Medicine and Health

Three-Dimensional Structural Insights Have Revealed the Distinct Binding Interactions of Agonists, Partial Agonists, and Antagonists with the µ Opioid Receptor

Z. Li, J. Liu, et al.

Explore the structural intricacies of the µ opioid receptor through this comprehensive review by Zoe Li, Jie Liu, Fan Dong, Nancy Chang, Ruili Huang, Menghang Xia, Tucker A Patterson, and Huixiao Hong. Delve into the distinctive binding interactions of agonists, partial agonists, and antagonists, paving the way for the next generation of safer opioid analgesics.

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Abstract

This review describes available 3D structures of the µ opioid receptor in the protein data bank and provides structural insights for the binding of agonists and antagonists to the receptor. Comparative analysis on the atomic details of the binding site in these structures was conducted and distinct binding interactions for agonists, partial agonists, and antagonists were observed. The findings in this article deepen our understanding of the ligand binding activity and shed some light on the development of novel opioid analgesics which may improve the risk benefit balance of existing opioids.

Publisher

International Journal of Molecular Sciences

Published On

Apr 11, 2023

Authors

Zoe Li, Jie Liu, Fan Dong, Nancy Chang, Ruili Huang, Menghang Xia, Tucker A Patterson, Huixiao Hong

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