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DprE1 as a Drug Target from Mycobacterium Tuberculosis

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Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis

Paul Joseph Dyson, Stewart Cole, John McKinney, Neeraj Dhar, Florence Pojer, Joao Pedro De Almeida Neres, Elizabeth Fullam

The benzothiazinone BTZ043 is a tuberculosis drug candidate with nanomolar whole-cell activity. BTZ043 targets the DprE1 catalytic component of the essential enzyme decaprenylphosphoryl-beta-D-ribofuranose-2'-epimerase, thus blocking biosynthesis of arabin ...

American Association for the Advancement of Science2012

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Benzothiazinones (BTZ) are a new class of drug candidates to combat tuberculosis that inhibit decaprenyl-phosphoribose epimerase (DprE1), an essential enzyme involved in arabinan biosynthesis. Using the checkerboard method and cell viability assays, we hav ...

Amer Soc Microbiology2012

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Benzothiazinones (BTZs) are antituberculosis drug candidates with nanomolar bactericidal activity against tubercle bacilli. Here we demonstrate that BTZs are suicide substrates of the FAD-dependent decaprenylphosphoryl-beta-D-ribofuranose 2'-oxidase DprE1, ...

2012

Towards a new tuberculosis drug: pyridomycin - nature's isoniazid

Stewart Cole, Florence Pojer, Claudia Sala, Ruben Hartkoorn, Joao Pedro De Almeida Neres, Swapna Uplekar, Raju Mukherjee, Sophie Magnet

Tuberculosis, a global threat to public health, is becoming untreatable due to widespread drug resistance to frontline drugs such as the InhA-inhibitor isoniazid. Historically, by inhibiting highly vulnerable targets, natural products have been an importan ...

Wiley Open Access2012

Measuring net protease activities in biological samples using selective peptidic inhibitors

Christian Heinis, Alessandro Angelini, Philippe Diderich, Lisa Pollaro, Silvia Bellotto, Hermann A. Wegner

The measurement of activities from individual proteases in biological samples is difficult because of the numerous proteases, their overlapping activities, and the lack of specific substrates. We applied selective protease inhibitors based on bicyclic pept ...

2012

New tuberculosis drugs on the horizon

Stewart Cole

Tuberculosis (TB) remains a major global health concern whose control has been exacerbated by HIV and the emergence of multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains of Mycobacterium tuberculosis. The demand for new and faster ...

2011

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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 ...

American Chemical Society2010

Decaprenylphosphoryl-beta-D-Ribose 2 '-Epimerase from Mycobacterium tuberculosis is a Magic Drug Target

Giulia Manina

Tuberculosis is still a leading cause of death in developing countries and a resurgent disease in developed countries. The selection and soaring spread of Mycobacterium tuberculosis multidrug-resistant (MDR-TB) and extensively drug-resistant strains (XDR-T ...

2010

Dual role of isocitrate lyase 1 in the glyoxylate and methylcitrate cycles in Mycobacterium tuberculosis

John McKinney

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 ...

2006

Genomics and the chemotherapy of leprosy

Stewart Cole

The information deduced from the genome sequence of Mycobacterium leprae is of immense value for the chemotherapy of leprosy. Knowing the complete set of genes, enzymes and proteins allows us to understand why some drugs are without effect whereas others a ...

2002