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Recent developments in trans-sialidase inhibitors of Trypanosoma cruzi
- Source :
- Journal of drug targeting. 25(6)
- Publication Year :
- 2017
-
Abstract
- Chagas is a lethal chronic disease that currently affects 8–10 million people worldwide, primarily in South and Central America. Trypanosoma cruzi trans-sialidase is an enzyme that is of vital importance for the survival of the parasite due to its key role in the transfer of sialic acid from the host to the parasite surface and it also helps the parasite combat the host’s immune system. This enzyme has no equivalent human enzyme; thus, it has become an interesting target for the development of inhibitors that combat the parasite. In this review, we summarize three classes of inhibitors (acceptor, donor and unrelated) with their inhibition values and their mode of action against this enzyme. Based on molecular docking, molecular dynamics and structure-activity relationship studies, it has been discovered that the molecules with –NH2, –OH and –COOH groups on an aromatic ring could be used as a scaffold for the development of new and potent trans-sialidase inhibitors due to their key interaction with...
- Subjects :
- 0301 basic medicine
Trypanosoma cruzi
Pharmaceutical Science
Neuraminidase
Sialidase
01 natural sciences
03 medical and health sciences
chemistry.chemical_compound
Structure-Activity Relationship
Immune system
Parasite hosting
Animals
Humans
Chagas Disease
Enzyme Inhibitors
Mode of action
Glycoproteins
chemistry.chemical_classification
Binding Sites
biology
010405 organic chemistry
biology.organism_classification
Trypanocidal Agents
0104 chemical sciences
Sialic acid
Molecular Docking Simulation
030104 developmental biology
Enzyme
chemistry
Biochemistry
Drug Design
Trans-acting
Subjects
Details
- ISSN :
- 10292330
- Volume :
- 25
- Issue :
- 6
- Database :
- OpenAIRE
- Journal :
- Journal of drug targeting
- Accession number :
- edsair.doi.dedup.....0c7440a33a9a6fbace2cecec3e8813b6