作为编码小分子图书馆合成信息的载体的非生物
Simon L Rössler1, Nathalie M Grob1, Stephen L Buchwald1
1Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
Science (New York, N.Y.)
|March 2, 2023
概括
研究人员开发了用于小分子合成的编码库 (PEL),克服了DNA的局限性. 这种新方法可以有效地发现治疗标的蛋白质配体.
科学领域:
- 化学生物学
- 合成化学
- 药物发现
背景情况:
- 基于DNA的编码加速了小分子对蛋白质标的发现.
- 基于寡核酸的编码在信息稳定性和密度方面面临挑战.
研究的目的:
- 建立下一代信息存储和小分子合成编码的非生物.
- 应用编码库 (PEL) 进行蛋白质配体的新发现.
主要方法:
- 使用化学稳定的非生物作为信息载体.
- 采用介导反应来有效合成多种纯净的PEL.
- 对碳酸无水酶IX,BRD4和MDM2目标进行亲和选择.
主要成果:
- 成功合成具有广泛化学多样性和高纯度的PEL.
- 从PEL中证明了新发现的小分子蛋白质配体.
- 确定了对主要致癌蛋白向的配体.
结论:
- 无生物作为强大的载体来编码小分子合成信息.
- 编码库为发现治疗性蛋白质配体提供了强大的平台.
- 这种方法提升了化学合成和药物发现方法.
相关概念视频
02:43Peptide Bonds
75.1K
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...
75.1K
01:28ATP and Macromolecule Synthesis
5.7K
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...
5.7K