EC Clinical and Medical Case Reports

Tuberculosis stands as a menacing infectious disease that has instilled worldwide apprehension owing to its profound impact on the well-being of afflicted individuals. Ethionamide is the second line drug therapy for active multidrug resistant tuberculosis. Functional impairment of EthA enzyme which is responsible for the activation of ETH (Ethionamide) result in drug resistance in Mtb. To combat against Ethionamide resistance and boost up its activity against Mtb in second line therapy of tuberculosis, various types of ETH boosters have been designed and/or developed by different strategies. These Ethionamide promoters work by upregulating the action of EthA enzyme. The gene responsible for downregulation of EthA enzyme is EthR gene and the process is called as ETH repression which is the cause of drug resistance. So, to get prevail over this Ethionamide resistance and to enhance ETH activation in Mtb infected cell, EthR inhibitors are designed and developed to upregulate the EthA enzyme. EthR inhibitors demonstrated the desired interaction into its DNA recognition site that results into inhibition of EthR activation.

 Keywords: Ethionamide repressor (EthR); Ethionamide (ETH); Ethionamide activator; Mycobacterium tuberculosis (Mtb)

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