UMIP-451 and -498 – Multiplexed Ultra-High Throughput GPCR Drug Discovery and Repurposing Using the DCyFIR Profiling Platform

Problem: G protein-coupled receptors(GPCRs) are the largest and most therapeutically targeted class oftransmembrane receptors in clinical medicine. More than 800 GPCRs detectdiverse physical and chemical signals (e.g., light, neurotransmitters,hormones) to regulate physiological function. Furthermore, more than one-thirdof FDA-approved drugs target more than 130 GPCRs. Despite their usefulness andsuccess as therapeutic targets, there remains an enormity of untapped potentialfor GPCR drug discovery, both in terms of small molecule regulators andengineered protein-based biologics such as nanobodies. Realizing this potentialrequires robust, low-cost, and scalable GPCR profiling technologies. Technology: Researchers at the University of Miami have developed a novel GPCR profiling platform calledDynamic Cyan Induction by Functional Integrated Receptors (DCyFIR). Thistechnology enables the cost-effective profiling of individual compounds andchemical libraries against pooled mixtures of several hundred GPCR barcodedcell strains (GPCR multiplexes) in a single experiment. Compared to lowerthroughput GPCR screening approaches, DCyFIR profiling enables the physicalscreening of huge numbers of compounds, and brings wet-laboratory throughput astep closer to what is done in silico. Additionally, because potential drugs aretested against large numbers of receptors simultaneously, DCyFIR profiling alsoprovides unique and valuable information about on- and off-target druginteractions and drug polypharmacology. As such, DCyFIR facilitates thediscovery of new GPCR lead compounds and the repurposing of approved drugs.Several high-impact papers (top 1-5% of all research outputs ever tracked by Altmetric)in PNAS, JBC, and Nature Reviews DrugDiscovery describe the details, applications, and discoveries of the DCyFIRprofiling platform. Peter Gutenberg pxg372@miami.edu 305-243-4604

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