German biochemists are developing a new approach against common ailments
A team of researchers from the TU Darmstadt is currently working on active ingredients that are to be used to combat widespread depression, chronic pain and obesity. The most important research results in brief:
- A certain protein is associated with chronic pain, obesity, and depression.
- The inhibition of the protein has led to disease relief in animal experiments.
- The active ingredient could help millions of people.
- Trials on humans are still pending.
The scientists, led by Felix Hausch, professor for structure-based drug research at the TU Darmstadt, discover a biochemical connection between chronic pain, obesity and depression. It is a protein called FKBP5, which plays a key role in energy metabolism, depression and chronic pain. The scientists are working on an active ingredient that blocks this protein molecule and thus reduces the suffering from the complaints mentioned. The study results were recently published in the "National Center for Biotechnology Information" (NCBI).
New active ingredient could help millions of people
The new active ingredients could represent a major breakthrough in the fight against diseases and could help a great many people. Because in Germany around four million people are affected by depression, according to the German Pain Society 16 million people suffer from chronic pain and on average every sixth German is affected by obesity (obesity).
Target for medication
Felix Hausch wants to use the protein FKBP51 as a target for medication. "If you block FKBP51, the tendency to depression, obesity and chronic pain should decrease," explains Hausch. The already approved pharmaceutical ingredient tacrolimus should serve as a starting point for the development of the inhibitors. Tacrolimus is a substance that is derived from bacteria and is already known to bind the protein FKBP51, among others.
Modification of the active ingredients
The scientists chemically modified the substance tacrolimus so that the protein is inhibited even better. In addition, the researchers made the change that only the protein FKBP51 is blocked and not similar protein molecules.
Two different active ingredient variants in production
The scientists are currently working with two different variants of the active ingredient. An active ingredient should aim to cross the blood-brain barrier and thus be effective against depression and chronic pain. The other variant should not get into the brain and should be optimized for use against obesity.
The first series of tests show positive results
The first series of tests on mice gave promising results and so far showed no side effects. In some mice, the researchers switched off the protein production of FKBP51 completely. Even these mice are doing surprisingly well, the researchers report. "They live for a similar length of time, move the same way and eat just as much as their non-manipulated peers," says the TU Darmstadt press release on the study results.
Eliminate chronic pain
According to Hausch, the scientists in animal experiments succeeded in specifically inhibiting chronic pain with FKBP51. The normal acute pain sensation was not impaired. "This is very important, because otherwise you burn your hand on the hot stove, for example," added Hausch.
When is it ready for the market?
The results so far are promising, but according to the researchers, drug development is far from over. "We still have to improve a few molecular properties," says Hausch. It would probably be a while before the substance was marketable, especially since the development effort is now growing exponentially. This includes, among other things, clinical tests on thousands of test subjects, which are a prerequisite for any drug approval. (vb)