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Species-dependent activities of G-protein-coupled receptor ligands: lessons from histamine receptor orthologs.
Histamine is a biogenic amine that exerts its biological effects as a neurotransmitter and local mediator via four histamine receptor (HR) subtypes (H(x)Rs) - H(1)R, H(2)R, H(3)R, and H(4)R -Expand
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Modulation of GPCRs by monovalent cations and anions
The recent resolution of G-protein-coupled receptor (GPCR) structures in complex with Na+ bound to an allosteric modulatory site has renewed interest of the regulation of GPCRs by ions. Here, weExpand
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Synthesis, biological evaluation, and computational studies of Tri- and tetracyclic nitrogen-bridgehead compounds as potent dual-acting AChE inhibitors and hH3 receptor antagonists.
Combination of AChE inhibiting and histamine H3 receptor antagonizing properties in a single molecule might show synergistic effects to improve cognitive deficits in Alzheimer's disease, since bothExpand
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Ligand-Specific Contribution of the N Terminus and E2-Loop to Pharmacological Properties of the Histamine H1-Receptor
There are species differences between human histamine H1 receptor (hH1R) and guinea pig (gp) histamine H1 receptor (gpH1R) for phenylhistamines and histaprodifens. Several studies showedExpand
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  • Open Access
Molecular Basis for the Selective Interaction of Synthetic Agonists with the Human Histamine H1-Receptor Compared with the Guinea Pig H1-Receptor
Previous studies revealed that phenylhistamines and histaprodifens possess higher potency and affinity at guinea pig histamine H1-receptor (gpH1R) than at human histamine H1-receptor (hH1R). However,Expand
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  • Open Access
New insights into the cross-linking and degradation mechanism of Diels-Alder hydrogels.
Eight-armed poly(ethylene glycol) was functionalized with furyl and maleimide groups. The two macromonomers were cross-linked by Diels-Alder (DA) reactions and the degradation behavior of the formedExpand
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  • Open Access
Structure-Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands
The enzyme butyrylcholinesterase (BChE) and the human cannabinoid receptor 2 (hCB2R) represent promising targets for pharmacotherapy in the later stages of Alzheimer's disease. We mergedExpand
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Influence of the N-terminus and the E2-loop onto the binding kinetics of the antagonist mepyramine and the partial agonist phenoprodifen to H(1)R.
Numerous competitive radioligand binding studies revealed significant differences between human and guinea pig histamine H(1)-receptors (hH(1)R and gpH(1)R), e.g. for the partial H(1)R agonistExpand
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Nanofibers resulting from cooperative electrostatic and hydrophobic interactions between peptides and polyelectrolytes of opposite charge.
We investigated whether cationic peptides that contain hydrophobic side chains were able to stabilize themselves via hydrophobic interactions between neighboring peptide molecules upon electrostaticExpand
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Competitive association binding kinetic assays: a new tool to detect two different binding orientations of a ligand to its target protein under distinct conditions?
Within the last years, for several ligands, binding to G protein-coupled receptors or other target proteins, a binding of the ligand in two different orientations is described. One appropriateExpand
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