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ACS Med Chem Lett. 2013 Oct 30;5(1):12-7. doi: 10.1021/ml400259d. eCollection 2014 Jan 9.

Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.

Author information

1
National Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
2
Centre for Translational and Chemical Biology, School of Biological Sciences, University of Edinburgh , Michael Swann Building, The King's Buildings, Mayfield Road, Edinburgh EH9 3JR, U.K.
3
Research Unit for Tropical Diseases, de Duve Institute and Laboratory of Biochemistry, Université catholique de Louvain , Avenue Hippocrate 74, B-1200 Brussels, Belgium.

Abstract

Human African Trypanosomiasis (HAT) is a severe, often fatal disease caused by the parasitic protist Trypanosoma brucei. The glycolytic pathway has been identified as the sole mechanism for ATP generation in the infective stage of these organisms, and several glycolytic enzymes, phosphofructokinase (PFK) in particular, have shown promise as potential drug targets. Herein, we describe the discovery of ML251, a novel nanomolar inhibitor of T. brucei PFK, and the structure-activity relationships within the series.

KEYWORDS:

Trypanosoma brucei; Trypanosoma cruzi; glycolysis; high-throughput screening; inhibitors; phosphofructokinase

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