New perspective in ion channel indicates treatment potential

Jul 09, 2010
New perspective in ion channel indicates treatment potential
A computer modelling of toxin and channel interaction

Scientists researching a toxin extracted from the venom of the honey bee have used this to inform the design of new treatments to alleviate the symptoms of conditions such as muscular dystrophy, depression and dementia.

Apamin, a natural peptide toxin found in bee venom, is known for its ability to block a type of that enables a high-speed and selective flow of out of nerves. The blocking of these channels in the brain causes nerves to become hyperexcitable, producing improved learning, which could have implications for the treatment of dementia and depression. In addition, injection of apamin improves the symptoms experienced by sufferers of myotonic (MD).

Until now, the exact mechanism by which apamin acts was poorly understood.  In a study published in the , two teams from the University of Bristol and the University of Liege in Belgium describe the results of their joint work on these KCa2 potassium ion channels, also called SK channels. 

Using computer models and a genetic approach, the researchers were able to pinpoint exactly where apamin binds to block the channel.  To block ion channels, most molecules act as a plug at their external mouth.  The researchers have discovered that apamin binds away from the channel pore, and causes the shape of the channel to change through an ‘allosteric’ mechanism, resulting in block.

This discovery could accelerate research into the design of new SK channel blockers which could imitate the action of apamin, to target SK channels in neural and muscular conditions such as , depression or MD. 

Professor Neil Marrion, from the University of Bristol’s Physiology & Pharmacology department, said: “Drug design depends on knowing the target.  Our findings have provided a new approach to designing a therapeutic agent that could help with the treatment of a number of conditions.”

Professor Vincent Seutin, from the GIGA Neurosciences at the University of Ličge, added: “I am very enthusiastic about the results of our study and I believe that, with the help of this piece of information, the targeting of these channels for the development of future drugs has been made easier.”

Explore further: Following a protein's travel inside cells is key to improving patient monitoring, drug development

Related Stories

Unraveling the mysteries of poison

Apr 13, 2006

Researchers from the Max Planck Institite for Biophysical Chemistry and other German and French colleagues have combined magnetic resonance spectroscopy (solid-state NMR) with special protein synthesis procedures to uncover ...

Complex channels

Jan 24, 2007

The messages passed in a neuronal network can target something like 100 billion nerve cells in the brain alone. These, in turn communicate with millions of other cells and organs in the body. How, then, do whole cascades ...

Revolution in understanding of ion channel regulation

Jan 30, 2008

A study at Rush University Medical Center in Chicago published this week in the online version of Biophysical Journal proposes that bubbles may control the opening and closing of ion channels. This new understanding of the ...

Modeling Cell 'Doors' Could Aid Drug Development

Jan 18, 2007

To open the door for better medicines, University of Pittsburgh assistant professor Michael D. Grabe thought he first needed to open the 'doors,' or channels, that allow for passage in and out of cells to see what science ...

Recommended for you

New method to analyse how cancer cells die

15 minutes ago

(Phys.org) —A team from The University of Manchester – part of the Manchester Cancer Research Centre - have found a new method to more efficiently manufacture a chemical used to monitor cancer cells.

The anti-inflammatory factory

Apr 22, 2014

Russian scientists, in collaboration with their colleagues from Pittsburgh University, have discovered how lipid mediators are produced. The relevant paper was published in Nature Chemistry. Lipid mediators are molecules that p ...

User comments : 0

More news stories

Phase transiting to a new quantum universe

(Phys.org) —Recent insight and discovery of a new class of quantum transition opens the way for a whole new subfield of materials physics and quantum technologies.

Imaging turns a corner

(Phys.org) —Scientists have developed a new microscope which enables a dramatically improved view of biological cells.