Depression, obesity and chronic pain can be treated by blocking the same protein & # 39;
- Scientists blocked the FKBP51 protein for the first time without affecting others
- Hope will lead to treatment in humans; FKBP51 is also being tested in cancer
- FKBP51 has many functions, from regulating glucose to managing stress
Depression, obesity and chronic pain could be treated by targeting the same protein, the research suggests.
One study found that blocking FKBP51 in mice relieved chronic pain, increased mood and stimulated weight loss.
This is the first time scientists are able to target this particular protein without affecting the function of others.
The researchers hope their study will lead to new treatments in humans, with FKBP51 inhibitors also being tested in alcoholism and cancer.
Depression, obesity and chronic pain could be treated by targeting the same protein (stock)
The research was conducted by the Technical University of Darmstadt, Germany, and led by Dr. Felix Hausch, professor of structure-based drug discovery.
"FKBP51 protein plays an important role in depression, obesity, diabetes and chronic pain states," Hausch said.
We developed the first highly potent and highly selective inhibitor FKBP51, called SAFit2, which is being tested in mice.
"Inhibition of FKBP51 could therefore be a new therapeutic option to treat all these conditions."
FKBP51 is expressed throughout the body, including in the brain, skeletal muscle tissue and fat.
It also has several roles, from regulating glucose uptake to controlling stress.
This has led researchers to believe that FKBP51 may be involved in the emergence of numerous conditions.
"I was intrigued by the peculiar regulatory role it seemed to play in cells," Hausch said.
WHAT IS DEPRESSION?
While it is normal to feel now and then, people with depression may feel persistently unhappy for weeks or months on end.
Depression can affect anyone at any age and is fairly common – about one in ten people will probably experience it at some point in their life.
Depression is a genuine health condition that people can not simply ignore or "get out of this".
The symptoms and effects vary but may include feeling constantly disturbed or hopeless or losing interest in the things you used to like.
It can also cause physical symptoms, such as sleep problems, tiredness, lack of appetite or sexual desire, and even physical pain.
In extreme cases, it can lead to suicidal thoughts.
Traumatic events can trigger you, and people with a family history may be more at risk.
It is important to see a doctor if you feel that you or someone you know has depression because it can be given with lifestyle changes, therapy, or medication.
Source: NHS Choices
And there was a known natural product that could serve as a starting point.
"Collectively, this seemed like an interesting protein to work on."
The difficulty was FKBP51 looks a lot like your & # 39; protein cousin & # 39; FKBP52.
"These two proteins are very similar in structure, but they are doing opposing things in cells," Hausch said.
& # 39; We have this yin-yang situation.
The selectivity between these two proteins is considered crucial, but this is difficult to achieve, since the two proteins are so similar.
"We found that FKBP51 can change its shape in a way that FKBP52 can not and that has allowed the development of highly selective inhibitors."
When rats were treated with SAFit2 – the main inhibitor of FKBP51 – they experienced less stress.
The animals were also less likely to gain weight, which is thought to be due to them having a reduced appetite.
And they had normal glucose levels and reduced pain as a result of treatment.
The full results will be presented at the American Chemical Society Spring 2019 conference in Orlando today.
But Dr. Hausch added that much more needs to be done before SAFit2 can be used in humans.
His team is also investigating the role of FKBP51 in cancer after tests have revealed that certain tumors of glioblastoma overexpress the protein.
They hope that FKBP51 inhibitors can be used when a patient's tumor has undergone a mutation beyond what can be treated with existing cancer drugs.
"We may be able to resensitize them to different types of chemotherapy using these specific inhibitors," Hausch said.
WHAT IS OBESITY? WHAT ARE THE RISKS OF HEALTH?
Obesity is defined as an adult with a BMI of 30 or greater.
A healthy person's BMI – calculated by dividing weight in kg by height in meters, and the response by height again – is between 18.5 and 24.9.
Among children, obesity is defined as being in the 95th percentile.
The percentiles compare young people to others of the same age.
For example, if a three-month-old child is in the 40th percentile of weight, this means that 40% of three-month-olds weigh the same or less than the baby.
About 58 percent of women and 68 percent of men in the UK are overweight or obese.
The condition costs the NHS about £ 6.1 billion out of a budget of £ 124.7 billion each year.
This is due to obesity increasing a person's risk of a number of life-threatening conditions.
Such conditions include type 2 diabetes, which can cause kidney disease, blindness, and even limb amputations.
Research suggests that at least one in six UK hospital beds is taken care of by a patient with diabetes.
Obesity also increases the risk of heart disease, which kills 315,000 people every year in the UK – making it the number one cause of death.
Carrying dangerous amounts of weight was also associated with 12 different types of cancer.
This includes the breast, which affects one in eight women at some point in their lives.
Among children, research suggests that 70 percent of obese young people have high blood pressure or high cholesterol, which puts them at risk for heart disease.
Obese children are also significantly more likely to become obese adults.
And if children are overweight, obesity in adulthood is usually more severe.
About one in five children start studying in the UK with overweight or obesity, which increases to one in three by the time they turn 10.