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Targeting Trypanosoma cruzi Sterol 14α-Demethylase (CYP51)
| Content Provider | PubMed Central |
|---|---|
| Author | Lepesheva, Galina I. Villalta, Fernando Waterman, Michael R. |
| Copyright Year | 2011 |
| Abstract | There are at least two obvious features that must be considered upon targeting specific metabolic pathways/enzymes for drug development: the pathway must be essential and the enzyme must allow the design of pharmacologically useful inhibitors. Here, we describe Trypanosoma cruzi sterol 14α-demethylase as a promising target for anti-Chagasic chemotherapy. The use of anti-fungal azoles, which block sterol biosynthesis and therefore membrane formation in fungi, against the protozoan parasite has turned out to be highly successful: a broad spectrum anti-fungal drug, the triazole compound posaconazole, is now entering phase II clinical trials for treatment of Chagas disease. This review summarizes comparative information on anti-fungal azoles and novel inhibitory scaffolds selective for Trypanosomatidae sterol 14α-demethylase through the lens of recent structure/functional characterization of the target enzyme. We believe our studies open wide opportunities for rational design of novel, pathogen-specific and therefore more potent and efficient anti-trypanosomal drugs. |
| Related Links | http://dx.doi.org/10.1016/b978-0-12-385863-4.00004-6 |
| Ending Page | 87 |
| Page Count | 23 |
| Starting Page | 65 |
| File Format | |
| ISSN | 0065308X |
| Journal | Advances in parasitology |
| Volume Number | 75 |
| Language | English |
| Publisher Date | 2011-01-01 |
| Access Restriction | Open |
| Subject Keyword | Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Medicine Parasitology |
