TP053 is a potent thienopyrimidine antitubercular agent that kills both replicating and nonreplicating Mycobacterium tuberculosis. It appears that TP053 is a prodrug, which is activated by mycothiol-dependent reductase Rv2466c.
potent thienopyrimidine antitubercular agent that kills both replicating and nonreplicating Mycobacterium tuberculosis.
The Journal of biological chemistry, 290(52), 31077-31089 (2015-11-08)
Rv2466c is a key oxidoreductase that mediates the reductive activation of TP053, a thienopyrimidine derivative that kills replicating and non-replicating Mycobacterium tuberculosis, but whose mode of action remains enigmatic. Rv2466c is a homodimer in which each subunit displays a modular
ACS chemical biology, 9(7), 1567-1575 (2014-06-01)
The emergence of multidrug- and extensively drug-resistant strains of Mycobacterium tuberculosis highlights the need to discover new antitubercular agents. Here we describe the synthesis and characterization of a new series of thienopyrimidine (TP) compounds that kill both replicating and non-replicating
The Journal of biological chemistry, 292(32), 13097-13110 (2017-06-18)
The Mycobacterium tuberculosis rv2466c gene encodes an oxidoreductase enzyme annotated as DsbA. It has a CPWC active-site motif embedded within its thioredoxin fold domain and mediates the activation of the prodrug TP053, a thienopyrimidine derivative that kills both replicating and
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