Opioid glycopeptide analgesics derived from endogenous enkephalins and endorphins

Yingxue Li, Mark R. Lefever, Dhanasekaran Muthu, Jean M. Bidlack, Edward J. Bilsky, Robin L Polt

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Over the past two decades, potent and selective analgesics have been developed from endogenous opioid peptides. Glycosylation provides an important means of modulating interaction with biological membranes, which greatly affects the pharmacodynamics and pharmacokinetics of the resulting glycopeptide analogues. Furthermore, manipulation of the membrane affinity allows penetration of cellular barriers that block efficient drug distribution, including the blood-brain barrier. Extremely potent and selective opiate agonists have been developed from endogenous peptides, some of which show great promise as drug candidates.

Original languageEnglish (US)
Pages (from-to)205-226
Number of pages22
JournalFuture Medicinal Chemistry
Volume4
Issue number2
DOIs
StatePublished - Feb 2012

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Endorphins
Glycopeptides
Enkephalins
Opioid Analgesics
Opiate Alkaloids
Membranes
Opioid Peptides
Blood-Brain Barrier
Glycosylation
Pharmaceutical Preparations
Analgesics
Pharmacokinetics
Peptides

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Molecular Medicine

Cite this

Opioid glycopeptide analgesics derived from endogenous enkephalins and endorphins. / Li, Yingxue; Lefever, Mark R.; Muthu, Dhanasekaran; Bidlack, Jean M.; Bilsky, Edward J.; Polt, Robin L.

In: Future Medicinal Chemistry, Vol. 4, No. 2, 02.2012, p. 205-226.

Research output: Contribution to journalArticle

Li, Yingxue ; Lefever, Mark R. ; Muthu, Dhanasekaran ; Bidlack, Jean M. ; Bilsky, Edward J. ; Polt, Robin L. / Opioid glycopeptide analgesics derived from endogenous enkephalins and endorphins. In: Future Medicinal Chemistry. 2012 ; Vol. 4, No. 2. pp. 205-226.
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