Scientists Create Detailed Picture of Membrane Protein

Researchers at The Scripps Research Institute have created the most detailed 3D picture yet of a membrane protein linked to learning, memory, anxiety, pain and brain disorders such as schizophrenia, Parkinson’s disease, Alzheimer’s disease and autism. The research — which focuses on the mGlu1 receptor — promises to have a major impact on new drug discovery efforts.  The mGlu1 receptor, which helps regulate the neurotransmitter glutamate, belongs to a category of molecules known as G protein-coupled receptors (GPCRs). GPCRs reside in the cell membranes and sense various molecules outside the cell, including odors, hormones, neurotransmitters and light. After binding these molecules, GPCRs trigger a specific response inside the cell. More than one-third of therapeutic drugs target GPCRs — including allergy and heart medications, drugs that target the central nervous system, and anti-depressants. Using a combination of techniques, including X-ray crystallography, structure-activity relationships, mutagenesis, and full-length dimer modeling, the research team achieved a high-resolution image of mGlu1 as well as a deeper understanding of the receptor’s function and pharmacology. The findings now provide a solid platform for much more reliable modeling of closely related receptors, which are equally important in drug discovery. To read more about this study, click here.