Now showing items 1-10 of 48
The development of selective inhibitors of NagZ : increased susceptibility of Gram-negative bacteria to β-lactams
(2013-10) - Journal article,
The increasing incidence of inducible chromosomal AmpC β-lactamases within the clinic is a growing concern because these enzymes deactivate a broad range of even the most recently developed β-lactam antibiotics. As a result, ...
Non-natural acetogenin analogues as potent Trypanosoma brucei inhibitors
(2014-11) - Journal article,
Neglected tropical diseases remain a serious global health concern. Here, a series of novel bis-tetrahydropyran 1,4-triazole analogues based on the framework of chamuvarinin, a polyketide natural product isolated from the ...
One origin for metallo-β-lactamase activity, or two? An investigation assessing a diverse set of reconstructed ancestral sequences based on a sample of phylogenetic trees
(2014-10) - Journal article,
Bacteria use metallo-β-lactamase enzymes to hydrolyse lactam rings found in many antibiotics, rendering them ineffective. Metallo-β-lactamase activity is thought to be polyphyletic, having arisen on more than one occasion ...
The cyanobactin heterocyclase enzyme : A processive adenylase that operates with a defined order of reaction
(2013-12) - Journal article,
ALDH2 mediates 5-nitrofuran activity in multiple species
(2012-07-27) - Journal article,
Understanding how drugs work in vivo is critical for drug design and for maximizing the potential of currently available drugs. 5-nitrofurans are a class of pro-drugs widely used to treat bacterial and trypanosome infections, ...
Biochemical characterization of the initial steps of the Kennedy pathway in Trypanosoma brucei : the ethanolamine and choline kinases
(2008-10-01) - Journal article,
Ethanolamine and choline are major components of the trypanosome membrane phospholipids, in the form of GPEtn (glycero-phosphoethanolamine) and GPCho (glycerophosphocholine). Ethanolamine is also found as an integral ...
An enzymatic route to selenazolines
(2013-03-18) - Journal article,
Ringing the changes: Selenazolines have applications in medicinal chemistry, but their synthesis is challenging. We report a new convenient and less toxic route to these heterocycles that starts from commercially available ...
The respiratory arsenite oxidase : structure and the role of residues surrounding the rieske cluster
(2013-08-30) - Journal article,
The arsenite oxidase (Aio) from the facultative autotrophic Alphaproteobacterium Rhizobium sp. NT-26 is a bioenergetic enzyme involved in the oxidation of arsenite to arsenate. The enzyme from the distantly related ...
The AEROPATH project targeting Pseudomonas aeruginosa : crystallographic studies for assessment of potential targets in early-stage drug discovery
(2013-01) - Journal article,
Bacterial infections are increasingly difficult to treat owing to the spread of antibiotic resistance. A major concern is Gram-negative bacteria, for which the discovery of new antimicrobial drugs has been particularly ...