Rational drug design in parasitology: trans-sialidase as a case study for Chagas disease.

Abstract

Trypanosoma cruzi trans-sialidase is a potential target for Chagas disease chemotherapy. From the specific need of T. cruzi to obtain sialic acid through trans-sialidase-mediated transfers from host sources and the lack of alternative to this for the parasite, a good case can be made for T. cruzi trans-sialidase to serve as a potential drug target against Chagas disease. This review deals with both the particular aspects relevant to T. cruzi trans-sialidase as a target and generalises the situation for drug design in its broader aspects on the basis of some special problems in terms of rational drug design that T. cruzi trans-sialidase raises, particularly those of multiple gene copies and active site plasticity.

• Authors: João Neres, Richard A Bryce, Kenneth T Douglas
• Journal: Drug discovery today (Drug Discov Today) Vol. 13 Issue 3-4 Pg. 110-7 (Feb 2008) ISSN: 1359-6446 [Print] England
• PMID: 18275908 (Publication Type: Journal Article, Review)

Chemical References

• Antiprotozoal Agents
• Enzyme Inhibitors
• Glycoproteins
• trans-sialidase
• Neuraminidase

Topics

• Animals
• Antiprotozoal Agents (chemistry, pharmacology)
• Chagas Disease (drug therapy, enzymology, pathology)
• Drug Design
• Enzyme Inhibitors (chemistry, pharmacology)
• Glycoproteins (antagonists & inhibitors, metabolism)
• Humans
• Molecular Structure
• Neuraminidase (antagonists & inhibitors, metabolism)
• Parasitology (methods)
• Trypanosoma cruzi (drug effects, enzymology)