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Related Concept Videos

Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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...
Drug Absorption Mechanism: Carrier-Mediated Membrane Transport01:19

Drug Absorption Mechanism: Carrier-Mediated Membrane Transport

Certain large, lipid-insoluble drug molecules that resemble amino acids, peptides, or glucose, require specialized carrier proteins to facilitate their diffusion across cell membranes. This transport can occur through either facilitated diffusion, which does not require energy input, or active transport, which does require energy input.
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport01:23

Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport

Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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...
Cellular Membranes and Drug Transport01:24

Cellular Membranes and Drug Transport

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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Related Experiment Video

Updated: Jun 28, 2026

High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies
07:10

High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies

Published on: September 29, 2023

Technologies for transporter drug discovery.

Adam B Weinglass1, Maria L Garcia, Gregory L Kaczorowski

  • 1Merck Research Laboratories, Department of Ion Channels, Rahway, New Jersey 07065, USA. adam_weinglass@merck.com

Channels (Austin, Tex.)
|November 8, 2008
PubMed
Summary
This summary is machine-generated.

Transporter proteins are key drug targets but hard to screen. This review covers new targets and technologies for transporter drug discovery and pharmacokinetic assessment.

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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

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Related Experiment Videos

Last Updated: Jun 28, 2026

High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies
07:10

High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies

Published on: September 29, 2023

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
18:57

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

Published on: October 17, 2013

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
08:31

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biochemistry

Background:

  • Transporters are crucial drug targets implicated in various diseases like asthma, cardiovascular conditions, diabetes, and neuroscience disorders.
  • The complex mechanisms of transporters pose significant challenges for developing high-throughput screening (HTS) methods.
  • Understanding transporter function is vital for effective drug development.

Purpose of the Study:

  • To provide an updated overview of potential transporter targets for drug discovery.
  • To evaluate existing and emerging technologies that facilitate transporter screening.
  • To assess the impact of these technologies on lead optimization and pharmacokinetic profiling.

Main Methods:

  • Literature review of recent advancements in transporter research.
  • Analysis of current high-throughput screening technologies for transporter assays.
  • Evaluation of methods for lead optimization and pharmacokinetic assessment of transporter modulators.

Main Results:

  • Identification of several promising transporter families as drug targets.
  • Discussion of technological innovations enabling more efficient transporter screening.
  • Assessment of how new technologies aid in optimizing drug candidates and predicting pharmacokinetics.

Conclusions:

  • Despite challenges, advancements in technology are improving transporter-targeted drug discovery.
  • Novel screening and optimization strategies are essential for leveraging transporters as therapeutic targets.
  • Further development of screening technologies will accelerate the discovery of drugs modulating transporter function for various diseases.