External action of di- and polyamines on maxi calcium-activated potassium channels: an electrophysiological and molecular modeling study

Biophysical Journal
T WeigerA Hermann

Abstract

In this study we compared polyamines to various diamines, and we modeled flexibility as well as hydrophobicity properties of these molecules to examine possible structural differences that could explain their external effects on the channels. The natural polyamines (putrescine, cadaverine, spermidine, spermine) and diamines increasing in CH2 chain length from C2 to C12 were used to probe maxi calcium-activated potassium (BK) channels in GH3 pituitary tumor cells when applied extracellularly. In single-channel recordings we found polyamines as well as diamines up to 1,10-diaminodecane to be ineffective in altering channel current amplitudes or kinetics. In contrast, 1,12-diamino dodecane (1,12-DD) was found to be a reversible blocker, with a blocking site at an electrical distance (z delta) of 0.72 within the channel. It reduced single-channel current amplitude, mean channel open time, and channel open probability. In computer simulations structural data, such as flexibility, hydration, and log D values, were calculated. 1,12-DD showed the largest flexibility of all diamines (minimum N-N distance 9.9 A) combined with a marked hydrophobicity due to a 4-5 A hydrophobic intersegment between hydrophilic ends in the molecule, as conf...Continue Reading

References

Apr 1, 1978·The Journal of Physiology·E Neher, J H Steinbach
Mar 1, 1991·The Journal of Physiology·J CopelloL Reuss
Aug 1, 1989·The Journal of Membrane Biology·M CornejoW B Guggino
Mar 1, 1986·The Biochemical Journal·A E Pegg
Dec 1, 1988·Pflügers Archiv : European journal of physiology·A VillarroelR Latorre
Jun 1, 1973·The Journal of General Physiology·A M Woodhull
Jul 1, 1984·The Journal of General Physiology·A L Blatz, K L Magleby
Aug 1, 1995·Pflügers Archiv : European journal of physiology·M Gomez, P Hellstrand
Jan 1, 1995·Annual Review of Pharmacology and Toxicology·D M Rock, R L Macdonald
Apr 1, 1993·Trends in Neurosciences·R H ScottA C Dolphin
Jun 1, 1994·The Journal of Membrane Biology·T Weiger, A Hermann

❮ Previous
Next ❯

Citations

Jun 6, 2003·European Journal of Biochemistry·Rui WangLingyun Wu
Mar 6, 2013·Molecular Pharmaceutics·Monica Sala-RabanalColin G Nichols
Mar 9, 2004·Biochimica Et Biophysica Acta·Mauro Salvi, Antonio Toninello
Oct 4, 2006·Free Radical Biology & Medicine·Irina G SavaAntonio Toninello
Mar 29, 2000·Journal of Molecular Biology·R IyerA H Delcour
Mar 7, 2021·International Journal of Molecular Sciences·Adonis Z WuSheng-Nan Wu
Apr 19, 2003·The Journal of Experimental Biology·S H RolenJ Caprio
May 18, 1999·Archives of Biochemistry and Biophysics·L Dalla ViaA Toninello
Sep 14, 2007·International Journal of Biological Macromolecules·Nasrollah Rezaei-GhalehMohsen Nemat-Gorgani
Jul 17, 2010·Fungal Genetics and Biology : FG & B·Cecilia AbreuAna Ramon

❮ 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.