A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity.

• Main Authors: Elizabeth R Sharlow (Author), Todd A Lyda (Author), Heidi C Dodson (Author), Gabriela Mustata (Author), Meredith T Morris (Author), Stephanie S Leimgruber (Author), Kuo-Hsiung Lee (Author), Yoshiki Kashiwada (Author), David Close (Author), John S Lazo (Author), James C Morris (Author)
• Format: Book
• Published: Public Library of Science (PLoS), 2010-04-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

The parasitic protozoan Trypanosoma brucei utilizes glycolysis exclusively for ATP production during infection of the mammalian host. The first step in this metabolic pathway is mediated by hexokinase (TbHK), an enzyme essential to the parasite that transfers the gamma-phospho of ATP to a hexose. He...