能够通过脂质和细胞膜运输离子的酶响应性载体
Ye Rin Choi1, Bom Lee1, Jinhong Park2
1Department of Chemistry, Yonsei University , Seoul 120-749, Korea.
Journal of the American Chemical Society
|December 10, 2016
概括
研究人员开发了酶激活的载体,用于通过膜控制离子的传输. 这些载体通过提高溶解度和实现向激活来增强药物输送.
科学领域:
- 膜运输
- 生物化学
- 药物输送系统
背景情况:
- 离子运输对于细胞功能至关重要.
- 开发水分子的向输送系统仍然是一个挑战.
- 提供受控激活和交付的潜力.
研究的目的:
- 引入和验证可控离子运输的载体概念.
- 在特定条件下研究酶介导的转载体激活.
- 评估水性附属物对前载体溶解度和膜分离的影响.
主要方法:
- 合成具有和糖系结合的亲水性附属体的前体.
- 使用乙酶 (PLE) 和葡萄糖酶 (AOG) 进行化.
- 通过脂质双层和细胞膜进行离子输送测试.
- 根据pH值进行激活研究.
主要成果:
- 前载体最初在脂友膜中不活跃,但被特定的酶激活.
- 在pH 7. 4时,PLE激活了以结为导体的前体.
- 在pH值为5. 5 - 6时,AOG激活了甘氨酸结合载体.
- 水性附属物增强了载体的水溶性,有助于分娩.
结论:
- 代载体策略可以控制离子运输的酶特异激活.
- 条件激活允许通过膜进行有针对性的输送和运输.
- 这种方法有望改善疏水性药物的输送.
更多相关视频
07:38Functional Characterization of Na+/H+ Exchangers of Intracellular Compartments Using Proton-killing Selection to Express Them at the Plasma Membrane
Published on: March 30, 2015
9.7K
09:59Functional Reconstitution and Channel Activity Measurements of Purified Wildtype and Mutant CFTR Protein
Published on: March 9, 2015
12.7K
相关概念视频
Carrier-Mediated Transport
1.5K
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...
1.5K
Facilitated Diffusion
1.5K
The plasma membrane, a critical structure in cellular biology, houses an array of transporters, or carrier proteins, interspersed within its lipid bilayer. These proteins play a crucial role in solute transport through facilitated diffusion, a form of passive diffusion that uses transporters to move the molecules across the membrane.
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
1.5K
Membrane Transporters
18.7K
Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
18.7K
Drug Absorption Mechanism: Carrier-Mediated Membrane Transport
6.7K
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...
6.7K
The Significance of Membrane Transport
43.5K
The transport of solutes across the cell membrane is essential for metabolic processes, like maintaining cell size and volume, generating the action potential, exchanging nutrients and gases, etc. Membrane transport can be either passive or active. It can be simple diffusion, facilitated, or mediated transport aided by transport proteins such as transporters and channels.
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...
43.5K
Active Transport
2.5K
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...
2.5K
