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Related Concept Videos

Membrane Transporters01:31

Membrane Transporters

11.1K
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...
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Nonlinear Pharmacokinetics: Role of Transporters01:27

Nonlinear Pharmacokinetics: Role of Transporters

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A drug's nonlinear kinetics can be influenced by a diverse range of transporter proteins that serve as crucial players in drug distribution. These transporters, found within cells, can enhance or reduce local drug concentrations by facilitating the influx or efflux of drugs. For instance, the expression of xenobiotic transporters can be influenced by factors such as age and gender, potentially impacting the linearity of drug response.
Polymorphisms occurring in drug transporters can alter...
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The Significance of Membrane Transport01:44

The Significance of Membrane Transport

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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...
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Hepatic Drug Clearance: Role of Transporters01:14

Hepatic Drug Clearance: Role of Transporters

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In the liver and bile canaliculi, influx and efflux transporters modification can influence intrinsic clearance. Transporters play a significant role in moving drugs within liver cells. Elaborate models, such as the Biopharmaceutical Classification System (BCS), are essential to relate transporters to drug disposition. This system categorizes drugs into four classes based on solubility and permeability, providing insights into elimination routes and the effects of transporters following oral...
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Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

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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,...
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Author Spotlight: Expression and Purification of Human Solute Carrier Transporters Using Codon-Optimized Genes
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The Concise Guide to PHARMACOLOGY 2023/24: Transporters.

Stephen P H Alexander1, Doriano Fabbro2, Eamonn Kelly3

  • 1School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.

British Journal of Pharmacology
|December 20, 2023
PubMed
Summary
This summary is machine-generated.

The Concise Guide to Pharmacology 2023/24 offers a comprehensive overview of drug targets and their interactions. This biennial publication provides a citable record of pharmacological data, including transporters and G protein-coupled receptors.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biochemistry

Background:

  • The Concise Guide to Pharmacology is a biennial publication detailing drug targets and ligands.
  • Previous editions have been published since 2013/14.
  • The guide is a citable, point-in-time record of pharmacological data.

Purpose of the Study:

  • To provide an updated overview of approximately 1800 drug targets and 6000 interactions.
  • To offer concise, tabular summaries of key drug target properties.
  • To link to an open-access knowledgebase for detailed information.

Main Methods:

  • Compilation of data on drug targets and ligand interactions.
  • Categorization of targets into six major groups: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes, and transporters.
  • Inclusion of nomenclature guidance and information on pharmacological tools.

Main Results:

  • Details on approximately 1800 drug targets and over 6000 interactions with 3900 ligands.
  • Emphasis on selective pharmacology where available.
  • The guide is presented in a landscape format for easy comparison.

Conclusions:

  • The 2023/24 guide provides an essential, up-to-date reference for pharmacological information.
  • It serves as a permanent, citable record superseding previous editions.
  • Official IUPHAR classification and nomenclature for human drug targets are included.