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Researchers Develop GPCR ‘Fingerprints’ for Major Drug Development Targets

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Published on : Dec 23, 2015

The growing prevalence of respiratory, cardiovascular, and reproductive conditions along with increase in nervous system disorders and various cancers worldwide has boosted the global G-protein coupled receptors (GPCRs) market. While the market has witnessed rising demand for improved GPCR assays, assay systems, and platforms for ADME toxicity studies and drug discovery, government efforts and partnerships among the key players have further propelled the market growth. Though the high cost associated with the maintenance of cell lines and costly equipment have restrained the overall market, development of technologically advanced GPCR assays will open new avenues for the market. One such recent development has been the creation of ‘fingerprints’ for major drug development targets.

Researchers at the Florida campus of Scripps Research Institute have developed detailed ‘fingerprints’ of a class of surface receptors that would be highly beneficial for drug development. The study focuses on the interactions of GPCRs with their signalling mediators- the G proteins. Presently, GPCRs account for around 40% of all prescription pharmaceuticals available in the market. They play a pivotal role across many physiological functions as they transmit signals from outside the cell to its interior. As an outside substance binds to a GPCR, G protein is activated inside the cell to exhibit a certain cellular response. 

The study has revealed that individual GPCRs engage with multiple G proteins with varying degrees. The study is aimed at 14 different types of G proteins at once. The human body has 16 different types of G proteins. According to Alan Smrcka, a prominent GPCR researcher, the findings suggest that GPCR fingerprinting approach can be implemented to predict the G protein coupling specificity of a GPCR in a native system.