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 language | English (US) |
|---|---|
| Pages (from-to) | 7372-7375 |
| Number of pages | 4 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 52 |
| Issue number | 23 |
| DOIs | |
| State | Published - Dec 10 2009 |
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery
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Cite this
Sinha, B., Cao, Z., Murray, T. F., & Aldrich, J. V. (2009). Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. Journal of Medicinal Chemistry, 52(23), 7372-7375. https://doi.org/10.1021/jm9007592