Related Experiment Video

Updated: Mar 22, 2026

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
08:59

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment

Published on: December 3, 2020

8.9K

Expression Patterns of Organic Anion Transporting Polypeptides 1B1 and 1B3 Protein in Human Pediatric Liver

Margaret M S Thomson1, Ronald N Hines1, Erin G Schuetz1

  • 1Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, Tennessee (M.M.S.T., B.M.); Department of Pediatrics, Medical College of Wisconsin, Milwaukee, Wisconsin (R.N.H.); and Department of Pharmaceutical Sciences, St. Jude Children's Research Hospital Memphis, Tennessee (E.G.S.).

Drug Metabolism and Disposition: the Biological Fate of Chemicals
|April 22, 2016
PubMed

Insights

Pediatric drug disposition is complex. This study reveals that organic anion transporting polypeptide 1B3 (OATP1B3) expression changes significantly with age in children, impacting drug therapy.

Area of Science:

  • Pharmacology
  • Pediatrics
  • Biochemistry

Background:

  • Drug disposition pathways in children are not fully understood, complicating pharmacotherapy.
  • Ontogeny of drug-metabolizing enzymes and transporters is crucial for pediatric drug development.
  • Uptake transporters like organic anion transporting polypeptide (OATP) 1B1 and 1B3 play a key role in drug transport.

Purpose of the Study:

  • To assess the developmental pattern of OATP1B1 and OATP1B3 protein expression in pediatric liver specimens.
  • To understand the ontogeny of OATP1B1 and OATP1B3 in relation to age.

Main Methods:

  • Relative protein quantification using Western blotting.
  • Analysis of 80 human pediatric liver specimens from 9 days to 12 years of age.
  • Comparison of OATP1B3 expression across different pediatric age groups.

Main Results:

  • OATP1B3 showed high expression at birth, decreasing in early infancy, and increasing in preadolescence.
  • Relative OATP1B3 expression was significantly higher in infants (<3 months) compared to older children.
  • OATP1B1 exhibited high interindividual variability but no significant age-related expression changes.

Conclusions:

  • OATP1B3 expression undergoes significant ontogenic changes in children, influencing drug disposition.
  • Both transcriptional and post-translational modifications contribute to OATP1B3 developmental patterns.
  • Understanding OATP ontogeny is vital for optimizing pediatric pharmacotherapy.

More Related Videos

Human Liver Spheroids from Peripheral Blood for Liver Disease Studies09:51

Human Liver Spheroids from Peripheral Blood for Liver Disease Studies

Published on: January 27, 2023

2.3K
Isolation of Primary Human Proximal Tubule Epithelial Cells and Their Use in Creating a Microphysiological Model of the Renal Proximal Tubule07:06

Isolation of Primary Human Proximal Tubule Epithelial Cells and Their Use in Creating a Microphysiological Model of the Renal Proximal Tubule

Published on: May 9, 2025

987

Related Concept Videos

Pharmacokinetics in Pediatric Patients: Drug Metabolism01:24

Pharmacokinetics in Pediatric Patients: Drug Metabolism

In pediatric care, understanding the nuances of hepatic drug metabolism is crucial, as it significantly differs from that of adults. This divergence is primarily due to the developmental stage of drug-metabolizing enzymes, which affects how medications are processed in the body. In neonates, for instance, the activity of Phase I enzymes—critical for the initial breakdown of drugs—is markedly reduced, functioning at just 20–40% of the levels seen in adults. This reduction poses...
317
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...
105
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...
1.5K
ABC Transporters: Exporter01:31

ABC Transporters: Exporter

ATP-binding cassette or ABC transporter is the largest superfamily of integral membrane proteins. The transporters have transmembrane-binding domains (TMDs) and nucleotide-binding domains (NBDs). The TMDs are specific to their substrates, whereas the NBDs are similar to engines that complete ATP hydrolysis to complete the substrate transport. They can be full transporters consisting of two TMDs and NBDs, half transporters with one TMD and NBD, while some encoded with a single TMD or NBD are...
7.1K
Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption01:23

Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption

Understanding the physiological differences in the pediatric population is crucial for effective pharmacotherapy. Neonates, infants, and children exhibit significant variations in gastric pH, gastric emptying time, intestinal transit time, and biliary function. These variations profoundly affect oral drug absorption, necessitating a nuanced approach to pediatric dosing.Neonates present with a unique physiological profile, having a gastric pH greater than 4 and faster and more irregular gastric...
669
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,...
370