Chemists unlock potential target for drug development

January 19, 2012
Chemistry professor Dana Spence, right, is seen working in his lab with a graduate student. Credit: MSU University Relations

A receptor found on blood platelets whose importance as a potential pharmaceutical target has long been questioned may in fact be fruitful in drug testing, according to new research from Michigan State University chemists.

A team led by Dana Spence of MSU's Department of Chemistry has revealed a way to isolate and test the receptor known as P2X1. By creating a new, simple method to study it after blood is drawn, the team has unlocked a potential new for many diseases that impact , such as diabetes, hypertension and .

Researchers can evaluate the receptor not only in developing but also re-testing existing medications that could work now by attaching to the receptor.

"Scientists are always looking for new 'druggable' in the human body," Spence said. "This receptor, P2X1, has long been viewed as not important in platelets; our studies show that is not necessarily true. The receptor is very active; you just need to be careful in working with it."

The research is published in the current issue of , a journal from the Royal Society of Chemistry in London.

The main job of platelets is to help prevent bleeding via clotting, Spence said. They work by getting sticky in the bloodstream, but the problem with some diseases such as diabetes or sickle-cell anemia is that the platelets get sticky even when they shouldn't, preventing proper blood flow and blocking vessels.

Platelets are activated when their receptors are "turned on"; currently, researchers have always focused on the P2Y receptor, which is easily studied. On the other hand, the P2X1 receptor was not thought to play a major role in platelet activation, and it proved very troublesome to study since it became desensitized once blood is drawn from the body, Spence said.

Though scientists tried a pair of methods to get around that issue – by using different additives or enzymes – the results did not prove fruitful in studying the receptor.

What Spence and his team found is that by adding a simple molecule called NF449 – originally thought to block the receptor – they were able to activate the P2X1 receptor in platelets after a blood draw.

"We have discovered a way to prepare and handle platelets so that we can study the receptor authentically," he said. "This research opens up new avenues of study and will allow researchers and pharmaceutical companies to re-appraise this receptor as a druggable target."

Explore further: New molecule could be key to anti-heart attack drug

More information: The research paper can be found at Analytical Methods at

Related Stories

New molecule could be key to anti-heart attack drug

April 18, 2008

When too many blood platelets stick together in the bloodstream, they form dangerous clots that can clog blood vessels and cause a heart attack. If a clot doesn’t get dissolved or rapidly removed, it can cause permanent ...

How life-threatening blood clots take hold

April 16, 2009

When plaques coating blood vessel walls rupture and expose collagen, platelets spring into action to form a blood clot at the damaged site. Now, a new report in the April 17th issue of the journal Cell, a Cell Press publication, ...

Method for manufacturing patient-specific human platelets

November 22, 2010

Skin cells from humans can be revamped into pro-clotting cells called platelets, according to a study published on November 22 in the Journal of Experimental Medicine. Patients with diseases causing thrombocytopenia—platelet ...

Recommended for you

A new form of real gold, almost as light as air

November 25, 2015

Researchers at ETH Zurich have created a new type of foam made of real gold. It is the lightest form ever produced of the precious metal: a thousand times lighter than its conventional form and yet it is nearly impossible ...

Getting under the skin of a medieval mystery

November 23, 2015

A simple PVC eraser has helped an international team of scientists led by bioarchaeologists at the University of York to resolve the mystery surrounding the tissue-thin parchment used by medieval scribes to produce the first ...

Moonlighting molecules: Finding new uses for old enzymes

November 27, 2015

A collaboration between the University of Cambridge and MedImmune, the global biologics research and development arm of AstraZeneca, has led researchers to identify a potentially significant new application for a well-known ...


Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.