Binding of β-endorphin and its fragments to the nonopiod receptor of murine peritoneal macrophages |
| |
Authors: | Yu A Kovalitskaya V B Sadovnikov A A Kolobov Yu A Zolotarev V V Yurovsky V M Lipkin E V Navolotskaya |
| |
Institution: | (1) Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Pushchino Branch, Russian Academy of Sciences, pr. Nauki 6, Pushchino, Moscow oblast, 142290, Russia;(2) State Research Center, Institute of Extrapure Biopreparations, FMBA of the Russian Federation, St. Petersburg, 197110, Russia;(3) Institute of Molecular Genetics, Russian Academy of Sciences, pl. Kurchatova 2, Moscow, 123182, Russia;(4) Department of Neurosurgery, University of Maryland, Baltimore, USA |
| |
Abstract: | The tritium-labeled selective agonist of the nonopioid β-endorphin receptor the decapeptide immunorphin (3H]SLTCLVKGFY) with a specific activity of 24 Ci/mmol was prepared. It was shown that 3H]immunorphin binds with a high affinity to the non-opioid β-endorphin receptor of mouse peritoneal macrophages (K d 2.4 ± 0.1 nM). The specific binding of 3H]immunorphin to macrophages was inhibited by unlabeled β-endorphin (K i of the 3H]immunorphin-receptor complex 2.9 ± 0.2 nM) and was not inhibited by unlabeled naloxone, α-endorphin, γ-endorphin, and Met5]enkephalin (K i > 10 μM). Thirty fragments of β-endorphin were synthesized, and their ability to inhibit the specific binding of 3H]immunorphin to macrophages was studied. It was found that the shortest peptide having practically the same inhibitory activity as β-endorphin is its fragment 12–19 (K i 3.1 ± 0.3 nM). |
| |
Keywords: | β -endorphin macrophages peptides receptors |
本文献已被 SpringerLink 等数据库收录! |
|