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Abstract

Grant Number:	1R03MH082340-01A1
Project Title:	Identification of Inhibitors of Trypanosoma Brucei Hexokinases

PI Information:	Name	Email	Title
	MORRIS, JAMES CULVIN.	jmorri2@clemson.edu

Abstract: DESCRIPTION (provided by applicant): Current therapies for African sleeping sickness, caused by the protozoan parasite Trypanosoma brucei, are toxic and inefficacious. Glycolysis is a promising target in the fight against T. brucei, as the pathway is essential. Inhibitors of hexokinase (TbHK), a key glycolytic enzyme, have been shown to be toxic to trypanosomes. Since the trypanosomal HKs share little similarity with their human counterpart, they make a promising target for therapy development. We have recently cloned and expressed active recombinant TbHK, and have modified standard enzyme assays for high throughput identification of inhibitors. Here we propose to provide the Molecular Libraries Screening Centers Network with sufficient recombinant protein (and the methods used to monitor its activity under high throughput conditions) in order to identify inhibitors that may prove useful lead compounds as both anti-trypanosomal drugs and as tools for better understanding of the biochemistry of TbHKs.

Public Health Relevance:
This Public Health Relevance is not available.

Thesaurus Terms:
Trypanosoma brucei, enzyme activity, enzyme inhibitor, hexokinase, high throughput technology
peptide library, recombinant protein, small molecule
NIH Roadmap Initiative tag, biotechnology

Institution:	CLEMSON UNIVERSITY
	OFFICE OF SPONSORED PROGRAMS
	CLEMSON, SC 296345702
Fiscal Year:	2007
Department:	GENETICS AND BIOCHEMISTRY (0318)
Project Start:	29-SEP-2007
Project End:	31-AUG-2008
ICD:	NATIONAL INSTITUTE OF MENTAL HEALTH
IRG:	ZMH1

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