Studies on the active site-directed plasmin inhibitor: It may control plasmin having multifunctional properties

2015 Fiscal Year Final Research Report

• Project/Area Number: 25460164
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Kobe Gakuin University
• Principal Investigator: TSUDA YUKO 神戸学院大学, 薬学部, 教授 (10098478)
• Co-Investigator(Kenkyū-buntansha): HIDAKA KOUSHI 神戸学院大学, 薬学部, 講師 (30445960)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: プラスミン / 阻害剤 / 活性部位指向型 / 炎症性疾患治療薬

Outline of Final Research Achievements

Plasmin (PL) plays a dominant role in the fibrinolysis pathway so that PL inhibitors have been used as a hemostatic agent. Additionally, PL is activated in specific regions of the extracellular milieu to digest many proteins on the localized cell surface resulting in inducing cell inversion and metastasis and alternating the expression of cytokines. In this work, we disclosed 1) PL inhibitor (YO-2) attenuated both aGVHD- and colitis-associated lethality in mice; 2) more potent and selective PL inhibitor was obtained.

Free Research Field

医薬品化学