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Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-02-09 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00477
Sreedhar R. Tummalapalli 1 , Rohit Bhat 1 , Agnieszka Chojnowski 1 , Monika Prorok 1 , Tamara Kreiss 1 , Ronald Goldberg 1 , Stacie Canan 2 , Natalie Hawryluk 2 , Deborah Mortensen 2 , Vikram Khetani 3 , Jerome Zeldis 3 , John J. Siekierka 1 , David P. Rotella 1
Affiliation  

Lymphatic filariasis infects over 120 million people worldwide and can lead to significant disfigurement and disease. Resistance is emerging with current treatments, and these therapies have dose limiting adverse events; consequently new targets are needed. One approach to achieve this goal is inhibition of parasitic protein kinases involved in circumventing host defense mechanisms. This report describes structure–activity relationships leading to the identification of a potent, orally bioavailable stress activated protein kinase inhibitor that may be used to investigate this hypothesis.

中文翻译:

应激激活的蛋白激酶抑制剂的淋巴丝虫病的发现。

淋巴丝虫病在全世界感染超过1.2亿人,并可能导致严重的容貌和疾病。目前的治疗方法产生了耐药性,这些疗法具有限制剂量的不良事件。因此,需要新的目标。实现该目标的一种方法是抑制参与规避宿主防御机制的寄生蛋白激酶。该报告描述了结构-活性关系,从而确定了一种有效的,口服生物利用的应激活化蛋白激酶抑制剂,该抑制剂可用于研究该假设。
更新日期:2018-02-09
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