Overview
G protein-coupled receptors (GPCRs) represent the predominant receptor class in the human body and have been implicated in a broad range of
ailments, including allergies, cardiovascular dysfunction, depression, obesity, cancer, pain, diabetes, and a variety of central nervous system
disorders. Not surprisingly, GPCRs are also the largest group of cellular targets for conventional therapeutics. Estimates suggest that some 80
currently-marketed drugs that target GPCRs account for as much as $30 to $60 billion in annual sales.
With as many as 1000 unique GPCR genes in the human genome, it is clear that these receptors remain woefully under-exploited as therapeutic
targets. Consequently, a growing number of academic and commercial laboratories have developed myriad screening methods to identify novel GPCRs and
their ligands. These approaches run the gamut from simple affinity assays to sophisticated fluorescence-based methods, constitutive activation of
GPCRs to simulate ligand binding, and screening via libraries and/or GPCR-laden microarrays. In vivo targeting designed to activate or inactivate GPCR
genes in mice has begun to yield critical insights into receptor function in mammals.
A significant number of challenges have yet to be overcome before the full potential of GPCRs can be realized, including the fact that most GPCRs
lack identified ligands, relatively little structural information exists, and the recent recognition that virtually all GPCRs form oligomeric
complexes
in vivo. Despite these and other hurdles, the therapeutic potential of GPCR-targeted drugs remains enormous. Given the pharmaceutical
industry' s prior GPCR successes, investigators, armed with a bounty of genomic and proteomic information, are expected to rapidly accelerate the
process of identifying GPCRs and expedite the movement of drugs that target them through clinical trials and into the marketplace.
This report describes the current state-of-the-art in both GPCR screening and downstream technology, as well as the various strategies being
employed by firms in the field to advance their technologies and products. Also included are capsules of key competitors and expert commentaries.
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