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Related Concept Videos

Membrane Transporters01:31

Membrane Transporters

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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

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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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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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The Significance of Membrane Transport01:44

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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.
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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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Cellular Membranes and Drug Transport01:24

Cellular Membranes and Drug Transport

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Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
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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 2019/20: Transporters.

Stephen P H Alexander1, Eamonn Kelly2, Alistair Mathie3

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

British Journal of Pharmacology
|November 12, 2019
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Summary

The Concise Guide to Pharmacology 2019/20 offers a summary of 1800 human drug targets, including G protein-coupled receptors and enzymes. This biennial publication provides a citable record of pharmacology data, linking to a comprehensive online knowledgebase.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biomedical Science

Background:

  • The Concise Guide to Pharmacology is a biennial publication series.
  • It serves as a crucial resource for understanding human drug targets and their properties.
  • The 2019/20 edition builds upon previous iterations, offering updated information.

Purpose of the Study:

  • To provide a concise overview of approximately 1800 human drug targets.
  • To emphasize selective pharmacology and link to a detailed open-access knowledgebase (www.guidetopharmacology.org).
  • To offer a permanent, citable record of pharmacological data as of mid-2019.

Main Methods:

  • Compilation of data on nearly 1800 human drug targets.
  • 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, information on pharmacological tools, key references, and further reading suggestions.

Main Results:

  • Presents concise summaries of key properties for 1800 human drug targets.
  • Highlights selective pharmacology where available.
  • Provides links to the comprehensive www.guidetopharmacology.org knowledgebase for detailed information.

Conclusions:

  • The Concise Guide to Pharmacology 2019/20 serves as an essential, citable reference for drug targets.
  • It offers a valuable snapshot of pharmacological knowledge contemporary to mid-2019.
  • Collaboration with NC-IUPHAR ensures official nomenclature and classification for human drug targets.