Determination of p-glycoprotein ATPase activity using luciferase

Biological & Pharmaceutical Bulletin
Tamihide MatsunagaShigeru Ohmori

Abstract

We investigated whether P-glycoprotein (P-gp) ATPase activity of Caco-2 cell membranes could be estimated by measuring consumption of ATP using luciferin-luciferase reaction, and whether the results would be useful for assessment of the interactions between P-gp and drugs. The vanadate-sensitive ATPase activity of Caco-2 cell membranes was measured rapidly with high sensitivity using luciferin-luciferase reaction. Cyclosporin A, verapamil, digoxin and quinidine stimulated the ATPase activity concentration-dependently with Km values of 5.3, 0.9, 1.2 and 4.1 microM, respectively. These values except for digoxin were comparable with previous reports. The ATPase activity and P-gp mRNA expression in Caco-2 cells were induced by all-trans-retinoic acid, digoxin and levothyroxine, but not dexamethasone or rifampicin. This method was useful to assess interactions with P-gp and drugs, and was used to elucidate the mechanisms of interaction of levothyroxine and digoxin.

References

Jan 1, 1989·Proceedings of the National Academy of Sciences of the United States of America·C Cordon-CardoJ R Bertino
May 1, 1988·Cancer·S Retsas, A R Gershuny
Feb 1, 1995·Journal of Bioenergetics and Biomembranes·G A Scarborough
Jan 26, 1996·The Journal of Biological Chemistry·M MüllerB Sarkadi
Mar 4, 1997·Proceedings of the National Academy of Sciences of the United States of America·A SparreboomO van Tellingen
Feb 7, 1998·The Journal of Clinical Investigation·R B KimG R Wilkinson
May 20, 1999·Annual Review of Pharmacology and Toxicology·S V AmbudkarM M Gottesman
Oct 21, 1999·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·M VerschraagenJ H Beijnen
Apr 28, 2000·International Journal of Clinical Pharmacology and Therapeutics·U I SchwarzW Kirch
Feb 22, 2002·International Journal of Cancer. Journal International Du Cancer·Xavier DeclèvesJean-Michel Scherrmann
Mar 14, 2002·Biochemical and Biophysical Research Communications·Kohji TakaraTeruyoshi Yokoyama
Sep 18, 2002·Clinical Pharmacology and Therapeutics·Werner SiegmundHeyo K Kroemer
Mar 11, 2003·The Journal of Pharmacy and Pharmacology·Arabelle PfrunderJürgen Drewe
Apr 3, 2003·The Journal of Biological Chemistry·Ina L UrbatschAlan E Senior
Apr 18, 2003·Journal of Medicinal Chemistry·Dietmar SchwabJörg Huwyler
May 27, 2003·The Journal of Pharmacology and Experimental Therapeutics·Jasminder SahiEdward L LeCluyse
Sep 2, 2003·Pharmaceutical Research·Michael D PerloffDavid J Greenblatt
Apr 10, 2004·Drug Metabolism Reviews·Shufeng ZhouBalram Chowbay

❮ Previous
Next ❯

Citations

Jan 24, 2014·Marine Drugs·Dioxelis Lopez, Sergio Martinez-Luis
Sep 5, 2012·Analytical and Bioanalytical Chemistry·Umit Hakan YildizBo Liedberg
Oct 3, 2018·Current Medicinal Chemistry·Jiahua CuiLarry M C Chow

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.