Solid Phase Synthesis and Opioid Receptor Binding Properties of Presumable Dermorphin Precursor Derivatives

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概要

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• Presumable dermorphin precursor peptide derivatives comprized of 35 amino acids and their fragments, which are based on the amino acid sequence determined by recombinant deoxyribonucleic acid (DNA) techniques, were synthesized by the solid phase method. A 35-residue peptide amide containing L-Ala^2-dermorphin sequence at the N-terminus (1) as well as its D-Ala^2 isomer (2) and the C-terminal 20-residue peptide amide were found to be unexpectedly stable against aminopeptidase M digestion and in rat brain membrane fractions mixture, suggesting that the C-terminal Glu-rich moiety of 1 and 2 serves to protect from enzymatic breakdown. In the opioid receptor binding assay, 2 showed 40 and 25-fold higher affinities than 1 for μ and δ-receptors, respectively. The N-terminal 15-residue peptide fragment of 2 showed greatly increased affinities for both receptors, being one half of those of dermorphin, whereas that of 1 showed low affinities. Opioid receptor binding properties of these synthetic peptides may be useful in investigation of the processing to dermorphin.

• 社団法人日本薬学会の論文
• 1991-05-25

著者

• 鈴木 謙次

  東北薬科大学

• 安保 明博

  Tohoku College of Pharmacy

• 佐々木 有亮

  Tohoku College of Pharmacy

• 鈴木 謙次

  Tohoku College of Pharmacy

関連論文

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