Researchers from Heptares Therapeutics, a drug company, have discovered the 3-D structure of a protein receptor that mediates our response to stress, according to a new study in Nature. Using a powerful X-ray machine at Diamond Light Source, the UK's national particle accelerator, they were able to detail the structure of CRF1, a find that they say opens up the possibility of creating specially tailored drugs to treat depression and anxiety.
CRF1, a molecule on the outside of cells on the pituitary gland, releases CRF, hormones involved in regulating our stress response that over time contribute to anxiety and depression.
A vital aspect of the discovery is that the receptor has a small binding pocket located in a much different position than other G-protein-coupled receptors, (GPCRs). Knowing the structure of Class B GPCRs like CRF1 could potentially help researchers develop drugs that better target receptors within the same family, Heptares claims. Scientists could just design a drug that pops right into that pocket.
“The finding that the structure of CRF1, a Class B GPCR, is completely different to previously solved Class A receptors confirms why Class B receptors could not previously be modeled for the purpose of rational drug design," said Fiona Marshall, Chief Scientific Officer for Heptares, in a press statement. "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," she later told the Sunday Times. The company says it could possibly also lead to targeted drugs for Type 2 diabetes and osteoporosis, since those diseases deal with receptors of the same class and structure. /Popsci.Com/