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Related Concept Videos

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance01:07

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

Drug transporters are critical in drug absorption, distribution, and excretion processes. They should be included in physiological-based pharmacokinetic (PBPK) models, which help predict human drug disposition. However, predicting this is challenging during drug development, especially when liver transport is involved. However, with a realistic representation of body transport processes, an accurate model may be possible.
A recent model describes pravastatin's hepatobiliary excretion, mediated...
The Significance of Membrane Transport01:44

The Significance of Membrane Transport

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...
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters01:16

Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

The pharmacogenetics of drug transporters is increasingly recognized as a critical factor influencing interindividual variability in drug absorption, distribution, and elimination. These membrane-bound proteins regulate drugs' movement across cellular barriers by actively pumping them out (efflux) or facilitating their uptake (influx). Among the major transporter families, ATP-binding cassette (ABC) and solute carrier (SLC) transporters play particularly prominent roles. Genetic polymorphisms...
Induced-fit Model01:13

Induced-fit Model

Most chemical reactions in cells require enzymes—biological catalysts that speed up the reaction without being consumed or permanently changed. They reduce the activation energy needed to convert the reactants into products. Enzymes are proteins, that usually work by binding to a substrate—a reactant molecule that they act upon.
Enzymes exhibit substrate specificity, meaning that they can only bind to certain substrates. This is mainly determined by the shape and chemical characteristics of...
Allosteric Proteins-ATCase01:19

Allosteric Proteins-ATCase

Binding sites linkages can regulate a protein's function.  For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to  N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
Physiological Pharmacokinetic Models: Assumption with Protein Binding01:13

Physiological Pharmacokinetic Models: Assumption with Protein Binding

Physiological models with protein binding in pharmacokinetics offer a sophisticated approach to understanding drug disposition. These models consider drug-protein interactions, enabling them to effectively predict drug concentrations in different organs and tissues. This precision aids in accurate drug dosing, providing a significant advantage over conventional models. A key process within these models is equilibration, which ensures that drug concentrations achieve a steady state within the...

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Related Experiment Video

Updated: Jun 19, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
10:29

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

Predictive computational models of substrate binding by a nucleoside transporter.

Catharine J Collar1, Mohammed I Al-Salabi, Mhairi L Stewart

  • 1Department of Chemistry, Georgia State University, Atlanta, Georgia 30303, USA.

The Journal of Biological Chemistry
|October 8, 2009
PubMed
Summary

Researchers identified key structural features for inhibiting the P2 aminopurine transporter in Trypanosoma brucei. This discovery aids in designing new antiparasitic drugs by predicting compound interactions with transporters.

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Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time
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Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time

Published on: March 11, 2021

Related Experiment Videos

Last Updated: Jun 19, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
10:29

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time
08:33

Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time

Published on: March 11, 2021

Area of Science:

  • Parasitology and Drug Discovery
  • Computational Biology and Molecular Modeling

Background:

  • Drug transporters are crucial for antiparasitic drug efficacy and resistance.
  • The P2 aminopurine transporter is essential for Trypanosoma brucei uptake of drugs like melarsoprol and diamidines.

Purpose of the Study:

  • To investigate the structural basis of P2 aminopurine transporter inhibition by various compounds.
  • To develop predictive models for identifying novel antiparasitic drug candidates targeting this transporter.

Main Methods:

  • Determined inhibition constants (K(i)) for diverse compounds using competition experiments with [(3)H]adenosine.
  • Employed computational biology to analyze structure-activity relationships and build predictive models for transporter inhibition.

Main Results:

  • Identified a common pharmacophore and key structural characteristics responsible for P2 transporter inhibition.
  • Developed a predictive model for compound interaction with the P2 transporter based on structural features.

Conclusions:

  • The study provides molecular insights into P2 transporter inhibition mechanisms.
  • The developed model serves as a quantitative tool for designing novel antiparasitic compounds targeting specific transporters without requiring protein structural data.