2. Academic Validation
  3. Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors

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

  • J Med Chem. 2009 Dec 10;52(23):7372-5. doi: 10.1021/jm9007592.
Bhaswati Sinha 1,  Zhengyu Cao,  Thomas F Murray,  Jane V Aldrich
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Lawrence, Kansas 66045, USA.
PMID: 19621878 DOI: 10.1021/jm9007592
Abstract

A series of potent electrophilic affinity labels (IC(50) = 0.1-5 nM) containing either a bromoacetamide or isothiocyanate based on the mu Opioid Receptor (MOR) selective peptide dermorphin were prepared. All four analogues exhibited wash resistant inhibition of [(3)H]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.

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