SciBx talked to Drs. Ray Stevens and Michael Hanson about the GPCR Consortium’s plans to unlock GPCR structure information for drug discovery. The goal is to elucidate the 3D structures of a large number of GPCRs and generate high-resolution pictures that can be used to explore how the receptors work and aid the design of new compounds.
Amgen (United States), Sanofi (Europe) and ONO (Japan) were the first to join the GPCR Consortium, which officially launched in October 2014. The research is currently planned to be conducted, but not limited to three leading academic sites: iHuman Institute at ShanghaiTech University, Shanghai Institute of Materia Medica, a member of the Chinese Academy of Sciences, and the University of Southern California in Los Angeles.
The GPCR Consortium hopes to attract up to five additional industry members to achieve the initiative’s goal of determining structures of 200 of the 826 known human GPCRs, prioritized in disease areas that initially include diabetes, cancer, and mental disorders.
Dr. Hanson, president of the GPCR Consortium, noted that GPCRs constitute the largest family of proteins in the human body and represent therapeutic targets for about 40% of marketed drugs. “What is surprising is that these developed drugs really only target a handful of the known family of GPCRs. So there is a vast untapped potential out there,” he said. But “at the moment, we only have structures for 26 of the 826 known human GPCRs. There is a lot that we do not know about this family.”
“There are a lot of GPCR data being generated, including but not limited to structural data, novel signaling pathways, allosteric modulation and polypharmacology,” said Dr. Stevens. “We are developing solutions to integrate access and ultimately utilize all of this data to accelerate the process of drug discovery.”