相关实验视频
Updated: May 12, 2026

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Oligopeptide Competition Assay for Phosphorylation Site Determination
Published on: May 18, 2017
选择性检测全性酸酶抑制剂的选择性检测
Ralf Schneider1, Claudia Beumer, Jeffrey R Simard
1Chemical Genomics Centre der Max-Planck-Gesellschaft, Dortmund, Germany.
Journal of the American Chemical Society
|April 25, 2013
概括
开发新的酸酶抑制剂对于治疗癌症等疾病至关重要. 这项研究引入了一种新的高通量选试验,以发现全酸酸酶抑制剂,克服了以前方法的局限性.
科学领域:
- 生物化学 生物化学
- 酶学 是一种酶学.
- 药物发现 药物发现 药物发现
背景情况:
- 通过酶和酶对蛋白质的酸化调节细胞功能.
- 酸化失调有助于癌症和炎症等疾病.
- 虽然激酶抑制剂是成功的,但由于选择性和电荷问题,没有任何酸酶抑制剂得到临床批准.
研究的目的:
- 开发一种用于发现全性酸酶抑制剂的新型试验.
- 为了解决对全调节器缺乏合适的选系统的问题.
- 为了能够识别具有改善药理性质的候选药物.
主要方法:
- 开发一种新的结合性试验.
- 测试旨在检测结合于异质口袋的配体.
- 测试验证用于高通量选 (HTS).
主要成果:
- 该试验成功检测了与蛋白质氨酸酸酶1B (PTP1B) 的全囊结合的配体.
- 该试验表明,在异质性和基质竞争性联体之间存在明显的歧视.
- 该试验适用于高通量选应用.
结论:
- 开发了一种新的,选择性试验,用于发现全酸酶抑制剂的发现.
- 这种测试有助于识别新型酸酶调节剂.
- 该试验克服了以前方法的局限性,为新疗法铺平了道路.
相关概念视频
Allosteric Regulation
Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
Protein Kinases and Phosphatases
Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Allosteric Proteins-ATCase
Binding sites linkages can regulate a protein's function. For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
Enzyme Inhibition
Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.
Transducer Mechanism: Enzyme-Linked Receptors
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:

