Abstract
The information of the complete genome sequences of Trypanosoma cruzi revealed that its genome contains nearly to 10,000 protein-coding genes. This vast amount of new information allows the identification of therapeutic targets in an accurate and undoubtedly forms. The current post-genomic period is a special moment in the anti-T. cruzi drug discovery and development ushering this moment as the anti-Chagas drug discovery era. In this review we describe, from a medicinal chemistry point of view, several identified potential biological targets for drugs development. We discuss the validity and druggability as anti-Chagas objectives of prenyl converting and transferring enzymes, cAMP-specific phosphodiesterases, polyamine and trypanothione synthetic pathways, triosephosphate isomerase, α-hydroxyacid dehydrogenases and trans-sialidase.
Keywords: Chagas' disease, enzymatic inhibitors, drugs development, Trypanosoma cruzi, ergosterol biosynthetic pathway, trypanothione reductase, farnesyltransferase inhibitors, cAMP-specific phosphodiesterases, Dipyridamole, sulfinyl radicals, glutathionylated products
Current Enzyme Inhibition
Title: Targets for Anti-T. cruzi Drugs in the Post-Genomic Era
Volume: 6 Issue: 4
Author(s): Alicia Merlino, Mercedes Gonzalez and Hugo Cerecetto
Affiliation:
Keywords: Chagas' disease, enzymatic inhibitors, drugs development, Trypanosoma cruzi, ergosterol biosynthetic pathway, trypanothione reductase, farnesyltransferase inhibitors, cAMP-specific phosphodiesterases, Dipyridamole, sulfinyl radicals, glutathionylated products
Abstract: The information of the complete genome sequences of Trypanosoma cruzi revealed that its genome contains nearly to 10,000 protein-coding genes. This vast amount of new information allows the identification of therapeutic targets in an accurate and undoubtedly forms. The current post-genomic period is a special moment in the anti-T. cruzi drug discovery and development ushering this moment as the anti-Chagas drug discovery era. In this review we describe, from a medicinal chemistry point of view, several identified potential biological targets for drugs development. We discuss the validity and druggability as anti-Chagas objectives of prenyl converting and transferring enzymes, cAMP-specific phosphodiesterases, polyamine and trypanothione synthetic pathways, triosephosphate isomerase, α-hydroxyacid dehydrogenases and trans-sialidase.
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Cite this article as:
Merlino Alicia, Gonzalez Mercedes and Cerecetto Hugo, Targets for Anti-T. cruzi Drugs in the Post-Genomic Era, Current Enzyme Inhibition 2010; 6 (4) . https://dx.doi.org/10.2174/157340810794578533
DOI https://dx.doi.org/10.2174/157340810794578533 |
Print ISSN 1573-4080 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6662 |
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