生物介导药物输送:生物载体是否介导生物联体的吸收?
Ravi Tripathi1, Xiaoxiao Yang1, Dongning Liu1
1Department of Chemistry and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA, USA.
Journal of enzyme inhibition and medicinal chemistry
|September 8, 2025
概括
依赖的多种维生素运输体 (SMVT) 不能运输缺乏碳酸基的生物联体,这就挑战了它们在向癌症药物输送中的应用. 需要进一步的研究来了解生物联体运输机制.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 癌症治疗方法 癌症治疗方法
背景情况:
- 在癌细胞中,依赖的多维生素输送体 (SMVT) 过度表达.
- 生物合物正在通过SMVT探索针对性药物输送.
- 生物素合物缺乏用于SMVT识别所必需的碳基.
研究的目的:
- 通过实验验证SMVT是否携带生物联体.
- 研究生物化前药物的细胞内丰富机制.
- 评估卡基在中小企业中介运输中的作用.
主要方法:
- 使用SMVT过度表达癌细胞的细胞培养实验.
- 生物化CO前药物的细胞内丰富试验.
- 竞争测试使用过多的生物素.
- 评估缺乏碳酸基的生物素类似物.
主要成果:
- 在SMVT过度表达细胞中观察到产药丰富.
- 过多的生物素没有抑制前药物丰富,表明SMVT没有参与.
- 没有碳酸基的生物素类似物表现出多种效应,表明了替代的运输途径.
- 这些发现挑战了SMVT对生物联体的直接运输.
结论:
- SMVT不太可能是生物联体的载体.
- 碳基组对于SMVT对生物化化合物的识别至关重要.
- 需要进行进一步的研究,以阐明生物联体的运输机制,以便有效的药物输送.
相关概念视频
Carrier-Mediated Transport
1.2K
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...
1.2K
Drug Biotransformation: Overview
3.7K
Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
3.7K
Drug Biotransformation: Overview
2.5K
Biotransformation, also known as drug metabolism, is a vital physiological process that chemically alters drugs, facilitating their elimination from the body and terminating their action. This process involves two main phases: phase I and phase II reactions. Phase I reactions, including oxidation, reduction, and hydrolysis, introduce or unmask polar functional groups on the drug molecule, thereby increasing its water solubility. By enhancing water solubility, the drug becomes more hydrophilic...
2.5K
Drug Absorption Mechanism: Carrier-Mediated Membrane Transport
5.8K
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...
5.8K
Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport
1.6K
Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
1.6K
Bioavailability Enhancement: Drug Permeability Enhancement
191
Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
191


