ホルモンデリバリー : オピオイドペプチドの脂質膜への分配と配向に基づくレセプター選択性の制御

概要

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Peptide hormones elicit the effect by binding to the specific receptor in cell membrane. On the other hand, several peptide hormones have been shown to be distributed to the lipid membrane with taking a defined conformation. The peptides are incorporated into the lipid membrane through the hydrophobic interaction, electrostatic interaction, and dipole interaction, etc. Due to these factors, the enkephalin derivative was also shown to interact with the lipid membrane stereoselectively. These findings support the membrane compartment concept, which predicts that the peptide is incorporated into a certain region of the membrane (compartment) where the binding site of the receptor locates, resulted in the enhancement of their association. Opioid receptors exist in three different types, δ, μ, and κ, and the binding sites supposedly locate over, on, and inside membrane, respectively. Several enkephalin derivatives were synthesized and discussed on the relation of the receptor affinity and selectivity with the membrane affinity.
日本膜学会の論文