通过可见光介导脱硫C-C键形成合成DNA编码的宏环
Yi Gan1, Yumei Zeng1, Haojie Guan1
1HitGen Inc., Building 6, No. 8 Huigu 1st East Road, Tianfu International Bio-Town, Shuangliu District, Chengdu 610200, Sichuan, P. R. China.
Organic letters
|November 28, 2024
概括
我们开发了一种新的DNA兼容的方法,使用光介导的C-C键形成来制造宏环. 这种策略有效地产生了多样化的DNA编码的宏循环,克服了药物发现的类循环的挑战.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 生物技术是生物技术.
背景情况:
- DNA编码库 (DEL) 技术是发现生物活性化合物的强大平台.
- 宏环是一种有前途的治疗类,但它们的合成,特别是循环化,具有挑战性.
- 需要有效的宏环DEL合成方法来加速药物发现.
研究的目的:
- 开发一种新的DNA兼容的宏循环化策略,用于构建宏循环DELs.
- 为了实现各种DNA编码的宏循环的高效合成.
- 为了克服目前在DEL生产中的酸环化方法的局限性.
主要方法:
- 可见光介导的脱硫C-C键形成用于宏环化.
- 整合循环化策略与DNA编码库技术.
- 与各种线性基质进行兼容性测试.
主要成果:
- 一种新的宏循环化策略被成功开发和验证.
- 该方法在温和条件下顺利进行,产量好.
- 该反应证明了与多种线性基质的兼容性,使得具有不同环形大小的结构多样化的DNA编码宏循环的生成成为可能.
结论:
- 开发的可见光中介宏循环化策略是DNA编码图书馆技术的重大进步.
- 这种方法提供了一种高效和多用途的方法来合成各种宏环.
- 该战略具有很大的潜力,可以加速发现新的生物活性宏环治疗方法.
更多相关视频
11:09Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation
Published on: August 1, 2018
10.7K
08:48Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
11.8K
相关概念视频
ATP and Macromolecule Synthesis
5.2K
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...
5.2K
Cycloaddition Reactions: Overview
2.5K
Cycloadditions are one of the most valuable and effective synthesis routes to form cyclic compounds. These are concerted pericyclic reactions between two unsaturated compounds resulting in a cyclic product with two new σ bonds formed at the expense of π bonds. The [4 + 2] cycloaddition, known as the Diels–Alder reaction, is the most common. The other example is a [2 + 2] cycloaddition.
2.5K
Cycloaddition Reactions: MO Requirements for Photochemical Activation
2.0K
Some cycloaddition reactions are activated by heat, while others are initiated by light. For example, a [2 + 2] cycloaddition between two ethylene molecules occurs only in the presence of light. It is photochemically allowed but thermally forbidden.
2.0K
Maxam-Gilbert Sequencing
11.1K
In the same year as the discovery of the Sanger sequencing method, another group of scientists, Allan Maxam and Walter Gilbert, demonstrated their chemical-cleavage method for DNA sequencing. The Maxam-Gilbert method relies on using different chemicals that can cleave the DNA sequence at specific sites, the separation of resulting DNA fragments of variable size using electrophoresis, and deciphering the DNA sequence from the resulting gel bands.
Challenges of the Maxam-Gilbert Method
The...
Challenges of the Maxam-Gilbert Method
The...
11.1K
