Peptidomimetics and Their Applications for Opioid Peptide Drug Discovery

Research output: Contribution to journalReview articlepeer-review

3 Scopus citations


Despite various advantages, opioid peptides have been limited in their therapeutic uses due to the main drawbacks in metabolic stability, blood-brain barrier permeability, and bioavailability. Therefore, extensive studies have focused on overcoming the problems and optimizing the therapeutic potential. Currently, numerous peptide-based drugs are being marketed thanks to new synthetic strategies for optimizing metabolism and alternative routes of administration. This tutorial review briefly introduces the history and role of natural opioid peptides and highlights the key findings on their structure-activity relationships for the opioid receptors. It discusses details on opioid peptidomimetics applied to develop therapeutic candidates for the treatment of pain from the pharmacological and structural points of view. The main focus is the current status of various mimetic tools and the successful applications summarized in tables and figures.

Original languageEnglish (US)
Article number1241
Issue number9
StatePublished - Sep 2022
Externally publishedYes


  • analgesic drugs
  • bioavailability
  • locally constrained peptides
  • opioid receptors
  • peptide backbone modifications
  • peptidomimetic

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology


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