对一种细菌多药物运输蛋白的 doxorubicin 运输测量
Pei-Yu Hsieh1, Hendrik W van Veen1
1Department of Pharmacology, University of Cambridge, Cambridge, United Kingdom.
Methods in enzymology
|November 27, 2025
概括
我们开发了新的方法来测量多药物载体的活性,例如Vibrio cholerae (NorM-VC) 的NorM. 这些测试使用多克索鲁比,可以适应在细菌细胞和蛋白质体中进行高通量查.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 微生物学 微生物学
背景情况:
- 多种药物载体对于细菌抗生素耐药性至关重要.
- 来自Vibrio cholerae (NorM-VC) 的MATE家族输送器NorM作为离子/抗生素交换器起作用.
- 现有的结构和机制数据需要可访问的活动分析.
研究的目的:
- 建立方便的方法来测量Norm-VC的运输活动.
- 为了使在非致病性系统和细胞模拟中进行活动评估.
- 为了促进多药物传输器功能的高通量选.
主要方法:
- 对NORM-VC的表达和净化.
- 将净化的NorM-VC溶解成蛋白质体.
- 在Lactococcus lactis和proteoliposomes中进行多克索鲁素运输测定.
主要成果:
- 成功表达和净化功能NorM-VC.
- 在复制的蛋白质体和乳球菌中证明了多克索鲁比辛的运输活性.
- 验证了一种适用于高通量选的方法.
结论:
- 提出的方法为评估NorM-VC活动提供了一个强大的平台.
- 这些测量可以很容易地适应其他MATE家族的传送器和基板.
- 促进对多重耐药机制和药物发现的进一步研究.
更多相关视频
08:57Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice
Published on: October 5, 2017
11.4K
13:40In vitro Investigation of the MexAB Efflux Pump From Pseudomonas aeruginosa
Published on: February 17, 2014
12.2K
相关概念视频
ABC Transporters: Exporter
6.2K
ATP-binding cassette or ABC transporter is the largest superfamily of integral membrane proteins. The transporters have transmembrane-binding domains (TMDs) and nucleotide-binding domains (NBDs). The TMDs are specific to their substrates, whereas the NBDs are similar to engines that complete ATP hydrolysis to complete the substrate transport. They can be full transporters consisting of two TMDs and NBDs, half transporters with one TMD and NBD, while some encoded with a single TMD or NBD are...
6.2K
Carrier-Mediated Transport
981
Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
981
Drug Absorption Mechanism: Carrier-Mediated Membrane Transport
5.7K
Certain large, lipid-insoluble drug molecules that resemble amino acids, peptides, or glucose, require specialized carrier proteins to facilitate their diffusion across cell membranes. This transport can occur through either facilitated diffusion, which does not require energy input, or active transport, which does require energy input.
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
5.7K
ABC Transporters: Importer
3.3K
ATP-binding cassette or ABC transporters are a class of ATP-driven pumps that hydrolyze ATP to move solutes across the membrane. They can be grouped into importers and exporters. While exporters are present in all domains of life, importers exist only in bacteria and some plants.
In bacteria, based on the number of transmembrane helices and the chemical nature of their substrates, the ABC importers can be divided into three types:
In bacteria, based on the number of transmembrane helices and the chemical nature of their substrates, the ABC importers can be divided into three types:
3.3K
