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

Research output: Contribution to journal › Article

9 Citations (Scopus)

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
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

Fingerprint

Affinity Labels

mu Opioid Receptor

Peptides

Ala(2)-MePhe(4)-Gly(5)-enkephalin

Opioid Receptors

Inhibitory Concentration 50

dermorphin

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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

Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. / Sinha, Bhaswati; Cao, Zhengyu; Murray, Thomas F.; Aldrich, Jane V.

In: Journal of Medicinal Chemistry, Vol. 52, No. 23, 10.12.2009, p. 7372-7375.

Research output: Contribution to journal › Article

Sinha, B, Cao, Z, Murray, TF & Aldrich, JV 2009, 'Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors', Journal of Medicinal Chemistry, vol. 52, no. 23, pp. 7372-7375. https://doi.org/10.1021/jm9007592

Sinha B, Cao Z, Murray TF, Aldrich JV. Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. Journal of Medicinal Chemistry. 2009 Dec 10;52(23):7372-7375. https://doi.org/10.1021/jm9007592

Sinha, Bhaswati ; Cao, Zhengyu ; Murray, Thomas F. ; Aldrich, Jane V. / Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. In: Journal of Medicinal Chemistry. 2009 ; Vol. 52, No. 23. pp. 7372-7375.

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10.1021/jm9007592