在小分子,和蛋白质中采用介质的碳酸
Martin Gazvoda1, Heemal H Dhanjee1, Jacob Rodriguez1
1Department of Chemistry, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.
Journal of the American Chemical Society
|April 19, 2022
概括
研究人员开发了一种新的催化方法, 这种技术通过使密集群的向输送来增强中子捕获疗法.
科学领域:
- 医学化学
- 生物结合化学
- 中子捕获疗法
背景情况:
- 碳酸具有显著的治疗潜力,特别是在中子捕获疗法中.
- 有限的方法可以将碳酸纳入像和蛋白质这样的生物分子.
研究的目的:
- 在小分子,和蛋白质上安装carborane部分的一般和有效策略.
- 通过克服疏水性等挑战,使碳酸能够在向治疗中使用.
主要方法:
- 催化C-X (X=C,S,N) 键形成用于碳装置.
- 在室温下在水性缓冲物中选择性结合囊残留物.
- 使用特定的试剂与二硫酸连接剂在水性海斯蒂丁缓冲剂中进行蛋白质结合.
主要成果:
- 在小分子,,纳米体,亲体和抗体疗法 (trastuzumab, cetuximab) 上成功安装了含有碳基的组.
- 证明碳酸结合物 (亲体ZHER2,特拉斯图祖马布) 保持了目标抗原的结合.
- 在HER2阳性细胞系试验中,结合蛋白保持其生物活性.
结论:
- 开发的以为媒介的方法提供了一种多功能方法,用于将碳纳入多种生物分子.
- 这一策略有助于推进基于碳的治疗方法,特别是用于中子捕获疗法.
- 这种方法克服了碳酸的疏水性,并保持了生物分子的功能,为新的治疗药物铺平了道路.
相关概念视频
Cationic Chain-Growth Polymerization: Mechanism
2.4K
The cationic polymerization mechanism consists of three steps: initiation, propagation, and termination. In the initiation step of the polymerization process, the π bond of a monomer gets protonated by the Lewis acid catalyst, which is formed from boron trifluoride and water. The protonation of the π bond generates a carbocation stabilized by the electron‐donating group. In the propagation step, the π bond of the second monomer acts as a nucleophile and attacks the...
2.4K
Peptide Bonds
78.2K
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...
78.2K
Anionic Chain-Growth Polymerization: Overview
2.2K
The polymerization process that involves carbanion as an intermediate is called anionic polymerization. It is also a type of addition or chain-growth polymerization. Anionic polymerization gets initiated by a strong nucleophile such as an organolithium or a Grignard reagent. The most commonly used initiator for anionic polymerization is butyl lithium. Monomers involved in anionic polymerization must possess a vinyl group bonded to one or two electron-withdrawing groups. For instance,...
2.2K
Anionic Chain-Growth Polymerization: Mechanism
2.1K
The mechanism for anionic chain-growth polymerization involves initiation, propagation, and termination steps. In the initiation step, a nucleophilic anion, such as butyl lithium, initiates the polymerization process by attacking the π bond of the vinylic monomer. As a result, a carbanion, stabilized by the electron‐withdrawing group, is generated. The resulting carbanion acts as a Michael donor in the propagation step and attacks the second vinylic monomer, which acts as a Michael...
2.1K
Preparation of Carboxylic Acids: Carboxylation of Grignard Reagents
5.0K
Carboxylic acids can be prepared by the carboxylation of Grignard reagents (RMgX). This method is convenient for converting alkyl (primary, secondary or tertiary), vinyl, benzyl, and aryl halides to carboxylic acids with one additional carbon than the starting RMgX.
5.0K
α-Bromination of Carboxylic Acids: Hell–Volhard–Zelinski Reaction
3.2K
The method to achieve α-brominated carboxylic acids using a mixture of phosphorus tribromide and bromine is known as the Hell–Volhard–Zelinski reaction. The reaction is catalyzed by phosphorus tribromide, which can be used directly or produced in situ from red phosphorus and bromine. The mechanism comprises PBr3 catalyzed conversion of acid to acid bromide and hydrogen bromide. The acid bromide enolizes to its enol form in the presence of HBr. The nucleophilic enol attacks the...
3.2K


