Barton, Victoria, Fisher, Nicholas, Biagini, Giancarlo ORCID: https://orcid.org/0000-0001-6356-6595, Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192 and O'Neill, Paul M. (2010) 'Inhibiting Plasmodium cytochrome bc1: a complex issue.'. Current Opinion in Chemical Biology, Vol 14, Issue 4, pp. 440-446.
Full text not available from this repository.Abstract
The cytochrome bc(1) complex is a key mitochondrial enzyme that catalyses transfer of electrons maintaining the membrane potential of mitochondria. Currently, atovaquone is the only drug in clinical use targeting the Plasmodium falciparum bc(1) complex. The rapid emergence of resistance to atovaquone resulted in a costly combination with proguanil (Malarone), limiting its widespread use in resource-poor disease-endemic areas. Cheaper alternatives that can overcome resistance are desperately required. Here we describe recent advances of bc(1)-targeted inhibitors that include hydroxynaphthoquinones (atovaquone analogues), pyridones (clodipol analogues), acridine related compounds (acridinediones and acridones) and quinolones. Significantly, many of these developmental compounds demonstrate little cross resistance with atovaquone-resistant parasite strains, and selected classes have excellent oral activity profiles in rodent models of malaria.
Item Type: | Article |
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Subjects: | QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials QX Parasitology > Protozoa > QX 135 Plasmodia |
Faculty: Department: | Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group |
Digital Object Identifer (DOI): | https://doi.org/10.1016/j.cbpa.2010.05.005 |
Depositing User: | Mary Creegan |
Date Deposited: | 13 Jun 2011 11:02 |
Last Modified: | 06 Feb 2018 13:03 |
URI: | https://archive.lstmed.ac.uk/id/eprint/2033 |
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