Pepducins are cell-penetrating peptides that act as intracellular modulators of signal transference from receptors to G proteins.
Pepducins were first developed at the Tufts Medical Center laboratories of Dr. Athan Kuliopulos and Dr. Lidija Covic.
[1] Pepducins employ lipidated fragments of intracellular G protein-coupled receptor loops to modulate GPCR action in targeted cell-signaling pathways.
[2] A pepducin molecule consists of a short peptide derived from a GPCR intracellular loop tethered to a hydrophobic moiety.
This structure allows pepducin lipopeptides to anchor in the cell membrane lipid bilayer and target the GPCR/G protein interface via a unique intracellular allosteric mechanism.