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Activation of Calcitonin Gene-Related Peptide and Adrenomedullin Receptors by PEGylated Adrenomedullin 明石, 絵美子 34672 アカシ, エミコ Akashi, Emiko Nagata, Sayaka 7827 Yamasaki, Motoo 34475 北村, 和雄 7929 キタムラ, カズオ 50204912 Kitamura, Kazuo adrenomedullin calcitonin gene-related peptide polyethylene glycol receptor activity-modifying protein calcitonin receptor-like receptor inflammatory bowel disease Adrenomedullin (AM) improves colitis in animal models and patients with inflammatory bowel disease. We have developed a PEGylated AM derivative (PEG-AM) for clinical application because AM has a short half-life in the blood. However, modification by addition of polyethylene glycol (PEG) may compromise the function of the original peptide. In this paper, we examined the time course of cAMP accumulation induced by 5 and 60 kDa PEG-AM and compared the activation of calcitonin gene-related peptide (CGRP), AM1 and AM2 receptors by AM, 5 and 60 kDa PEG-AM. We also evaluated the effects of antagonists on the action of 5 and 60 kDa PEG-AM. PEG-AM stimulated cAMP production induced by these receptors; the increase in cAMP levels resulting from application of PEG-AM peaked at 15 min. Moreover, PEG-AM activity was antagonized by CGRP (8–37) or AM (22–52) (antagonists of CGRP and AM receptors, respectively) and the maximal response was not suppressed. These findings indicate that the effects of PEG-AM are similar to those of native AM. Citation: Akashi, E., Nagata, S., Yamasaki, M., & Kitamura, K. (2020). Activation of Calcitonin Gene-Related Peptide and Adrenomedullin Receptors by PEGylated Adrenomedullin. Biological & pharmaceutical bulletin, 43(11), 1799–1803. https://doi.org/10.1248/bpb.b20-00373 Pharmaceutical Society of Japan 2020-11-01 VoR journal article application/pdf Biological and Pharmaceutical Bulletin 11 43 1799 1803 0918-6158 https://miyazaki-u.repo.nii.ac.jp/record/2000170/files/論文(Akashi).pdf http://hdl.handle.net/10458/0002000170 https://miyazaki-u.repo.nii.ac.jp/records/2000170 eng © 2020 The Pharmaceutical Society of Japan open access