Identification via a Parallel Hit Progression Strategy of Improved Small Molecule Inhibitors of the Malaria Purine Uptake Transporter that Inhibit Plasmodium falciparum Parasite Proliferation

• Published in: ACS infectious diseases Vol. 5; no. 10; pp. 1738 - 1753
• Main Authors: Sosa, Yvett, Deniskin, Roman, Frame, I. J, Steiginga, Matthew S, Bandyopadhyay, Deepak, Graybill, Todd L, Kallal, Lorena A, Ouellette, Michael T, Pope, Andrew J, Widdowson, Katherine L, Young, Robert J, Akabas, Myles H
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 11.10.2019
• Subjects: high throughput screen; drug discovery; malaria; purine; transporter

Emerging resistance to current antimalarial medicines underscores the importance of identifying new drug targets and novel compounds. Malaria parasites are purine auxotrophic and import purines via the Plasmodium falciparum equilibrative nucleoside transporter type 1 (PfENT1). We previously showed t...