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Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs.

ABSTRACT: Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest to treat pain. Pain may associate with inflamed tissue characterized by acidic pH. The potentially low pH at tissue targeted by opioid drugs in pain management could impact drug binding to the opioid receptor, because opioid drugs typically have a protonated amino group that contributes to receptor binding, and the functioning of GPCRs may involve protonation change. In this review, we discuss the relationship between structure, function, and dynamics of opioid receptors from the perspective of the usefulness of computational studies to evaluate protonation-coupled opioid-receptor interactions.

SUBMITTER: Lesnik S

PROVIDER: S-EPMC8707250 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature

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Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs.

Lešnik Samo S Bertalan Éva É Bren Urban U Bondar Ana-Nicoleta AN

International journal of molecular sciences 20211212 24

Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest to treat pain. Pain may associate with inflamed tissue characterized by acidic pH. The potentially low pH at tissue targeted by opioid drugs in pain management could impact drug binding to the opioid receptor, because opioid drugs typically have a protonated amino group that contributes to receptor binding, and the functioning of GPCRs may involve protonation change. In this review, we discus ...[more]

PMID: 34948150

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