[Structure of mu and delta opioid receptors].
Copyright policy )[Structure of mu and delta opioid receptors].
The opioid receptor family is composed of three members, the µ, δ and κ opioid receptors, that respond to classical opioid alkaloids such as morphine and heroin as well as endogenous peptide ligands like endorphins. They belong to the G-protein-coupled receptor (GPCR) superfamily, and are excellent therapeutic targets for pain control. I will discuss new insights into conserved elements of opioid ligand recognition and structural features associated with ligand subtype selectivity based on the crystal structures we obtained for µ-OR and δ-OR. These data also provide a structural explanation and validation for the "message-address" model of opioid receptor pharmacology in which distinct "message" (efficacy) and "address" (selectivity) determinants are contained within a single ligand. Comparison of the "address" region of the OR with other GPCRs reveals this structural organization may be a more general phenomenon, extending to other GPCR families as well. Finally, I will discuss the µ-OR oligomeric arrangement in the crystal structure and its potential implication in opioid receptor function.
Models, Molecular, Receptors, Opioid, mu, Substrate Specificity, Receptors, Opioid, delta, Animals, Humans, Protein Interaction Domains and Motifs, Protein Multimerization, Protein Structure, Quaternary, Conserved Sequence, Protein Binding
Models, Molecular, Receptors, Opioid, mu, Substrate Specificity, Receptors, Opioid, delta, Animals, Humans, Protein Interaction Domains and Motifs, Protein Multimerization, Protein Structure, Quaternary, Conserved Sequence, Protein Binding
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