Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.

• Misu, Ryosuke

• Noguchi, Taro

• Ohno, Hiroaki

• 大石, 真也

• Fujii, Nobutaka

抄録

Neurokinin B (NKB) is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R). NKB with the consensus sequence of the tachykinin peptide family also binds to other tachykinin receptors [neurokinin-1 receptor (NK1R) and neurokinin-2 receptor (NK2R)] with low selectivity. In order to identify the structural requirements for the development of novel potent and selective NK3R agonists, a structure-activity relationship (SAR) study of [MePhe(7)]-NKB and other naturally occurring tachykinin peptides was performed. The substitutions to naturally occurring tachykinins with Asp and MePhe improved the receptor binding and agonistic activity for NK3R. The corresponding substitutions to NKB provided an NK3R selective analog.

収録刊行物

• Bioorganic & medicinal chemistry

  Bioorganic & medicinal chemistry 21 (8), 2413-2417, 2013-04-15

  Elsevier BV

キーワード

• Neurokinin B
• [MePhe7]-neurokinin B
• NK3R
• Tachykinin
• GnRH

詳細情報

• CRID: 1050001335769652480
• NII論文ID: 120005244454
• NII書誌ID: AA10938083
• ISSN: 09680896
• HANDLE: 2433/173403
• 本文言語コード: en
• 資料種別: journal article
• データソース種別:
  • IRDB
  • CiNii Articles