Related Experiment Video

Updated: Oct 18, 2026

In vitro Organoid Culture of Primary Mouse Colon Tumors
07:33

In vitro Organoid Culture of Primary Mouse Colon Tumors

Published on: May 17, 2013

Function and expression of multidrug resistance-associated protein family in human colon adenocarcinoma cells

T Hirohashi1, H Suzuki, X Y Chu

  • 1Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo, Japan.

The Journal of Pharmacology and Experimental Therapeutics
|December 22, 1999
PubMed

Insights

Multidrug resistance-associated proteins (MRPs) in Caco-2 cells facilitate organic anion transport. The study demonstrates ATP-dependent uptake of DNP-SG and E217bG, suggesting cMOAT/MRP2

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cell Biology

Background:

  • Organic anions are actively transported across intestinal epithelial cells.
  • The multidrug resistance-associated protein (MRP) family plays a role in intestinal efflux.

Purpose of the Study:

  • To investigate the function and expression of MRP proteins in intestinal organic anion transport.
  • To examine the role of MRPs in the efflux of organic anions using Caco-2 cells.

Main Methods:

  • Utilized Caco-2 cells, a human adenocarcinoma cell line mimicking enterocytes.
  • Investigated uptake of [(3)H]2,4-Dinitrophenyl-S-glutathione (DNP-SG) and [(3)H]17beta-estradiol 17-beta-D-glucuronide (E(2)17betaG) into brush-border membrane vesicles (BBMVs).
  • Employed ATP-dependent transport assays, ATPase inhibitor studies, reverse-transcriptase polymerase chain reaction (RT-PCR), and Northern blot analysis.

Main Results:

  • Demonstrated ATP-dependent uptake of DNP-SG and E(2)17betaG in Caco-2 BBMVs.
  • RT-PCR detected MRP1, MRP3, and MRP5; Northern blot showed extensive expression of cMOAT/MRP2 and MRP3.
  • cMOAT/MRP2 was continuously expressed, while MRP3 expression followed confluency; MRP1 and MRP5 showed minimal expression.

Conclusions:

  • Caco-2 cells possess ATP-dependent transport systems for DNP-SG and E(2)17betaG.
  • The observed transport activity in BBMVs likely involves cMOAT/MRP2, potentially localized to the brush border.
  • MRP3 may be involved in basolateral transport, contributing to overall organic anion handling in intestinal cells.

More Related Videos

Methods to Study Epithelial Transport Protein Function and Expression in Native Intestine and Caco-2 Cells Grown in 3D11:27

Methods to Study Epithelial Transport Protein Function and Expression in Native Intestine and Caco-2 Cells Grown in 3D

Published on: March 16, 2017

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...
Tumor Progression02:07

Tumor Progression

Tumor progression is a phenomenon where the pre-formed tumor acquires successive mutations to become clinically more aggressive and malignant. In the 1950s, Foulds first described the stepwise progression of cancer cells through successive stages.
Colon cancer is one of the best-documented examples of tumor progression. Early mutation in the APC gene in colon cells causes a small growth on the colon wall called a polyp. With time, this polyp grows into a benign, pre-cancerous tumor. Further...
Abnormal Proliferation02:23

Abnormal Proliferation

Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the daughter...
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
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...
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...