Peptide receptors belong to the B class of G-protein-coupled receptors (GPCRs). This is a large group of several hundred GPCRs that are activated by extracellular protein or peptide ligands. Endogenous peptide receptor ligands bind to the N' terminus and/or the 3 extracellular loops of the receptor. The peptide-receptor binding domains are large, conferring high ligand affinity and specificity. Small molecule drugs however only bind to small 'hot spots' that are essential for GPCR activation.
Peptide receptors represent a large, promising group of pharmacological targets for treating human disease. Consistent with the array of physiological roles of peptide receptors, the range of conditions in which they are dysregulated is vast and includes cardiovascular, endocrine and metabolic disorders.
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