Breakthrough in GPCR Understanding
News Aug 26, 2016
Integral Molecular has announced a major advancement in understanding the functionality of G protein-coupled receptors (GPCRs), the largest protein superfamily in the human genome, providing unprecedented insight for human disease therapeutics.
The work answers the fundamental question of how GPCRs, a complex class of membrane protein on the cell surface, transmit signals across the outer membrane to orchestrate internal signaling events implicated in diseases including HIV, heart disease, and cancer. This work published by Wescott et al., appears in the current issue of Proceedings of the National Academy of Sciences. The study employed Integral Molecular’s Shotgun Mutagenesis platform for the most detailed and comprehensive study of the GPCR CXCR4 completed to date.
“Integral Molecular’s ability to exhaustively study complex proteins through mutagenesis, coupled with our structural insights, has propelled our understanding of CXCR4 and other GPCRs,” said Dr. Tracy Handel, collaborator and co-author from the University of California in San Diego and a leading expert in chemokine receptor structural biology. “CXCR4 has been studied for over two decades, but the detailed mechanism for how it and other GPCRs receive and transmit information to trigger cellular responses had yet to be fully described.”
“Using our Shotgun Mutagenesis platform, we’ve successfully mapped key molecular interactions within CXCR4 that can be manipulated to manage diseases such as cancer and HIV,” said Dr. Benjamin Doranz, President and Chief Scientific Officer at Integral Molecular. “GPCRs comprise about a third of existing drug targets, so our results have significant implications for the discovery of new, as well as improved, therapeutics”
About 422 million people around the world, including more than 30 million Americans, have diabetes. Obesity is the most significant risk factor for type 2 diabetes. yet about 30 percent of obese people do not develop type 2 diabetes or other metabolic conditions. New research aims to understand on a cellular level, how this separation occurs.READ MORE
Measuring hand grip can help identify youths who could benefit from lifestyle changes, says new research. While other studies have shown that muscle weakness as measured by grip strength is a predictor of unhealthy outcomes - including cardiovascular and metabolic diseases - this is the first to do so for adolescent health over time.READ MORE