Title：ONO-5046, a novel inhibitor of human neutrophil elastase

标题：ONO-5046，一种新型的人中性粒细胞弹性蛋白酶抑制剂

Authors: Kawabata K., Suzuki M., Sugitani M., Imaki K., Toda M., Miyamoto T.

作者：Kawabata K., Suzuki M., Sugitani M., Imaki K., Toda M., Miyamoto T.

Journal: Biochemical and Biophysical Research Communications

期刊：《生物化学与生物物理研究通讯》

Publication Date: June 14, 1991

出版日期：1991年6月14日

Volume/Issue: 177(2)
Pages: 814-820
DOI: 10.1016/0006-291x(91)91862-7

Abstract

The study introduces ONO-5046, a potent and specific inhibitor of human neutrophil elastase (HNE). Neutrophil elastase is an enzyme involved in the degradation of proteins during inflammation, and its overactivity can lead to tissue damage in various diseases, such as acute lung injury and chronic obstructive pulmonary disease (COPD).

摘要

本研究介绍了ONO-5046，一种有效且特异性强的人中性粒细胞弹性蛋白酶（HNE）抑制剂。中性粒细胞弹性蛋白酶是一种在炎症期间参与蛋白质降解的酶，其过度活性可能导致多种疾病中的组织损伤，如急性肺损伤和慢性阻塞性肺疾病（COPD）。

Key Findings

1. Inhibition Mechanism: ONO-5046 exhibits strong inhibitory effects on HNE with a high degree of specificity, meaning it does not significantly inhibit other proteases.
2. Biochemical Properties: The study provides detailed biochemical analysis, including the binding affinity and inhibitory concentration (IC50) of ONO-5046 against HNE.
3. Therapeutic Potential: Due to its specificity and potency, ONO-5046 is highlighted as a potential therapeutic agent for conditions involving excessive neutrophil elastase activity.

主要发现

1. 抑制机制： ONO-5046对HNE表现出强抑制作用，具有高度特异性，即对其他蛋白酶没有显著抑制作用。
2. 生化特性： 研究提供了详细的生化分析，包括ONO-5046对HNE的结合亲和力和抑制浓度（IC50）。
3. 治疗潜力： 由于其特异性和效力，ONO-5046被强调为治疗涉及过度中性粒细胞弹性蛋白酶活性的疾病的潜在药物。

Experimental Details

• Enzyme Assays: Various assays were conducted to determine the inhibitory effect of ONO-5046 on HNE.
• Comparative Analysis: ONO-5046 was compared with other elastase inhibitors, demonstrating superior specificity and potency.
• Cell Studies: The impact of ONO-5046 on neutrophil activity was assessed in cell culture models.

实验细节

• 酶测定： 进行了各种测定以确定ONO-5046对HNE的抑制作用。
• 比较分析： 将ONO-5046与其他弹性蛋白酶抑制剂进行比较，显示出优越的特异性和效力。
• 细胞研究： 在细胞培养模型中评估了ONO-5046对中性粒细胞活性的影响。

相关产品及其CAS号：

1.Nafamostat: CAS 81525-10-2

Nafamostat is a synthetic serine protease inhibitor that inhibits neutrophil elastase among other proteases.