CHAPTER 13: Peptide Therapeutics: Neuropeptides

The development of neuropeptide therapeutics poses several difficulties, including stability, bioavailability, receptor selectivity, and the ability (or not) to cross membrane barriers. In this chapter we discuss briefly the efforts that are being made to address these problems using selective examples for the melanocortin, bradykinin and opioid systems. The use of conformational constraint, topographical constraint, and computational approaches to ligand design, including ligand–receptor homology modeling are discussed as an approach to enhance the properties of peptides for the development of peptide therapeutics.