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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.


Bhaswati Sinha, Zhengyu Cao, Thomas F Murray, Jane V Aldrich. Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. Journal of medicinal chemistry. 2009 Dec 10;52(23):7372-5

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PMID: 19621878

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