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

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

doi:10.1021/jm9007592

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

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

Department of Pharmacology and Neuroscience

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

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	https://doi.org/10.1021/jm9007592
State	Published - Dec 10 2009

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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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.",

author = "Bhaswati Sinha and Zhengyu Cao and Murray, {Thomas F.} and Aldrich, {Jane V.}",

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AU - Sinha, Bhaswati

AU - Cao, Zhengyu

AU - Murray, Thomas F.

AU - Aldrich, Jane V.

PY - 2009/12/10

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AB - 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.

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