Abstract
The significant increase in the detection of drug-resistant strains of Mycobacterium tuberculosis caused an urgent need for the discovery new antituberculosis drugs. Development of bioinformatics and computational sciences enabled the progress of new strategies leading to design, discovery and identification of a series of interesting drug candidates. In this short review, we would like to present recently discovered compounds targeting important mycobacterial proteins: DNA topoisomerases and the transcriptional repressor of EthA monooxygenase - EthR.
Keywords:
drug target; ethionamide; fluoroquinolone; high-throughput screening; in silico docking; molecular hybridization; tuberculosis drug discovery.
MeSH terms
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Animals
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Antitubercular Agents / chemistry
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Antitubercular Agents / pharmacology*
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Antitubercular Agents / therapeutic use
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Bacterial Proteins / antagonists & inhibitors*
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Bacterial Proteins / metabolism
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DNA Topoisomerases / metabolism
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Drug Development
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Humans
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Mycobacterium tuberculosis / drug effects*
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Mycobacterium tuberculosis / metabolism
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Repressor Proteins / antagonists & inhibitors*
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Repressor Proteins / metabolism
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Topoisomerase Inhibitors / chemistry
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Topoisomerase Inhibitors / pharmacology*
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Topoisomerase Inhibitors / therapeutic use
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Tuberculosis / drug therapy*
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Tuberculosis / microbiology
Substances
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Antitubercular Agents
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Bacterial Proteins
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EthR protein, Mycobacterium tuberculosis
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Repressor Proteins
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Topoisomerase Inhibitors
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DNA Topoisomerases