim Animal Health, Binger Str 173, 55216 Ingelheim am Rhein, Germany.
Trends in parasitology
|May 9, 2025
概括
基于分子标的查对于发现新的抗寄生虫药物至关重要,它补充了传统的表型查方法. 这种方法已经产生了大量的抗寄生虫剂,证明了它与其他查策略相结合时的价值.
科学领域:
- 药物发现 药物发现 药物发现
- 寄生虫学的寄生虫学
- 药用化学 医学化学
背景情况:
- 抗寄生虫药物发现历史上依赖于全生物体查 (表型查).
- 基于分子标的查发挥了有限的作用,并且经常被低估.
- 很少有销售的抗寄生虫药物仅仅通过基于分子标的方法被发现.
研究的目的:
- 评估基于分子标的查在抗寄生虫药物发现中的相关性和影响.
- 突出基于分子标的查与表型查一起成功应用的成功应用.
- 强调整合不同查方法用于识别新型抗寄生虫剂的价值.
主要方法:
- 历史和当前的抗寄生虫药物发现策略的审查.
- 对表型查与基于分子标的查的文献分析.
- 使用基于分子标的方法开发的成功抗寄生虫药物的案例研究.
主要成果:
- 表型查已经主导了抗寄生虫药物发现文献.
- 基于分子标的查导致发现了重要的抗寄生虫药物类别,包括异zolines,bispyrazoles,depsipeptides和praziquantel衍生物.
- 成功的抗寄生虫药物证明了基于分子标的方法在与表型查相结合时的有效性.
结论:
- 基于分子标的查是抗寄生虫药物发现的有价值和有效的策略.
- 将基于分子标的查与表型查相结合,有助于发现新型抗寄生虫药物.
- 基于分子标的查的感知较少的相关性受到使用这种方法发现的药物的成功挑战.
相关概念视频
Drug Discovery: Overview
7.1K
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...
7.1K
Genetic Screens
4.8K
Genetic screens are tools used to identify genes and mutations responsible for phenotypes of interest. Genetic screens help identify individuals or a group of people at risk of developing genetic diseases and help them with early intervention, targeted therapy, and reproductive options.
Forward genetic screens
Forward or “classical” genetic screens involve creating random mutations in an organism’s DNA using radiation, mutagens, or insertion of additional bases, which...
Forward genetic screens
Forward or “classical” genetic screens involve creating random mutations in an organism’s DNA using radiation, mutagens, or insertion of additional bases, which...
4.8K
Epistasis Analysis
4.8K
Although Mendel chose seven unrelated traits in peas to study gene segregation, most traits involve multiple gene interactions that create a spectrum of phenotypes. When the interaction of various genes or alleles at different locations influences a phenotype, this is called epistasis. Epistasis often involves one gene masking or interfering with the expression of another (antagonistic epistasis). Epistasis often occurs when different genes are part of the same biochemical pathway. The...
4.8K


