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Press Release

Integral Molecular announces breakthrough in understanding the functionality of GPCRs, the largest class of drug targets in human disease

Integral Molecular,Inc.
Posted on: 25 Aug 16

Integral Molecular, an industry leader in membrane protein antibody discovery, 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 Integral Molecular

Integral Molecular is a research-driven biotechnology company creating a pipeline of therapeutic antibodies against under-exploited membrane protein targets, including GPCRs, ion channels, transporters, and viral envelope proteins, using its proprietary MPS Discovery Engine®. This platform is built on the company’s Lipoparticle and Shotgun Mutagenesis technologies and over 15 years of experience optimizing membrane proteins, enabling the isolation, characterization, and engineering of monoclonal antibodies against otherwise intractable membrane protein targets. Integral Molecular discovers antibodies for partners in parallel with its own independent work developing antibodies for licensing. The company currently has therapeutic programs focused on pain, autoimmunity, and infectious diseases.

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Last updated on: 25/08/2016

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