Abstract 1385 Identifying δ- and κ-opioid protomer selective compounds utilizing robust computational workflows for future δ-κ-opioid heteromer receptor targeting

While μ-opioid agonists remain the therapeutic gold standard for pain management, abuse liability, tolerance, and the risk of life-threatening side effects like respiratory depression severely limit their clinical utility. Amongst the search for viable alternatives are novel agonists targeting the δ- or κ-opioid receptors (DOR and KOR, respectively). Unfortunately, the current landscape of drugs that singly target DOR or KOR protomers has shown limited efficacy and undesirable side effects (e.g., dysphoria).

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Publication Details

Journal
Journal of Biological Chemistry
Published
2025-05-01
DOI
https://doi.org/10.1016/j.jbc.2025.109028
Primary Topic
Neuropeptides and Animal Physiology
Type
article
Field-Weighted Citation Impact
0.00

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Abstract 1385 Identifying δ- and κ-opioid protomer selective compounds utilizing robust computational workflows for future δ-κ-opioid heteromer receptor targeting

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Abstract 1385 Identifying δ- and κ-opioid protomer selective compounds utilizing robust computational workflows for future δ-κ-opioid heteromer receptor targeting

Stanton F. McHardy, Donald E. Rounds, Kelly A. Berg, Michael J. Wedemeyer, Nicholas A. Clanton, Krystalle Diaz
article en

Abstract

While μ-opioid agonists remain the therapeutic gold standard for pain management, abuse liability, tolerance, and the risk of life-threatening side effects like respiratory depression severely limit their clinical utility. Amongst the search for viable alternatives are novel agonists targeting the δ- or κ-opioid receptors (DOR and KOR, respectively). Unfortunately, the current landscape of drugs that singly target DOR or KOR protomers has shown limited efficacy and undesirable side effects (e.g., dysphoria).

Journal of Biological ChemistryVol. 301(5)
The University of Texas at San Antonio (US)
City University of New York, National Institutes of Health
Openalex Percentile: Top 85%
Neuropeptides and Animal Physiology
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