Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors

Bhaswati Sinha, Zhengyu Cao, Thomas F. Murray, Jane V. Aldrich

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

A series of potent electrophilic affinity labels (IC50= 0.1-5 nM) containing either a bromoacetamide or isothiocyanate based on the μ opioid receptor (MOR) selective peptide dermorphin were prepared. All four analogues exhibited wash resistant inhibition of [3H]DAMGO binding at subnanomolar to nanomolar concentrations, suggesting that these analogues bind covalently to MOR. To our knowledge, these peptides are the highest affinity peptide-based affinity labels for MOR reported to date.

Original languageEnglish
Pages (from-to)7372-7375
Number of pages4
JournalJournal of Medicinal Chemistry
Volume52
Issue number23
DOIs
StatePublished - Dec 10 2009

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Affinity Labels
mu Opioid Receptor
Peptides
Ala(2)-MePhe(4)-Gly(5)-enkephalin
Opioid Receptors
Inhibitory Concentration 50
dermorphin

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Cite this

Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. / Sinha, Bhaswati; Cao, Zhengyu; Murray, Thomas F.; Aldrich, Jane V.

In: Journal of Medicinal Chemistry, Vol. 52, No. 23, 10.12.2009, p. 7372-7375.

Research output: Contribution to journalArticle

Sinha, Bhaswati ; Cao, Zhengyu ; Murray, Thomas F. ; Aldrich, Jane V. / Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. In: Journal of Medicinal Chemistry. 2009 ; Vol. 52, No. 23. pp. 7372-7375.
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