Document Type
Article
Publication Date
3-8-2018
Journal / Book Title
ACS medicinal chemistry letters
Abstract
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.
DOI
10.1021/acsmedchemlett.7b00477
Montclair State University Digital Commons Citation
Tummalapalli, Sreedhar R.; Bhat, Rohit; Chojnowski, Agnieszka; Prorok, Monika; Kreiss, Tamara; Goldberg, Ronald; Canan, Stacie; Hawryluk, Natalie; Mortensen, Deborah; Khetani, Vikram; Zeldis, Jerome; Siekierka, John; and Rotella, David, "Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis" (2018). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 182.
https://digitalcommons.montclair.edu/chem-biochem-facpubs/182
Published Citation
Tummalapalli, S. R., Bhat, R., Chojnowski, A., Prorok, M., Kreiss, T., Goldberg, R., ... & Rotella, D. P. (2018). Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis. ACS medicinal chemistry letters, 9(3), 210-214.