論文

査読有り 国際誌
2002年

Design and Synthesis of novel tetra-peptide motilin agonists

Bioorganic and Medicinal Chemistry
  • Masayuki Haramura
  • ,
  • Kouichi Tsuzuki
  • ,
  • Akira Okamachi
  • ,
  • Kenji Yogo
  • ,
  • Makoto Ikuta
  • ,
  • Toshiro Kozono
  • ,
  • Hisanori Takanashi
  • ,
  • Eigoro Murayama

10
6
開始ページ
1805
終了ページ
1811
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/S0968-0896(02)00027-5

A series of novel tetra-peptide motilin agonists, having the general structure H-Phe-Val-X-Ile-NH2, were designed, on the basis of structure-activity relationship studies of motilin. Peptides, in which X is a side chain substituted tryptophan residue, have agonistic activity. H-Phe-Val-Trp(2′-CH2CH2OH)-Ile-NH2(7), H-Phe-Val-Trp(2′-SCH3)-Ile-NH2(8), and H-Phe-Val-Trp(2′-SCH2CH2CH3)-Ile-NH 2 (9), showed an EC50 for contractile activity in the rabbit smooth muscle of 14.1±3.2, 12.9±4.1, and 4.6±1.6 μM, respectively. Interaction of the tryptophan aliphatic side chain with motilin receptor appears to influence the signal transduction via motilin receptor. © 2002 Elsevier Science Ltd. All rights reserved.

リンク情報
DOI
https://doi.org/10.1016/S0968-0896(02)00027-5
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/11937338
Scopus
https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=0036009877&origin=inward
Scopus Citedby
https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=0036009877&origin=inward
ID情報
  • DOI : 10.1016/S0968-0896(02)00027-5
  • ISSN : 0968-0896
  • PubMed ID : 11937338
  • SCOPUS ID : 0036009877

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