A5047988722- Cholinesterase and Neurodegenerative Diseases
- Computational Drug Discovery Methods
- RNA Interference and Gene Delivery
- Photoreceptor and optogenetics research
- Natural Antidiabetic Agents Studies
- Nicotinic Acetylcholine Receptors Study
- Photochromic and Fluorescence Chemistry
- Medicinal Plants and Neuroprotection
- Cannabis and Cannabinoid Research
- Alzheimer's disease research and treatments
- Immune cells in cancer
- Nanoplatforms for cancer theranostics
- Chemical Synthesis and Analysis
- Chemokine receptors and signaling
- Dendrimers and Hyperbranched Polymers
- Neuroscience and Neuropharmacology Research
University of Würzburg
2020-2024
Technical University of Munich
2017
Max Planck Computing and Data Facility
2017
We present the synthesis and characterization of merged human butyrylcholinesterase (hBChE) inhibitor/cannabinoid receptor 2 (hCB2R) ligands for treatment neurodegeneration. In total, 15 benzimidazole carbamates were synthesized tested their inhibition cholinesterases, also with regard to pseudoirreversible binding mode affinity toward both cannabinoid receptors in radioligand studies. After evaluation a calcium mobilization assay as well β-arrestin (βarr2) recruitment assay, two compounds...
Abstract Flavonoids are polyphenolic natural products and have shown significant potential as disease‐modifying agents against neurodegenerative disorders like Alzheimer's disease (AD), with activities even in vivo. Hybridization of the taxifolin silibinin cinnamic acid led to an overadditive effect these compounds several phenotypic screening assays related neurodegeneration AD. Therefore, we exchanged flavonoid part hybrids different flavonoids, which show higher efficacy than or...
Benzimidazole-based inhibitors of butyrylcholinesterase were designed and tested for their activity selectivity in vitro , leading to compound (11d) that attenuated Aβ 25-35 -induced learning impairments an Alzheimer's disease mouse model.
The interleukin-8 receptor beta (CXCR2) is a highly promising target for molecular imaging of inflammation and inflammatory diseases. This due to its almost exclusive expression on neutrophils. Modified fluorinated ligands were designed based squaramide template, with different modification sites synthetic strategies explored. Promising candidates then tested affinity CXCR2 in NanoBRET competition assay, resulting tracer candidate
Starting from multifunctional triazacyclononane-triphosphinate chelator cores, dendritic molecules with the ability to bind metal ions within their framework were synthesized. A cooperative interaction of cages resulted in a markedly increased affinity towards 67/68GaIII. hexameric PSMA inhibitor conjugate high (IC50 = 1.2 nM) and favorable vivo PET imaging properties demonstrated practical applicability. The novel scaffolds are useful for synthesis structurally well-defined multimodal...
Abstract Considerable effort has previously been invested in a light‐controlled inhibition of the enzyme acetylcholinesterase (AChE). We found that novel azobenzene‐based bistacrine AChE inhibitor switched faster than known dithienylethene based and inverted photo‐controlled interactions photoisomers compared to its congener. Furthermore, we have optimized described tacrine‐based inhibitor. Isomerization upon irradiation with UV light was observed aqueous medium showed no fatigue over...
Abstract Purpose A neuropathological hallmark of Alzheimer’s disease (AD) is the presence amyloid-β (Aβ) plaques in brain, which are observed a significant number cognitively normal, older adults as well. In AD, butyrylcholinesterase (BChE) becomes associated with β aggregates, making it promising target for imaging probes to support diagnosis AD. this study, we present synthesis, radiochemistry, vitro and preliminary ex vivo investigations selective, reversible BChE inhibitor PET-tracer...