Bhaswati Sinha, Zhengyu Cao, Thomas F Murray, Jane V Aldrich
Department of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Lawrence, Kansas 66045, USA.
Journal of medicinal chemistry 2009 Dec 10A 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
PMID: 19621878
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