Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 9, Issue 3, Pages 210-214Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00477
Keywords
Parasitic kinase inhibitor; stress-activated kinase; lymphatic filariasis
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Funding
- Margaret and Herman Sokol Endowment
- Celgene Global Health
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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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