TY - JOUR
T1 - Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis
AU - Tummalapalli, Sreedhar R.
AU - Bhat, Rohit
AU - Chojnowski, Agnieszka
AU - Prorok, Monika
AU - Kreiss, Tamara
AU - Goldberg, Ronald
AU - Canan, Stacie
AU - Hawryluk, Natalie
AU - Mortensen, Deborah
AU - Khetani, Vikram
AU - Zeldis, Jerome
AU - Siekierka, John J.
AU - Rotella, David P.
N1 - Publisher Copyright:
© 2018 American Chemical Society.
PY - 2018/3/8
Y1 - 2018/3/8
N2 - 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.
AB - 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.
KW - Parasitic kinase inhibitor
KW - lymphatic filariasis
KW - stress-activated kinase
UR - http://www.scopus.com/inward/record.url?scp=85043460516&partnerID=8YFLogxK
U2 - 10.1021/acsmedchemlett.7b00477
DO - 10.1021/acsmedchemlett.7b00477
M3 - Article
AN - SCOPUS:85043460516
SN - 1948-5875
VL - 9
SP - 210
EP - 214
JO - ACS Medicinal Chemistry Letters
JF - ACS Medicinal Chemistry Letters
IS - 3
ER -