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Heterocyclic chem. continues to be in the focus of life science-oriented research. Fluorine, a unique tool for finetuning biol. properties, offers an extra bonus in this context. The lecture features three pertinent issues. First, proven and novel routes t ...
We have expressed the 5-HT3 receptor with two transient expression sytems: the Semliki Forest virus and the HEK293EBNA. Both systems allow the rapid expression of functional receptor protein at very high level: up to 107 receptors per cell. Large scale pro ...
In this thesis, two different fluorescent labeling techniques for in vivo investigations on the 5-HT3 receptor (5-HT3R) functions are presented. This plasma membrane protein contains five subunits surrounding an ion channel that opens after binding of a 5- ...
Epidermal Langerhans cells (LC) play a pivotal role in initiating and maintaining primary immune responses in the skin. In the present study, we asked whether peroxisome proliferator-activated receptor-alpha (PPARalpha) activation modulates LC function. Ou ...
Disaccharide and oligosaccharide mimics are potentially more selective glycosidases inhibitors than simple monosaccharide mimics. They represent also more selective ligands for lectins and oligosaccharide receptors and can become immunostimulating agents. ...
Sequential stages in the life cycle of the ionotropic 5-HT3 receptor (5-HT3R) were resolved temporally and spatially in live cells by multicolor fluorescence confocal microscopy. The insertion of the enhanced cyan fluorescent protein into the large intrace ...
Chem. and biol. labeling is fundamental for the elucidation of the function of proteins within biochem. cellular networks. In particular, fluorescent probes allow detection of mol. interactions, mobility and conformational changes of proteins in live cells ...
23-Alkyl-substituted and 6,23-alkyl-disubstituted derivatives of chenodeoxycholic acid are identified as potent and selective agonists of TGR5, a G-protein coupled receptor for bile acids (BAs). In particular, we show that methylation at the C-23(S) positi ...
New 2-(aminomethyl)-5-(hydroxymethyl)pyrrolidine-3,4-diol derivatives were synthesized from (5S)-5-[(trityloxy)methyl]pyrrolidin-2-one (6) (Schemes 1 and 2) and their inhibitory activities toward 25 glycosidases assayed (Table). The influence of the config ...
Lipophilic polymer membranes incorporating binding sites are widely used in various potentiometric, amperometric, and optical sensors. Here, we report on the biofunctional modification of the surface of a Ca2+-selective membrane. A photoactivatable biotin ...