Hexanoylation of a VPAC 2 receptor-preferring ligand markedly increased its selectivity and potency
作者: Ingrid LangerFrançoise GregoireIngrid NachtergaelPhilippe De NeefPascale VertongenPatrick Robberecht
作者单位: 1Department of Biochemistry and Nutrition, School of Medicine, Université Libre de Bruxelles, Bât G/E, CP 611, 808 Route de Lennik, B-1070 Bruxelles, Belgium
刊名: Peptides, 2003, Vol.25 (2), pp.275-278
来源数据库: Elsevier Journal
DOI: 10.1016/j.peptides.2003.12.013
原始语种摘要: Abstract(#br)We synthesized a VIP analog that combines mutations that decrease the affinity for the VPAC 1 receptor but maintain a high affinity for the VPAC 2 receptor with an amino-terminal hexanoylation that increases the affinity for the VPAC 2 receptor with a limited decrease in the affinity of the VPAC 1 receptor. The resulting Hexanoyl[A 19 ,K 27,28 ]VIP had the expected properties of a high affinity for the VPAC 2 receptor and a low affinity for the VPAC 1 receptor and also a low affinity for the PAC 1 and secretin receptors. With a 1000-fold preference for the VPAC 2 receptor and a IC 50 value of binding of 1nM, this compound is the most potent and the most selective agonist presently described.
全文获取路径: Elsevier  (合作)
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影响因子:2.522 (2012)

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关键词翻译
关键词翻译
  • receptor 接受体
  • affinity 亲和力
  • potency 潜力
  • ligand 配合体
  • increased 增加
  • selectivity 选择性
  • presently 不久
  • expected 预期
  • maintain 
  • resulting 引起的