Abstract
Historically, seven transmembrane receptors (7TMs) [also referred to as G-protein-coupled receptors (GPCRs)] have been the mainstay biological target for pharmacological therapy. This is because they are conveniently located on the cell surface, and thus are the main points of transfer of chemical information from the extracellular space to the cytosol, and they control a myriad of cellular processes. This latter point becomes a two-edged sword in the utilization of 7TMRs as drug targets since it then requires some form of limitation of receptor signaling to achieve therapeutic drug selectivity.
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