New drugs in the pipeline for public health diseases

Swedish chemists synthesizing substances for blood clots, malaria, and hepatitis C.


Chemists at Linköping University in Sweden have developed three types of molecules, protease inhibitors, that can be further developed into drugs for cardiovascular diseases, malaria, and hepatitis C.

Proteases are a group of enzymes that play a major role in the course of certain diseases. If there is a molecule present that prevents the protease from working, the disease can be cured. Such substances are called inhibitors and are already in use in many drugs today.

Per-Ola Johansson, a doctoral candidate in organic chemistry, describes in his dissertation the synthesis of such protease inhibitors, designed for potential use in combating three different diseases: cardiovascular diseases (to prevent the formation of blood clots), malaria, and chronic jaundice of the type hepatitis C.

Thrombin is a protease that plays a key role when blood coagulates. In some individuals this process is hyperactive, which can lead to the formation of blood clots. The research team at Linköping University has synthesized a series of molecules that inhibit the activity of thrombin in varying degrees. The most active of these molecules give an indication of how to go about creating the optimal thrombin inhibitor to develop a functioning drug.

Malaria, which affects some 500 million people annually, killing nearly 2 million of them, is caused by a single-cell parasite that breaks down the hemoglobin in red blood corpuscles. For tools, the parasite makes use of a number of different protease enzymes. The research team has developed a large number of molecules that inhibit the activity of two of these, plasmepsin I and II. Some of these inhibitors have proven to be extremely effective and could be optimized to become a powerful new malaria drug.

Hepatitis C is caused by the virus HCV. When it proliferates, HCV forms a chain-shaped molecule that is cut in smaller pieces by various protease enzymes, and these pieces then build up new virus particles. The team has synthesized a series of inhibitors of NS3, one of the most important of these enzymes.

This work has been carried out under the supervision of Professor Ingemar Kvarnström, Professor Bertil Samuelsson, and Åsa Rosenquist, Ph.D., and in collaboration with the pharmaceutical companies Medivir and Astra Zeneca.

The dissertation is titled Design and synthesis of inhibitors that target the serine protease thrombin, the malarial aspartyl proteases plasmepsin I and II, and the hepatitis C virus NS3 serine protease.

Media Contact

Åke Hjelm alfa

More Information:

http://www.liu.se

All latest news from the category: Life Sciences and Chemistry

Articles and reports from the Life Sciences and chemistry area deal with applied and basic research into modern biology, chemistry and human medicine.

Valuable information can be found on a range of life sciences fields including bacteriology, biochemistry, bionics, bioinformatics, biophysics, biotechnology, genetics, geobotany, human biology, marine biology, microbiology, molecular biology, cellular biology, zoology, bioinorganic chemistry, microchemistry and environmental chemistry.

Back to home

Comments (0)

Write a comment

Newest articles

Superradiant atoms could push the boundaries of how precisely time can be measured

Superradiant atoms can help us measure time more precisely than ever. In a new study, researchers from the University of Copenhagen present a new method for measuring the time interval,…

Ion thermoelectric conversion devices for near room temperature

The electrode sheet of the thermoelectric device consists of ionic hydrogel, which is sandwiched between the electrodes to form, and the Prussian blue on the electrode undergoes a redox reaction…

Zap Energy achieves 37-million-degree temperatures in a compact device

New publication reports record electron temperatures for a small-scale, sheared-flow-stabilized Z-pinch fusion device. In the nine decades since humans first produced fusion reactions, only a few fusion technologies have demonstrated…

Partners & Sponsors