A5077948100- Supramolecular Self-Assembly in Materials
- Alzheimer's disease research and treatments
- DNA and Nucleic Acid Chemistry
- Chemical Synthesis and Analysis
- Synthesis and Reactions of Organic Compounds
- Synthesis and Characterization of Heterocyclic Compounds
- Ferrocene Chemistry and Applications
- Graph theory and applications
- Prion Diseases and Protein Misfolding
- RNA Interference and Gene Delivery
- HIV/AIDS drug development and treatment
- Advanced biosensing and bioanalysis techniques
- Crystallography and molecular interactions
- Lanthanide and Transition Metal Complexes
- Carbohydrate Chemistry and Synthesis
- Synthesis and Biological Evaluation
- Organometallic Complex Synthesis and Catalysis
- Genetic Neurodegenerative Diseases
- Electron Spin Resonance Studies
- Genetics and Neurodevelopmental Disorders
- Fluorine in Organic Chemistry
- Porphyrin and Phthalocyanine Chemistry
- Supramolecular Chemistry and Complexes
- Biochemical and Molecular Research
- Fungal and yeast genetics research
Max Delbrück Center
2011-2020
Freie Universität Berlin
2004-2007
CeNTech
2004-2006
Osnabrück University
2001-2006
Universität Innsbruck
2005
Cobalt-alkyne complexes are drugs with remarkable cytotoxicity. From the tested up to now we selected aspirin derivative [2-acetoxy-(2-propynyl)benzoate]hexacarbonyldicobalt (Co-ASS) as lead compound. To get more insight into mode of action, systematically modified alkyne ligand and determined cytotoxic properties resulting cobalt complexes. Further investigations were performed on drug lipophilicity, cellular uptake MCF-7 MDA-MB 231 breast cancer cells, DNA-binding efficacy, nuclear...
Recent structural studies show distinct morphologies for the fibrils of Aβ(1-42) and Aβ(1-40), which are believed not to co-fibrillize. We describe here a novel, structurally-uniform 1 : mixed fibrillar species, differs from both pure fibrils. It forms preferentially even when Aβ(1-40) peptides in non-stoichiometric ratio.
A series of C5-substituted 1,2,4-triaryl-1H-imidazoles was synthesized. Their gene-activating properties were determined on estrogen receptor alpha positive MCF-7 breast cancer cells, stably transfected with the plasmid EREwtcluc (MCF-7-2a cells). The influence 4-OH and 2-Cl substituents phenyl rings as well significance a methyl, ethyl, or group at C5 binding resulting gene activation in MCF-7-2a cells studied. alkyl aryl groups 1,2,4-tris(4-hydroxyphenyl)-1H-imidazole 1 increased...
Chemical exchange saturation transfer (CEST) is an MRI technique that allows mapping of biomolecules (small metabolites, proteins) with nearly the sensitivity conventional water proton MRI. In living organisms, several tissue-specific CEST effects have been observed and successfully applied to diagnostic imaging. these studies, particularly signals proteins showed a distinct correlation pathological changes. However, as depend on various properties determine affect chemical processes,...
Alzheimer's disease (AD) is characterized by two neuropathological hallmarks: senile plaques, which are composed of amyloid-β (Aβ) peptides, and neurofibrillary tangles, hyperphosphorylated tau protein. Aβ peptides derived from sequential proteolytic cleavage the amyloid precursor protein (APP). In this study, we identified a so far unknown mode regulation APP synthesis involving MID1 complex: binds to regulates translation mRNA. The underlying action involves mTOR pathway. Thus, inhibition...
The 1H-imidazoles 7a−e were synthesized and tested for biological activity in vitro. results pointed to a clear structure−activity relationship. introduction of an ethyl chain at C5 the 1,2,4-tris(4-hydroxyphenyl)-1H-imidazole 7a caused hormonal estrogen receptor positive MCF-7-2a cells. An o-chlorine substituent phenolic rings C2 C4 as realized 7b 7c increased antiproliferative effects against human breast cancer cell lines MCF-7 MDA-MB 231. Additionally, both compounds showed strong...
Assemblies of huntingtin (HTT) fragments with expanded polyglutamine (polyQ) tracts are a pathological hallmark Huntington's disease (HD). The molecular mechanisms by which these structures formed and cause neuronal dysfunction toxicity poorly understood. Here, we utilized available gene expression data sets selected brain regions HD patients controls for systematic interaction network filtering in order to predict disease-relevant, region-specific HTT partners. Starting from large...
The aggregation of amyloid-β (Aβ) is postulated to be the crucial event in Alzheimer's disease (AD). In particular, small neurotoxic Aβ oligomers are considered responsible for development and progression AD. Therefore, elimination thesis represents a potential causal therapy Starting from well-characterized d-enantiomeric peptide D3, we identified D3 derivatives that bind monomeric Aβ. underlying hypothesis ligands stabilize these species within various equilibria with assemblies, leading...
The self-assembly of the 42-residue amyloid-β peptide, Aβ42, into fibrillar aggregates is associated with neuronal dysfunction and toxicity in Alzheimer's disease (AD) patient brains, suggesting that small molecules acting on this process might interfere pathogenesis. Here, we present experimental evidence molecule sclerotiorin (SCL), a natural product belonging to group azaphilones, potently delays both seeded nonseeded Aβ42 polymerization cell-free assays. Mechanistic biochemical studies...
Supramolecular tetrameric aggregates of four molecules 7-deaza-2′-deoxyxanthosine are stabilized by unconventional C−H⋅⋅⋅O hydrogen bonds. In the solid state tetramers stack to form a nanotube (see picture), in center which water found also stacked. Supporting information for this article is available on WWW under http://www.angewandte.com or from author. Please note: The publisher not responsible content functionality any supporting supplied authors. Any queries (other than missing content)...
The 9-deazaguanine N7-2′-deoxyribofuranoside (3) as well the bromo and iodo derivatives 4a,b were synthesized incorporated in oligonculeotide duplexes triplexes. Their base pairing properties investigated compared with those of parent purine N7-2′-deoxyribofuanosides.
Abstract Triplex‐forming oligonucleotides (TFOs) containing 9‐deazaguanine N 7 ‐(2′‐deoxyribonucleoside) 1a and halogenated derivatives 1b,c were synthesized employing solid‐phase oligonucleotide synthesis. For that purpose, the phosphoramidite building blocks 5a – c 8a synthesized. Multiple incorporations of in place dC performed within TFOs, which involved sequence five consecutive ⋅ dG triplets as well three alternating dT dA triplets. These TFOs designed to bind a parallel orientation...
Abstract The syntheses of N 7 ‐glycosylated 9‐deazaguanine 1a as well its 9‐bromo and 9‐iodo derivatives 1b , c are described. regioselective 9‐halogenation with ‐bromosuccinimide (NBS) ‐iodosuccinimide (NIS) was accomplished at the protected nucleobase 4a (2‐{[(dimethylamino)methylidene]amino}‐3,5‐dihydro‐3‐[(pivaloyloxy)methyl]‐4 H ‐pyrrolo[3,2‐ d ]pyrimidin‐4‐one). Nucleobase‐anion glycosylation – 2‐deoxy‐3,5‐di‐ O ‐( p ‐toluoyl)‐α‐ D ‐ erythro ‐pentofuranosyl chloride ( 5 ) furnished...
Supramolekulare tetramere Aggregate aus vier Molekülen 7-Desaza-2′-desoxyxanthosin werden durch unkonventionelle C-H⋅⋅⋅O-Wasserstoffbrücken stabilisiert. Im Kristall bilden sich Stapelung der Tetramere Nanoröhren (siehe Bild), in deren Innern – ebenfalls gestapelte H2O-Moleküle befinden.
The 7-bromo- (4a) and 7-iodo- (4b) derivatives of 7-deaza-2'-deoxyxanthosine (5) are prepared. Furthermore, the building blocks 6-8 synthesized tested for their usage in oligonucleotide synthesis.
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Supramolecular tetrameric aggregates of four molecules 7-deaza-2′-deoxyxanthosine are stabilized by unconventional C−H⋅⋅⋅O hydrogen bonds. In the solid state tetramers stack to form a nanotube (see picture), in center which water found also stacked.