Modification of Peptides to Limit Metabolism

Isuru R. Kumarasinghe, Victor J Hruby

Research output: Chapter in Book/Report/Conference proceedingChapter

4 Scopus citations

Abstract

Naturally occurring endogenous peptide neurotransmitters and other peptides have had limited usage as drugs due to the rapid proteolysis in vivo. Rapid proteolysis of peptides by proteolytic enzymes can occur for many reasons and can be beneficial or non-beneficial depending upon the biological circumstances. If the metabolic stability of the peptides is a desired property, however, the pharmacophore residues of the endogenous hormone and neurotransmitter peptides which are essential for the biological activities need to be identified, and then protected from rapid proteolysis. In addition, proteolytic action and its specificity on metabolically unstable desired peptides needs to be further established in order to provide a better framework for designing metabolically stabilized peptides. We have systematically described some approaches which have been taken to stabilize peptides from proteolytic action.

Original languageEnglish (US)
Title of host publicationPeptide Chemistry and Drug Design
Publisherwiley
Pages247-270
Number of pages24
ISBN (Electronic)9781118995303
ISBN (Print)9780470317617
DOIs
StatePublished - Feb 13 2015

Keywords

  • Linear peptide versus cyclic peptide
  • Peptides to limit metabolism
  • Peptides with plasma stability
  • Peptidomimetics
  • Proteolytic degradation resistant peptides

ASJC Scopus subject areas

  • Medicine(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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  • Cite this

    Kumarasinghe, I. R., & Hruby, V. J. (2015). Modification of Peptides to Limit Metabolism. In Peptide Chemistry and Drug Design (pp. 247-270). wiley. https://doi.org/10.1002/9781118995303.ch7