Pharmacological characterization of the ATP-dependent low K(m) guanosine 3',5'-cyclic monophosphate (cGMP) transporter in human erythrocytes

Biochemical Pharmacology
Elisabeth SundkvistGeorg Sager

Abstract

The efflux pump for cGMP has been shown to be an ATP-energized multiorganic anion transporter. The present study was performed to extend the knowledge of the pharmacological characteristics of this efflux pump. Inside-out vesicles prepared from fresh blood were incubated with [3H]-cGMP (1 microM) with or without various concentrations of competitors for 120min at 37 degrees. The tested compounds could be divided in four groups: one with high affinity (K(i) < 5 microM), a second with moderate affinity (K(i): 5-50 microM), a third with low affinity (K(i): 0.1-5mM) and the fourth with extremely low or no affinity at all. With the mean K(i)-values given in parenthesis, the high affinity group consisted of mifepristone (0.2 microM), zaprinast (0.35 microM), dipyridamole (0.35 microM), estradiol 3-beta-glucuronide (0.42 microM), genistein (0.43 microM), estradiol 17-beta-glucuronide (0.47 microM), onapristone (1.3 microM), progesterone (1.7 microM) and sildenafil (3.6 microM). The inhibitors with medium affinity were estradiol (8 microM), sulfinpyrazone (13 microM), daunorubicin (23 microM), megestrol acetate (26 microM), doxorubicin (28 microM), 6-thioguanine (28 microM) and 6-thioguanosine-5'-monophosphate (32 microM). The low affi...Continue Reading

References

Jan 1, 1984·Journal of Receptor Research·R M LandmannF R Bühler
Dec 20, 1994·Proceedings of the National Academy of Sciences of the United States of America·M MüllerP L Jansen
Jul 1, 1996·Scandinavian Journal of Clinical and Laboratory Investigation·G SagerK E Kjørstad
Jun 7, 2000·Proceedings of the National Academy of Sciences of the United States of America·J WijnholdsP Borst
Jul 13, 2000·The Journal of Biological Chemistry·G JedlitschkyD Keppler

❮ Previous
Next ❯

Citations

Mar 22, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Georg SagerCatharina Engström
Sep 3, 2003·European Journal of Biochemistry·Antonios KlokouzasStephen B Hladky
Jan 22, 2008·Arthritis Research & Therapy·Barthold Deiters, Peter Prehm
Nov 22, 2011·Chinese Journal of Cancer·Kamlesh SodaniZhe-Sheng Chen
Apr 6, 2006·Pflügers Archiv : European journal of physiology·Piet BorstKoen van de Wetering
Oct 6, 2005·International Journal of Urology : Official Journal of the Japanese Urological Association·S Sirri BilgeSuleyman Celik
Mar 30, 2005·Biochemical Pharmacology·Chung-Pu WuMargery A Barrand
Oct 24, 2002·Neuroreport·Patrizia BalleriniFrancesco Caciagli
Oct 17, 2003·International Journal of Impotence Research·S H FrancisJ D Corbin
Mar 15, 2003·The Journal of Biological Chemistry·Peter R WielingaPiet Borst
Jun 15, 2013·American Journal of Physiology. Gastrointestinal and Liver Physiology·Othman Al-ShboulKarnam S Murthy
Jun 2, 2007·The Journal of Biological Chemistry·Tobias SchulzPeter Prehm
Jan 19, 2007·The FEBS Journal·Cornelia J F de WolfPiet Borst
Mar 4, 2008·The Journal of Experimental Biology·Jennifer M EvansShireen-Anne Davies
Aug 18, 2004·Neurochemistry International·Georg Sager
Jul 17, 2021·The Journal of Steroid Biochemistry and Molecular Biology·Sondre Ulstein OdlandGeorg Sager

❮ 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.

Related Papers

Neurochemistry International
Georg Sager
European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)
A OrboGeorg Sager
© 2022 Meta ULC. All rights reserved