Slow delayed rectifying potassium current (IKs ) - analysis of the in vitro inhibition data and predictive model development

Journal of Applied Toxicology : JAT
Sebastian PolakAleksander Mendyk

Abstract

The excitable cell membranes contain ion channels that allow the ions passage through the specific pores via a passive process. Assessment of the inhibition of the IKr (hERG) current is considered to be the main target during the drug development process, although there are other ionic currents for which drug-triggered modification can either potentiate or mask hERG channel blockade. Information describing the results of in vitro studies investigating the chemical-IKs current interactions has been developed in the current study. Based on the publicly available data sources, 145 records were collected. The final list of publications consists of 64 positions and refers to 106 different molecules connected with IKs current inhibition, with at least one IC50 value measured. Ultimately, 98 of the IC50 values expressed as absolute values were gathered. For 36 records the IC50 was expressed as a relative value. For the 11 remaining records, the inhibition was not clearly expressed. Based on the collected data the predictive models for the IC50 estimation were developed with the use of various algorithms. The extended Quantitative Structure-Activity Relationships (QSAR) methodology was applied and the in vitro research settings were in...Continue Reading

References

Mar 4, 1998·British Journal of Pharmacology·A E BuschF Lang
Feb 15, 2000·Journal of Cardiovascular Pharmacology·S E JonesT F McDonald
Aug 5, 2000·European Journal of Pharmacology·P ZhabyeyevT F McDonald
Jan 4, 2001·Naunyn-Schmiedeberg's Archives of Pharmacology·H GögeleinA E Busch
Feb 28, 2002·Naunyn-Schmiedeberg's Archives of Pharmacology·Alexander BachmannAndreas E Busch
May 16, 2002·British Journal of Pharmacology·János MagyarPéter P Nánási
Aug 15, 2002·European Journal of Pharmacology·Sathapana KongsamutDavid Rampe
Jan 23, 2003·The Journal of Pharmacology and Experimental Therapeutics·Ignacio MorenoEva Delpón
May 31, 2003·Journal of Cardiovascular Pharmacology·Benoit DroletJacques Turgeon
Jun 12, 2003·European Journal of Pharmacology·János TakácsJulius Gy Papp
Jun 20, 2003·Molecular Pharmacology·Guiscard SeebohmMichael C Sanguinetti
Sep 11, 2003·The Journal of Pharmacology and Experimental Therapeutics·Morten B ThomsenMarc A Vos
Oct 8, 2003·British Journal of Pharmacology·Sergey MissanTerence F McDonald
Feb 21, 2004·European Journal of Pharmacology·Anthony A FossaBernard Fermini
Jul 28, 2004·British Journal of Pharmacology·Gernot SchramStanley Nattel
Mar 30, 2005·Neural Networks : the Official Journal of the International Neural Network Society·Athanassia ChalimourdaAlex J Smola
Apr 9, 2005·Journal of Cardiovascular Electrophysiology·Dimitar P ZankovMinoru Horie
Apr 9, 2005·Journal of Cardiovascular Electrophysiology·Frida PerssonIngemar Jacobson
Jun 28, 2005·British Journal of Pharmacology·Ricardo GómezEva Delpón
Nov 10, 2005·The Journal of Pharmacology and Experimental Therapeutics·Alexander N KatchmanSteven N Ebert
Dec 13, 2005·British Journal of Pharmacology·Miao TianGui-Rong Li
Feb 17, 2006·European Journal of Pharmacology·Clemens Möller, Rainer Netzer
Feb 24, 2006·Journal of Cardiovascular Pharmacology·Elena S TrepakovaJoseph J Salata
Aug 15, 2006·Neuropharmacology·Bo Hjorth BentzenSøren-Peter Olesen
Feb 6, 2008·IEEE Transactions on Neural Networks·S K ShevadeK K Murthy
Sep 2, 2008·American Journal of Physiology. Heart and Circulatory Physiology·John P ImredyJoseph J Salata
May 15, 2009·Journal of Pharmacological and Toxicological Methods·Rob TowartDavid J Gallacher
Aug 26, 2009·British Journal of Pharmacology·Joffrey DucroqM Le Grand
Oct 13, 2009·Journal of Cardiovascular Electrophysiology·Antonio E LacerdaArthur M Brown
Apr 22, 2010·Cardiovascular Therapeutics·Harry J Witchel
Jul 28, 2010·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Aleksander MendykRenata Jachowicz
Aug 3, 2010·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Hui LiuGui-Rong Li
Jan 13, 2011·Journal of Pharmacological and Toxicological Methods·Pascal ChamperouxJean-Yves Le Guennec

❮ Previous
Next ❯

Citations

Jul 5, 2012·Journal of Applied Toxicology : JAT·Barbara WiśniowskaSebastian Polak

❮ 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.

© 2022 Meta ULC. All rights reserved