TAILIEUCHUNG - Assessment of the dissociation energetics of some selected ligand drugs bound on human serum albumin by differential scanning calorimetry

Drug-protein binding may play a role in the thermal energetics of protein denaturation and could lead to the determination of its equilibrium dissociation parameter. The aim of this study was to assess the energetics of a drug that was bound to human serum albumin (HSA) during thermal denaturation. Drugs that were bound at a single high-affinity primary binding site on HSA, including diazepam and ibuprofen, were employed. Commercial HSA was treated with charcoal to remove stabilizers and adjusted to 20% w/v in a pH buffered solution. Serial concentrations of individual drugs up to mmole/g-protein were added to the cleaned HSA solutions whereas diazepam was added to a commercial HSA solution. Samples were subjected to differential scanning calorimetry (DSC) set to run from 37 to 90°C at °C/min. Binding of the drug slightly increased the denaturing temperature of the cleaned HSA due to a shift in the equilibrium toward the native protein bound with the drug. Diazepam depressed the denaturing temperature of the commercial HSA by competing with the stabilizers already bound to the primary site of the HSA. | Nội dung Text Assessment of the dissociation energetics of some selected ligand drugs bound on human serum albumin by differential scanning calorimetry

• Y khoa - Dược
• Human serum albumin
• Lumry Eyring model
• Differential scanning calorimetry
• Dissociation energetics
• Human serum albumin
• BMC Chemistry
• Bovine serum albumin
• Principal binding site
• UV spectrophotometric
• Journal of Chemistry
• Bovine serum albumin binding
• Site selective binding
• Drug systems
• BMC Pediatrics
• Varicella vaccine
• Non inferiority
• HSA containing vaccine
• Injection vial walls
• Fluorescence quenching
• Molecular docking
• UV–vis absorption
• Tritium labelling method
• Interphase between subunits
• Accessible surface
• Space structure
• Biochemistry
• molecular Biology
• biological cells
• human serum
• genetics
• Scientific reports
• scientific research
• Medical Research
• chemical reaction
• BMC Pharmacology and Toxicology
• Type 2 diabetes
• β cell function
• Promoted β cell proliferation
• breast cancer
• medicine
• allosterically
• spectroscopic
• intermediate cells
• Report medicine
• traditional medicine
• Antimicrobial
• cell structure
• medical knowledge
• cytoplasm
• analysis of cytoplasmic
• trình bày báo cáo
• tài liệu báo cáo khoa học
• báo cáo y học
• nghiên cứu y học
• kiến thức y học
• oxidation
• tumor cells
• Structural biochemistry
• Structural Biology
• hemoglobin
• BMC Cancer
• Clinical trials
• Drug related toxicities
• Prophylactic management
• Randomized controlled trials