Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.
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ABSTRACT:
SUBMITTER: Tummalapalli SR
PROVIDER: S-EPMC5846038 | biostudies-literature | 2018 Mar
REPOSITORIES: biostudies-literature
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Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.
Tummalapalli Sreedhar R SR Bhat Rohit R Chojnowski Agnieszka A Prorok Monika M Kreiss Tamara T Goldberg Ronald R Canan Stacie S Hawryluk Natalie N Mortensen Deborah D Khetani Vikram V Zeldis Jerome J Siekierka John J JJ Rotella David P DP
ACS medicinal chemistry letters 20180209 3
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 bioavaila ...[more]
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