期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 9, 期 3, 页码 210-214出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00477
关键词
Parasitic kinase inhibitor; stress-activated kinase; lymphatic filariasis
资金
- Margaret and Herman Sokol Endowment
- Celgene Global Health
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.
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