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Related Concept Videos

Factors Affecting Protein-Drug Binding: Drug-Related Factors01:18

Factors Affecting Protein-Drug Binding: Drug-Related Factors

184
Drug binding to proteins is a complex phenomenon influenced by various drug-related factors, each playing a significant role in the interaction between drugs and proteins within the body.
One crucial factor in drug-protein binding is the drug's lipophilicity or its affinity for fat. More lipophilic drugs tend to have higher binding extents. For example, highly lipophilic drugs like cloxacillin exhibit substantial protein binding, with as much as 95% of the drug binding to proteins. In...
184
Protein-Drug Binding: Mechanism and Kinetics01:16

Protein-Drug Binding: Mechanism and Kinetics

856
Protein-drug binding refers to the interaction between drugs and proteins within the body. This binding process can occur intracellularly, involving drug interactions with enzymes or receptors within cells, or extracellularly, involving plasma proteins in the blood.
Various forces drive these interactions, including hydrogen bonds, hydrophobic interactions, ionic bonds, electrostatic interactions, and van der Waals forces. These bonds enable drugs to bind to specific sites on proteins,...
856
Factors Affecting Protein-Drug Binding: Protein-Related Factors01:20

Factors Affecting Protein-Drug Binding: Protein-Related Factors

245
Drug binding to proteins is a key aspect of pharmacokinetics and can influence a drug's distribution, absorption, and elimination in the body. Several factors, including the drug's physiochemical properties, protein concentration, disease states, and the number of binding sites on the protein, influence this process.
The physicochemical properties of a drug play a significant role in its ability to bind to proteins. Lipophilic drugs, which dissolve in fats, oils, and lipids, can be...
245
Factors Affecting Protein-Drug Binding: Drug Interactions01:23

Factors Affecting Protein-Drug Binding: Drug Interactions

262
Drug interactions are a critical aspect of pharmacology and can occur when two or more drugs compete for the same binding site. This competition can result in one drug displacing another, altering the effect of the displaced drug. Drug interactions are complex processes that rely heavily on how much of the displacer drug is present and how strongly it can bind to the same sites as the displaced drug.
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...
262
Factors Affecting Protein-Drug Binding: Patient-Related Factors01:29

Factors Affecting Protein-Drug Binding: Patient-Related Factors

108
Protein-drug binding, a pivotal aspect of pharmacokinetics, is subject to considerable variability influenced by an array of patient-related factors. The intricate interplay of age, individual differences, and pathological conditions significantly impact the binding dynamics and subsequent pharmacological effects.
Age stands as a key determinant in protein-drug binding. Neonates, characterized by low albumin content, experience heightened concentrations of unbound drugs such as phenytoin and...
108
Protein-protein Interfaces02:04

Protein-protein Interfaces

13.0K
Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a...
13.0K

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Related Experiment Video

Updated: Sep 3, 2025

Author Spotlight: A Computational Approach to Decipher Amino Acid Preferences in Multispecific Protein-Protein Interactions
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Protein Binding in Translational Antimicrobial Development-Focus on Interspecies Differences.

Hifza Ahmed1, Felix Bergmann1,2, Markus Zeitlinger1

  • 1Department of Clinical Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.

Antibiotics (Basel, Switzerland)
|July 27, 2022
PubMed
Summary

Plasma protein binding (PPB) is crucial for antibiotic development. This review covers PPB basics, its impact on antimicrobial activity and pharmacodynamics, and compares animal models to humans for better drug extrapolation.

Keywords:
antibioticsequilibrium dialysisfraction unboundinterspecies differencespharmacokineticsplasma protein bindingultracentrifugation

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Area of Science:

  • Pharmacology
  • Drug Development
  • Biochemistry

Background:

  • Plasma protein binding (PPB) significantly influences antibiotic properties like activity, clearance, and interactions.
  • Understanding PPB is vital for drug candidate assessment and clinical application.

Purpose of the Study:

  • To review the fundamentals of PPB, including key binding proteins (Albumin, AAG).
  • To examine PPB's effects on antibiotic antimicrobial activity and in vitro pharmacodynamic (PD) models.
  • To evaluate PPB differences between animal species and humans for improved preclinical translation.

Main Methods:

  • Literature review of PPB principles and methods.
  • Statistical analysis of PPB data across species (dog, rat, mouse, rabbit, monkey) versus humans.
  • Highlighting various PPB determination techniques (e.g., equilibrium dialysis, chromatography).

Main Results:

  • Significant differences in antibiotic PPB were observed between humans and dogs/mice.
  • No significant PPB differences were found between humans and rats/rabbits/monkeys.
  • Identified key methods for PPB determination with their respective pros and cons.

Conclusions:

  • PPB data in preclinical species like rats, rabbits, and monkeys may be more predictive for human outcomes.
  • This comparative analysis aids in selecting appropriate animal models for antibiotic drug development.
  • Accurate PPB assessment is essential for effective antibiotic PK/PD modeling and therapeutic index prediction.