通过光催化三位结合进行化学选择性改
Younong Yu1, Li-Kang Zhang2, Alexei V Buevich2
1Department of Discovery Chemistry , MRL, Merck & Co., Inc. , Kenilworth , New Jersey 07033 , United States.
Journal of the American Chemical Society
|May 16, 2018
概括
研究人员开发了一种新的光催化方法来选择性地修改. 这种技术可实现精确的和蛋白质结合,促进治疗性发现和生物结合应用.
科学领域:
- 光催化
- 有机化学
- 生物结合
背景情况:
- 选择性修改和蛋白质对于开发新疗法和研究工具至关重要.
- 由于其独特的化学特性,胺为化学选择性修饰提供了一个有希望的目标.
研究的目的:
- 发现一种针对酸β位置的新型化学选择性改方法.
- 评估已开发的光催化的基质范围和化学选择性.
- 证明该方法对内源性和蛋白质的适用性.
主要方法:
- 对酸 β-位置的光催化反应的开发.
- 通过各种和迈克尔受体测试该方法.
- 对其他氨基酸残留物的化学选择性进行评估.
- 该方法应用于内源性 (葡萄糖,GLP-1胺) 和对照蛋白 (胰岛素).
主要成果:
- 在酸的位上取得了成功的化学选择性结合.
- 该方法证明了和迈克尔受体的广泛基质范围.
- 观察到高化学选择性,其他氨基酸残留的修饰最小.
- 内源性糖和GLP- 1胺被有效结合.
- 缺乏氨酸的胰岛素在B链上表现出选择性的C端脱碳化结合.
结论:
- 已经建立了一种选择性基改的新型光催化方法.
- 这种方法为和蛋白质修饰提供了多功能工具.
- 该方法支持发现新的治疗,蛋白质标记和生物结合策略.
相关概念视频
Conjugate Addition to α,β-Unsaturated Carbonyl Compounds
5.6K
α,β-Unsaturated carbonyl compounds are molecules bearing a carbonyl and alkene functionality in conjugation with each other. The conjugation in the molecule leads to three resonance structures. The hybrid form exhibits two probable electrophilic sites: the carbonyl carbon and the β carbon.
5.6K
Histone Modification
16.2K
The histone proteins have a flexible N-terminal tail extending out from the nucleosome. These histone tails are often subjected to post-translational modifications such as acetylation, methylation, phosphorylation, and ubiquitination. Particular combinations of these modifications form “histone codes” that influence the chromatin folding and tissue-specific gene expression.
Acetylation
The enzyme histone acetyltransferase adds acetyl group to the histones. Another enzyme, histone...
Acetylation
The enzyme histone acetyltransferase adds acetyl group to the histones. Another enzyme, histone...
16.2K
Peptide Bonds
83.4K
A peptide bond covalently attaches amino acids through a dehydration reaction. One amino acid's carboxyl group and another amino acid's amino group combine, releasing a water molecule. The resulting bond is the peptide bond. The products that such linkages form are peptides. As more amino acids join this growing chain, the resulting chain is a polypeptide. Each polypeptide has a free amino group at one end. This end has the N-terminal, or the amino-terminal, and the other end has a free...
83.4K
Conjugated Proteins
29.0K
Simple proteins and protein complexes contain only amino acids. In contrast, many other proteins, called conjugated proteins, covalently bond with non-protein moieties.
Nucleoproteins are protein complexes that contain nucleic acids, categorized as deoxyribonucleoproteins (DNPs) or ribonucleoproteins (RNPs) respectively. The nucleosome is a typical example of a DNP where nuclear DNA is associated with histone proteins. The major antigen for the Covid-19 virus SARS-CoV is an RNP that is critical...
Nucleoproteins are protein complexes that contain nucleic acids, categorized as deoxyribonucleoproteins (DNPs) or ribonucleoproteins (RNPs) respectively. The nucleosome is a typical example of a DNP where nuclear DNA is associated with histone proteins. The major antigen for the Covid-19 virus SARS-CoV is an RNP that is critical...
29.0K
Conjugated Proteins
3.2K
3.2K
Spreading of Chromatin Modifications
9.5K
The histone proteins in the nucleosomes are post-translationally modified (PTM) to increase or decrease access to DNA. The commonly observed PTMs are methylation, acetylation, phosphorylation, and ubiquitination of lysine amino acids in the histone H3 tail region. These histone modifications have specific meaning for the cell. Hence, they are called "histone code". The protein complex involved in histone modification is termed as "reader-writer" complex.
Writers
The writer...
Writers
The writer...
9.5K


