“Dipeptoids”: From the Chemical Structure of the Endogenous Peptide to the Design of Peptidomimetics

The present review details the rational multi-step process followed for the discovery of a family of non-peptide CCK receptor ligands (“dipeptoids”), starting from the structure of the endogenous peptide, CCK8. Emphasis will be made on the N- and C-terminal modifications, on the singular effects of the stereochemical changes and the incorporation of conformational constraints into the structure of “dipeptoids”, and on the modifications directed to improve the pharmacological profile of these compounds to afford valuable clinical candidates.