由非核糖体胺天然产物启发的宏循环
Lara R Malins1, Justine N deGruyter1, Kevin J Robbins2
1Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Journal of the American Chemical Society
|March 23, 2017
概括
这项研究引入了一种新型的热力学方法,用于的宏循环化,在没有保护组的情况下从水中的胺中产生多样化的宏循环. 这种方法简化了复杂循环和天然产品的合成.
科学领域:
- 化学合成
- 有机化学
- 生物化学
背景情况:
- 的宏循环化对于开发治疗方法和理解生物过程至关重要.
- 现有的方法通常需要保护群体和恶劣的条件,限制范围和效率.
研究的目的:
- 开发一种多功能的热力学方法,用于的宏循环.
- 获取结构多样化的宏观循环,包括具有非原生基因的天然产品类似物和.
主要方法:
- 利用过渡性宏环胺对核友的反应性.
- 在温和条件下在水中进行反应,没有侧链保护组.
- 使用可变温度的NMR和循环二元化进行结构分析.
主要成果:
- 成功合成结构多样化的宏环,包括天然产品的类似物.
- 对所有蛋白质原性功能组的耐受性和与水性介质的兼容性.
- 使用非原生图案,同位素标签和生物直角手柄制备宏循环.
结论:
- 开发的热力学方法为的宏循环化提供了强大而通用的策略.
- 线性基质的预组织对于成功的宏循环并非必不可少.
- 该方法在环保条件下促进复杂循环的合成.
更多相关视频
08:48Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
12.5K
11:09Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation
Published on: August 1, 2018
11.3K
相关概念视频
Peptidoglycan Synthesis
3.5K
Structure of PeptidoglycanPeptidoglycan is a vital structural component of the bacterial cell wall, providing mechanical strength and shape to the cell. It consists of repeating units of two sugars—N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM)—linked by β-1,4 glycosidic bonds. These sugar chains are cross-linked by short peptide chains, forming a mesh-like polymer that surrounds the bacterial plasma membrane.Cytoplasmic Phase – Precursor SynthesisPeptidoglycan...
3.5K
Peptide Bonds
85.1K
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...
85.1K
ATP and Macromolecule Synthesis
7.1K
Biological macromolecules are organic compounds, predominantly composed of carbon atoms. The carbon atoms are covalently bonded with hydrogen, oxygen, nitrogen, and other minor elements. There are four major biological macromolecule classes: carbohydrates, lipids, proteins, and nucleic acids.
Most macromolecules are composed of single subunits, or building blocks, called monomers. The monomers combine with each other using covalent bonds to form larger molecules known as polymers.
Conversion of...
Most macromolecules are composed of single subunits, or building blocks, called monomers. The monomers combine with each other using covalent bonds to form larger molecules known as polymers.
Conversion of...
7.1K
