Evaluation of bisbenzamidines as inhibitors for matriptase-2

Beckmann Anna-Madeleine; Gilberg Erik; Gattner Susanne; Huang Tien L.; Eynde Jean Jacques Vanden; Mayence Annie; Bajorath Juergen; Stirnberg Marit; Guetschow Michael

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Evaluation of bisbenzamidines as inhibitors for matriptase-2

【24h】

Evaluation of bisbenzamidines as inhibitors for matriptase-2

机译：评估双苯甲m作为Matriptase-2抑制剂

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

The serine protease matriptase-2 has attracted much attention as a potential target for the treatment of iron overload diseases. In this study, a series of 27 symmetric, achiral bisbenzamidines was evaluated for inhibitory activity against human matriptase-2, against the closely related enzyme human matriptase, as well as against human thrombin, bovine factor Xa and human trypsin. The conformationally restricted piperazine derivative 19 and the oxamide-derived bisbenzamidine 1 were identified as the most potent inhibitors of this series for matriptase-2 and matriptase, respectively. (C) 2016 Elsevier Ltd. All rights reserved.

机译：丝氨酸蛋白酶Matriptase-2作为治疗铁超负荷疾病的潜在靶点已引起了广泛关注。在这项研究中，评估了一系列27种对称的非手性双苯甲m对人matriptase-2，紧密相关的人matriptase酶以及人凝血酶，牛因子Xa和人胰蛋白酶的抑制活性。构象受限的哌嗪衍生物19和草酰胺衍生的双苯甲m1分别被确定为该系列中对matriptase-2和matriptase最有效的抑制剂。（C）2016 Elsevier Ltd.保留所有权利。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2016年第15期|共5页
作者
Beckmann Anna-Madeleine; Gilberg Erik; Gattner Susanne; Huang Tien L.; Eynde Jean Jacques Vanden; Mayence Annie; Bajorath Juergen; Stirnberg Marit; Guetschow Michael;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类
关键词
Bisbenzamidines; Matriptase-2; Serine proteases;

机译：双苯甲m;Matriptase-2;丝氨酸蛋白酶;

相似文献

外文文献
中文文献
专利

1. Evaluation of bisbenzamidines as inhibitors for matriptase-2 [J] . Beckmann Anna-Madeleine, Gilberg Erik, Gattner Susanne, Bioorganic and Medicinal Chemistry Letters . 2016,第15期

机译：评估双苯甲m作为Matriptase-2抑制剂
2. Hepatocyte growth factor activator inhibitor type?2 (HAI-2) modulates hepcidin expression by inhibiting the cell surface protease matriptase-2 [J] . Eva Maurer, Marit Stirnberg, Michael Gütschow The biochemical journal . 2013,第3期

机译：肝细胞生长因子激活因子抑制剂2型（HAI-2）通过抑制细胞表面蛋白酶matriptase-2来调节hepcidin表达
3. Hepatocyte growth factor activator inhibitor type 2 (HAI-2) modulates hepcidin expression by inhibiting the cell surface protease matriptase-2 [J] . Maurer Eva, Guetschow Michael, Stirnberg Marit The Biochemical Journal . 2013,第Pta3期

机译：2型肝细胞生长因子激活因子抑制剂（HAI-2）通过抑制细胞表面蛋白酶matriptase-2来调节hepcidin表达
4. Quantitative Evaluation of Corrosion Inhibitors in the Laboratory: The First Step for Successful Application of Inhibitors in the Oil and Gas Industry [C] . Sankara Papavinasam, Radha Venkatesan, Sai Mudiam NACE international corrosion conference and expo . 2019

机译：实验室中腐蚀抑制剂的定量评估：抑制剂在石油和天然气工业中成功应用的第一步
5. Design, Synthesis, and Biological Evaluation of Non-Symmetric Small Molecules as Inhibitors of Plasminogen Activator Inhibitor (PAI-1). [D] . Anumala, Himabindu. 2014

机译：非对称小分子作为纤溶酶原激活物抑制剂（PAI-1）的抑制剂的设计，合成和生物学评估。
6. A Short Peptide Inhibitor as an Activity-Based Probe for Matriptase-2 [O] . Martin Mangold, Michael Gütschow, Marit Stirnberg 2018

机译：短肽抑制剂作为Matriptase-2的基于活性的探针。
7. A Short Peptide Inhibitor as an Activity-Based Probe for Matriptase-2 [O] . Martin Mangold, Michael Gütschow, Marit Stirnberg 2018

机译：作为基于活性的基于活性探针的短肽抑制剂-2
8. Field Evaluation of Corrosion Inhibitors for Concrete: Interim Report 2.211 Evaluation of Installation and Initial Condition of Bridge Repairs Done with 211 Corrosion-Inhibiting Admixtures and Topical Treatments [R] . Sprinkel, M. M., Ozyildirim, C. 1999

机译：混凝土缓蚀剂的现场评估：中期报告2.211使用211防腐蚀外加剂和局部处理评估桥梁维修的安装和初始条件

Evaluation of bisbenzamidines as inhibitors for matriptase-2

摘要

著录项

相似文献

相关主题

期刊订阅