Given the therapeutic and commercial success of small-molecule enzyme inhibitors, as
exemplified by kinase inhibitors in oncology, a major focus of current drug-discovery and …

2017 marks the 60th anniversary of Krebs' seminal paper on the glyoxylate shunt (and
coincidentally, also the 80th anniversary of his discovery of the citric acid cycle). Sixty years …

Covalent enzyme inhibitors are widely applied as biochemical tools and therapeutic agents.
As a complement to categorization of these inhibitors by reactive group or modification site …

Covalent inhibitors are experiencing a growing resurgence in drug design and are an
increasingly useful tool in molecular biology. The ability to attach inhibitors to their targets by …

Itaconate is a mammalian antimicrobial metabolite that inhibits the isocitrate lyases (ICLs) of
Mycobacterium tuberculosis. Herein, we report that ICLs form a covalent adduct with …

The mechanisms whereby Mycobacterium tuberculosis (Mtb) rewires the host metabolism in
vivo are surprisingly unexplored. Here, we used three high-resolution mass spectrometry …

The recent clinical and commercial success of covalent drugs has prompted a renewed
interest in covalent inhibitors as therapeutic agents. With this has come an increased …

Isocitrate lyase is important for lipid utilisation by Mycobacterium tuberculosis but its ICL2
isoform is poorly understood. Here we report that binding of the lipid metabolites acetyl-CoA …

Latent tuberculosis infection (LTBI) represents a major challenge to curing TB disease.
Current guidelines for LTBI management include only three older drugs and their …

We report the unprecedented reaction between a nitroalkane and an active-site cysteine
residue to yield a thiohydroximate adduct. Structural and kinetic evidence suggests the nitro …