Showing papers by "Thomas Ilg published in 2012"
TL;DR: Compounds were identified that show low µM to high nM half maximal inhibitory concentrations on insect TPS and that may serve as lead compounds for the development of insecticides with a novel mode of action.
Abstract: Trehalose phosphate synthase (EC 2.4.1.15; TPS) is the crucial enzyme for the biosynthesis of trehalose, the main haemolymph sugar of insects, and therefore a potential insecticidal molecular target. In this study, we report the functional heterologous expression of Drosophila melanogaster TPS, the gene identification, full length cDNA cloning and functional expression of cat flea (Ctenocephalides felis) TPS, and the Michaelis-Menten constants for their specific substrates glucose-6-phosphate and uridinediphosphate-glucose. A novel high throughput screening-compatible TPS assay and its use for the identification of the first potent insect TPS inhibitors from a large synthetic compound collection (>115 000 compounds) is described. One compound class that emerged in this screening, the 4-substituted 2,6-diamino-3,5-dicyano-4H-thiopyrans, was further investigated by analysing preliminary structure-activity relationships. Here, compounds were identified that show low µM to high nM half maximal inhibitory concentrations on insect TPS and that may serve as lead compounds for the development of insecticides with a novel mode of action.
25 citations
TL;DR: The apparent Michaelis–Menten constants K M and the molecular size of the recombinant enzyme are virtually identical to that of the native enzyme suggesting that the gene cloned in this study encodes the highly expressed AK enzyme of the sheep blowfly.
10 citations
Patent•
11 May 2012
TL;DR: In this paper, a veterinary composition for intramammary administration comprising a combination of an antibacterial agent and a Toll-Like-Receptor (TLR) agonist was described.
Abstract: The invention relates to a veterinary composition for intramammary administration comprising a combination of an antibacterial agent and a Toll-Like-Receptor (TLR) agonist and to the use of said composition for the treatment of mastitis in lactating ruminants.
4 citations