一种昆虫ABCC载体的潜在农药基质
Jinli Chen1,2,3, Dong Wang1,3, Wei Liu1,3
1School of Bioengineering, Dalian University of Technology, Dalian, China.
Insect science
|November 30, 2024
概括
农药耐药性是一个日益严重的问题. 这项研究确定了carbofuran和buprofezin作为Tribolium castaneum中TcABCC-9C载体的基质,揭示了管理抗虫剂耐药性的新目标.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 昆虫学 昆虫学是一门学科.
背景情况:
- 害虫对农药的耐药性降低了合成农药的有效性.
- ATP结合盒 (ABC) 载体,特别是ABCC子家族,通过作为排泄,与农药耐药性有关.
- 目前用于识别昆虫ABC载体的农药基质的方法通常依赖于转录量化.
研究的目的:
- 来识别来自Tribolium castaneum的ABCC-9C载体的潜在农药基质.
- 研究TcABCC-9C在调解农药耐药性的作用.
- 开发一种模型来识别其他ABCC载体的基质.
主要方法:
- 在体外ATPase活性测定以选农药基质.
- 亲和度评估,细胞毒性分析和基于RNA干扰的生物活性测试.
- 分子对接以预测农药与TcABCC-9C的结合相互作用.
主要成果:
- 卡博富兰和布普罗菲津被确定为TcABCC-9C的潜在基质.
- 在TcABCC-9C中发现了一种由8个跨膜螺旋体形成的两转位通道.
- 分子对接揭示了卡博富兰和布普罗菲津通过疏水相互作用与转位通道的相同部位结合.
结论:
- 在Tribolium castaneum中,TcABCC-9C在多种农药耐药性方面发挥着重要作用.
- 已确定的载体和结合部位为管理抗虫剂耐药性的潜在目标提供了机会.
- 开发的实验模型可以应用于其他ABCC载体和杀虫剂耐药性预测.
相关概念视频
01:06Carrier-Mediated Transport
278
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...
278
01:19Drug Absorption Mechanism: Carrier-Mediated Membrane Transport
3.5K
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...
3.5K
01:14Active Transport
496
Active transport is a critical biological process that allows cells to move solutes against an electrochemical gradient. This process requires direct energy input and is characterized by its selectivity, saturability, and susceptibility to competitive inhibition.
Primary active transporters, like Na+, K+ and -ATPase, directly utilize ATP to move ions across the membrane. These transporters play significant roles in various physiological processes. For instance, Na+, K+ and -ATPase maintain...
Primary active transporters, like Na+, K+ and -ATPase, directly utilize ATP to move ions across the membrane. These transporters play significant roles in various physiological processes. For instance, Na+, K+ and -ATPase maintain...
496
01:14Hepatic Drug Clearance: Role of Transporters
39
In the liver and bile canaliculi, influx and efflux transporters modification can influence intrinsic clearance. Transporters play a significant role in moving drugs within liver cells. Elaborate models, such as the Biopharmaceutical Classification System (BCS), are essential to relate transporters to drug disposition. This system categorizes drugs into four classes based on solubility and permeability, providing insights into elimination routes and the effects of transporters following oral...
39