title: From biased signalling to polypharmacology: unlocking unique intracellular signalling using pepducins.
abstract: For over a decade, pepducins have been utilized to develop unique pharmacological profiles that have been particularly challenging for traditional drug discovery methods. It is becoming increasingly clear that these cell-penetrating lipopeptides can access receptor conformations that are currently not accessible through orthosteric targeting. This review addresses the emerging concepts in the development of pepducins including the elicitation of biased signalling, pepducin polypharmacology and recent insight into their mechanism of action.
authors.affiliation: Department of Biochemistry and Molecular Biology, Thomas Jefferson University, Philadelphia, PA 19107, U.S.A. richard.carr.3rd@gmail.com.
authors.forename: Richard
authors.initials: R
authors.lastname: Carr
authors.affiliation: Department of Biochemistry and Molecular Biology, Thomas Jefferson University, Philadelphia, PA 19107, U.S.A.
authors.forename: Jeffrey L
authors.initials: JL
authors.lastname: Benovic
mesh_terms: D006801:Humans; D010455:Peptides / Q000494:pharmacology*; D064798:Polypharmacology; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry*; D015398:Signal Transduction
chemical_list: D010455:Peptides; D043562:Receptors, G-Protein-Coupled
keywords: G protein-coupled receptors; biased signalling; drug discovery; pepducins; polypharmacology