PROBLEM TO BE SOLVED: To provide a novel PAI-1 inhibitor, and a method for inhibiting PAI-1 activity using the PAI-1 inhibitor.SOLUTION: The invention provides: a PAI-1 inhibitor which inhibits the intramolecular interaction between a first region consisting of 3-9 amino acid residues comprising the glycine residue at position 374 in PAI-1 (plasminogen activator inhibitor 1) and a second region comprising the region from the asparagine at position 31 to the serine at position 35 in PAI-1 and a method for inhibiting PAI-1 activity which inhibits the intramolecular interaction between the first region and the second region in PAI-1 by binding a substance capable of binding to the first region consisting of the 3-9 amino acid residues comprising the glycine residue at position 374 in PAI-1 or the second region comprising the region from the asparagine at position 31 to the serine at position 35 in PAI-1, to PAI-1, in vitro or in vivo (where in vivo of human is excluded).COPYRIGHT: (C)2015,JPO&INPIT【課題】本発明は、新規なPAI-1阻害剤、及び当該PAI-1阻害剤を用いてPAI-1活性を阻害する方法を提供することを課題とする。【解決手段】PAI-1(プラスミノゲンアクチベータインヒビター-1)中の374位のグリシン残基を含む3~9のアミノ酸残基からなる第1領域とPAI-1の31位のアスパラギンから35位のセリンまでの領域を含む第2領域との分子内相互作用を阻害する、PAI-1阻害剤、及び、in vitro又はin vivo(但し、ヒトの生体内を除く。)において、PAI-1中の374位のグリシン残基を含む3~9のアミノ酸残基からなる第1領域又はPAI-1の31位のアスパラギンから35位のセリンまでの領域を含む第2領域に結合可能な物質とPAI-1とを結合させることにより、PAI-1中の前記第1領域と前記第2領域との分子内相互作用を阻害する、PAI-1活性の阻害方法。【選択図】なし
