Literature DB >> 11512153

Glycolysis as a target for the design of new anti-trypanosome drugs.

C L Verlinde1, V Hannaert, C Blonski, M Willson, J J Périé, L A Fothergill-Gilmore, F R Opperdoes, M H Gelb, W G Hol, P A Michels.   

Abstract

Glycolysis is perceived as a promising target for new drugs against parasitic trypanosomatid protozoa because this pathway plays an essential role in their ATP supply. Trypanosomatid glycolysis is unique in that it is compartmentalized, and many of its enzymes display unique structural and kinetic features. Structure- and catalytic mechanism-based approaches are applied to design compounds that inhibit the glycolytic enzymes of the parasites without affecting the corresponding proteins of the human host. For some trypanosomatid enzymes, potent and selective inhibitors have already been developed that affect only the growth of cultured trypanosomatids, and not mammalian cells.

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Year:  2001        PMID: 11512153     DOI: 10.1054/drup.2000.0177

Source DB:  PubMed          Journal:  Drug Resist Updat        ISSN: 1368-7646            Impact factor:   18.500


  50 in total

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3.  Crystallization and preliminary X-ray characterization of phosphoglucose isomerase from Mycobacterium tuberculosis H37Rv.

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4.  The crystal structure of glucokinase from Leishmania braziliensis.

Authors:  Gregory S Buechner; Matthew E Millington; Kay Perry; Edward L D'Antonio
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5.  Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.

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6.  In Vitro Testing of Potential Entamoeba histolytica Pyruvate Phosphate Dikinase Inhibitors.

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7.  Targeting the Pentose Phosphate Pathway: Characterization of a New 6PGL Inhibitor.

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8.  Glucose is toxic to glycosome-deficient trypanosomes.

Authors:  Tetsuya Furuya; Peter Kessler; Armando Jardim; Achim Schnaufer; Christopher Crudder; Marilyn Parsons
Journal:  Proc Natl Acad Sci U S A       Date:  2002-10-17       Impact factor: 11.205

9.  An expression system to screen for inhibitors of parasite glucose transporters.

Authors:  Torben Feistel; Cheryl A Hodson; David H Peyton; Scott M Landfear
Journal:  Mol Biochem Parasitol       Date:  2008-07-30       Impact factor: 1.759

10.  Structure-based approach to the identification of a novel group of selective glucosamine analogue inhibitors of Trypanosoma cruzi glucokinase.

Authors:  Edward L D'Antonio; Mason S Deinema; Sean P Kearns; Tyler A Frey; Scott Tanghe; Kay Perry; Timothy A Roy; Hanna S Gracz; Ana Rodriguez; Jennifer D'Antonio
Journal:  Mol Biochem Parasitol       Date:  2016-01-14       Impact factor: 1.759

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