From biased signalling to polypharmacology: unlocking unique intracellular signalling using pepducins

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From biased signalling to polypharmacology: unlocking unique intracellular signalling using pepducins

Carr, 3rd, Richard; Benovic, Jeffrey L

Biochemical Society transactions, 2016-Apr-15, Volume: 44, Issue: 2

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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.

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