Inter- and intramolecular domain interactions of the catalase-peroxidase KatG from M. tuberculosis
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The exact role of the DosR "dormancy" regulon in the pathogenesis of Mycobacterium tuberculosis is still unclear. It has been observed that members of the regulon, including dosR, are constitutively expressed in clinical isolates belonging to the W/Beijing ...
New drugs are required to counter the tuberculosis (TB) pandemic. Here, we describe the synthesis and characterization of 1,3-benzothiazin-4-ones (BTZs), a new class of antimycobacterial agents that kill Mycobacterium tuberculosis in vitro, ex vivo, and in ...
Benzothiazinones (BTZs) form a new class of potent antimycobacterial agents. Although the target of BTZs has been identified as decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1), their detailed mechanism of action remains obscure. Here we demonstrate th ...
The new antitubercular drug candidate 2-[2-S-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one (BTZ043) targets the DprE1 (Rv3790) subunit of the enzyme decaprenylphosphoryl-beta-d-ribose 2'-epimerase. To monit ...
We numerically study the dependence of the dynamics on the range of interaction Δ for the short-range square well potential. We find that, for small Δ, dynamics scale exactly in the same way as thermodynamics, both for Newtonian and Brownian microscopic dy ...
Tuberculosis is a chronic infectious disease caused by bacteria of the Mycobacterium tuberculosis complex. One of the major contributors to virulence and intercellular spread of M. tuberculosis is the ESAT-6 secretion system 1 (ESX-1) that has been lost by ...
We recently reported that 3,3-dimethyl-3H-benzofuro[3,2,f][1]-benzopyran and its hydrogenated analogue are selective in vitro inhibitors of mycobacterial growth. However, their lack of in vivo activity on a murine model of Mycobacterium tuberculosis infect ...
In this issue of Chem. & Biol., the groups of Tawfik and Griffiths present fluorescence-activated cell sorting of double emulsions as a generally applicable screen for enzyme activity. This novel methodol. increases the throughput of a typical enzyme scree ...
The success of Mycobacterium tuberculosis as a pathogen is largely attributable to its ability to persist in host tissues, where drugs that are rapidly bactericidal in vitro require prolonged administration to achieve comparable effects. Latency is a frequ ...
The role of isocitrate lyase (ICL) in the glyoxylate cycle and its necessity for persistence and virulence of Mycobacterium tuberculosis has been well described. Recent reports have alluded to an additional role for this enzyme in M. tuberculosis metabolis ...
