GPCRs are the most studied drug target class and have a proven record as valuable drug targets, with 40-50% of marketed drugs being modulators of GPCR function. Despite the intense effort focused on these targets by the pharmaceutical industry over many years, numerous challenges remain.
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The question of choosing which methods to use for analyte quantification (signal vs concentration determination, parameters, and format) continues to generate heated debates and divergent understanding.
G protein-coupled cell surface receptors (GPCRs) have served a fundamental role in modern pharmacology, due to their central importance in cell communication, and have been the target for the discovery of a large number of drugs. By one estimate, more than 40% of marketed drugs target GPCRs.