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article imageStudy unlocks structure of protein causing depression and anxiety

By JohnThomas Didymus     Jul 22, 2013 in Science
Scientists at Heptares Therapeutics, a company based in the UK, have determined the structure of a protein molecule produced by the pituitary gland responsible for feelings of stress, anxiety and depression in humans.
Scientists have long known that the pituitary gland plays an important role in stress, depression and anxiety responses by releasing stress chemicals into the blood.
However, this is the first time that scientists have been able to describe the molecular structure of the protein receptor CRF1 and confirm its role as the chemical responsible for triggering the stress response.
According to the researchers at Heptares Therapeutics, in a paper published on July 17, in the journal Nature, titled: "Structure of class B GPCR corticotropin-releasing factor receptor 1," corticotropin-releasing factor receptor 1 (CRF1) is the receptor for the stress hormone corticotropin-releasing factor (CRF) produced in the hypothalamus which stimulates production of adrenocorticotropic hormone (ACTH) and other stress hormones in the anterior lobe of the pituitary gland.
The hypothalamus is the part of the brain that produces hormones which control basic physiologic functions such as temperature control, mood and hunger.
The researchers used a particle accelerator called the Diamond Light Source located in Harwell, Oxfordshire, to study the detailed structure of CRF1. Elucidating the structure of the protein will help pharmacologists to develop drugs that can be used to target special sites on its molecule as a way of blocking it and preventing it from triggering the cascade of biochemical activities that precede stress response.
Dr. Fiona Marshall, Chief Scientific Officer at Heptares, and lead author in the study, said: "Stress related diseases such as depression and anxiety affect a quarter of adults each year, but what many people don't realise is that these conditions are controlled by proteins in the brain, one of which is CRF1."
Marshall added: “Now we know its shape, we can design a molecule that will lock into this crevice and block it so that CRF1 becomes inactive — ending the biochemical cascade that ends in stress.”
Dr. Andre Dore, a senior scientist with Heptares, said that knowledge of the structure of CRF1 can help to "solve closely related receptors that open up the potential for new drugs to treat a number of major diseases including Type 2 diabetes and osteoporosis."
More about CRF1, protein receptor, Heptares Therapeutics
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