脑啡肽酶
体内
脑啡肽酶
氨肽酶
药理学
炎症
体外
酶
结肠炎
化学
炎症性肠病
脑啡肽
医学
生物化学
免疫学
生物
疾病
氨基酸
内科学
受体
类阿片
亮氨酸
生物技术
作者
Elżbieta Kamysz,Maciej Sałaga,Małgorzata Sobocińska,Artur Giełdoń,Jakub Fichna
出处
期刊:Future Medicinal Chemistry
[Newlands Press Ltd]
日期:2016-11-15
卷期号:8 (18): 2231-2243
被引量:18
标识
DOI:10.4155/fmc-2016-0156
摘要
The pharmacotherapy of inflammatory bowel disease is difficult and currently available treatments bring mostly poor and unsatisfactory results.The purpose of this work was the synthesis of opiorphin, sialorphin, spinorphin and a series of their analogs and the in vitro characterization of their effect on degradation of enkephalin by neutral endopeptidase and aminopeptidase N. Consequently, we investigated in vivo the anti-inflammatory effect of the most active inhibitors selected in the in vitro studies (Pal-KKQRFSR & Pal-KKQHNPR). Putative inhibitor - enzyme (neutral endopeptidase or aminopeptidase N) complexes are also presented and their binding interfaces are identified.Our results suggest that Pal-KKQHNPR has the potential to become a valuable template for anti-inflammatory therapeutics for the treatment of GI tract inflammation.
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