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Lipopeptides based on the intracellular loops of cell-surface receptors, known as "Pepducins," represent a promising new class of compounds used for the study of membrane proteins and as potential therapeutics in a variety of diseases. Detailed knowledge of the three-dimensional structure of G-protein-coupled receptors (GPCRs) and delineation of the mechanisms of pepducin activation and biased G-protein signaling has facilitated the development of even more potent pepducin allosteric modulators.

Pepducins and Other Lipidated Peptides as Mechanistic Probes and Therapeutics