Computational rewiring of allosteric pathways reprograms GPCR selective responses to ligands
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The serotonin type 3 receptor (5HT3R) is a homopentameric, cation selective channel that mediates fast excitatory transmission in the nervous system. It is a member of the Cys-loop family of receptors that include the nicotinic acetylcholine receptor (nACh ...
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 ...
The subject of this thesis is the study of the structure and function of the human muscle nicotinic acetylcholine receptor (nAChR), which is a typical member of the large class of ligand-gated ion channels. Appropriate techniques, like site-directed mutage ...
G-protein coupled receptors (GPCRs) are the most abundant class of proteins in the cell body. Such receptors are of major interest as potential therapeutic targets. Downscaling and parallelization of bioanalytics opens novel routes to rapidly screen and id ...
In this thesis, I show the ability of engineered bivalent ligands to control HER signaling by taking advantage of the dimerization-dependent mechanism of the four different receptors in the HER (EGFR) family. While monovalent wild-type ligands form HER hom ...
Olfaction, the detection of odorous chemicals in the environment, is one of the oldest mammalian sensory systems and involves large number (up to 1000) of distinct G protein coupled olfactory receptors (OR). The chemical interaction of volatile molecules w ...
Organometallic ruthenium(II) complexes of the general formula [Ru(η6-p-cymene)Cl2(L)] and [Ru(η6-p-cymene)Cl(L)2][BPh4] with modified phenoxazine- and anthracene-based multidrug resistanc ...
Bile acids (BAs), a group of structurally diverse molecules that are primarily synthesized in the liver from cholesterol, are the chief components of bile. Besides their well-established roles in dietary lipid absorption and cholesterol homeostasis, it has ...
The application describes ligands for binding targets, the ligands preferably including peptides having at least one sulfated or sulfonated amino acid. The ligand preferably specifically binds to heparin binding sites of biomolecules. Compositions, systems ...
NOVELTY - Conjugate (I) of an agonist ligand directed to ligand-gated ion channels (LGICs) of the Cys loop-family with a chromophore, is new. USE - (I) is useful in the receptor proteins and/or their interaction with the agonistic ligand, where the interac ...