Synthesis and evaluation of microcin C analogs as aminoacyl-tRNA synthetase inhibitors. KU Leuven
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Synthesis of sugar- modified alpha-galactosylceramide (KRN 7000) analogues that potentially induce a Th1- polarised cytokine response mediated by NKT cells. The proposed modifications intent to establish an improved binding affinity with the CD1d protein, which should result in a bias towards a TH1 respons.
The synthesis of constrained x, B- or x, Y-diamino acid derivatives as building blocks for new substituted 2,4-diaminobutyric acid derivatives is of great importance in medicinal and agricultural chemistry. This research concerns the development of stereoselective syntheses and biochemical evaluation of new derivatives of 1,2-diaminocyclopropane-1-carboxylic acid, 2-amino-2-aziridin-2-ylacetic acid and 2-amino-3-aziridin-2-ylpropionic acid ...
A mevalonate independent pathway for isoprenoid biosynthesis, the so-called MEP pathway, has been discovered recently and validated as new drug target for the development of antimalarials. Fosmidomycin, a phosphonate that interferes with this pathway through inhibition of DOXP reductoisomerase, is a promising clinically effective antimalarial agent. This project aims at the development of of enantiomerically pure alpha-substituted ...
This project focusses on sucrose synthase as mediator for recycling of expensive nucleotide-activated sugar donors necessary for glycosylation of organic compounds by glycosyl transferases. To that end, an optimized variant of sucrose synthase will be generated by means of enzyme engineering. The whole process will be optimized and scaled-up to pilot facilities to allow for commercial exploitation of glycosylated compounds.
Glycosyltransferases are extremely efficient enzymes but require expensive nucleotide sugars as glycosyl donor. The current proposal aims to solve this problem by producing these compounds from sucrose (and analogues) as a cheap
and reactive substrate, using (mutant) sucrose synthase as biocatalyst.