FKBP51 protein is produced throughout the body — primarily in the brain, skeletal muscle, and adipose tissue. It also performs several functions, including glucose processing and stress management. This has led researchers to suggest that the FKBP51 protein may be involved in the occurrence of multiple conditions.
The difficulty for researchers concluded that the FKBP51 protein is very similar in structure to the FKBP52 protein. Scientists have discovered that FKBP51 can change its shape in the way that FKBP52 cannot, and this allowed them to develop highly selective inhibitors. When mice were treated with SAFit2 – an inhibitor of FKBP51 – they experienced less stress. Animals were also less likely to gain weight, which is believed to be associated with a decrease in appetite. In addition, the animals returned to normal glucose levels and decreased pain.
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“FKBP51 protein plays an important role in the development of depression, obesity, diabetes, and chronic pain,” says Dr. Felix Hausch. “We have developed a highly effective, highly selective inhibitor of the protein FKBP51 called SAFit2, which is now being tested in mice. Further suppression of the FKBP51 protein may become a new therapeutic agent for the treatment of the above conditions. "
Scientists hope that the results will lead to the development of new treatments for people, and are currently testing inhibitors of FKBP51 in the treatment of alcoholism and cancer. Doctors believe that FKBP51 inhibitors can be used when a patient’s tumor has mutated so much that it has become impossible to treat with the help of existing anti-cancer drugs.