A protein called “FK506-binding protein 51” also called FKBP51 has an association with chronic pain, obesity & depression. A research group has created a compound which obstructs this protein effectively in mice, resulting in relief from chronic pain induces positive effects such as good mood. The new compound can also be applied for the treatment of brain cancer & alcoholism. The results of their research will be presented today at the National Meeting of the American Chemical Society.
The principal investigator of the project, Doctor Felix Hausch: “The FKBP51 protein plays an important role in depression, obesity, diabetes, and chronic pain states. We developed the first highly potent, highly selective FKBP51 inhibitor, called SAFit2, which is now being tested in mice. Inhibition of FKBP51 could thus be a new therapeutic option to treat all of these conditions.”
FKBP51 is extracted through various parts of the body like skeletal muscle tissue & brain. It has numerous effects such as protein has the potential for restricting the burning of fat & absorption of glucose. Hence it has an impact on stress responses as well.
However, there is a lot of resemblance between FKBP51 & its nearest protein cousin ‘FKBP52’. Hausch said: “These two proteins are very similar in structure, but they are doing opposing things in cells. We have this yin-yang situation. Selectivity between these two proteins is thought to be crucial, but this is hard to achieve since the two proteins are so similar. We discovered that FKBP51 can change its shape in a way that FKBP52 can’t, and this allowed the development of highly selective inhibitors.”
A lot of effort still needs to be put into getting FKBP51 inhibitors to a level where they can be employed as a drug agent in human testing. Meanwhile, the team is also discovering other applications of FKBP51 inhibitors. According to Hausch, “We may be able to resensitize them to different types of chemotherapy using these specific inhibitors,” he says.