A5070830358- Biochemical Analysis and Sensing Techniques
- Olfactory and Sensory Function Studies
- Advanced Chemical Sensor Technologies
- RNA and protein synthesis mechanisms
- Wnt/β-catenin signaling in development and cancer
- Neurobiology and Insect Physiology Research
- Cancer-related gene regulation
- Analytical Chemistry and Chromatography
- Inflammatory mediators and NSAID effects
- Bacterial Genetics and Biotechnology
- Pharmacogenetics and Drug Metabolism
- Asthma and respiratory diseases
- Eicosanoids and Hypertension Pharmacology
- Immunotherapy and Immune Responses
- Phytochemistry and Bioactive Compounds
- Cytokine Signaling Pathways and Interactions
- Receptor Mechanisms and Signaling
- Protein purification and stability
- RNA regulation and disease
- DNA and Nucleic Acid Chemistry
- Marine Sponges and Natural Products
- Sirtuins and Resveratrol in Medicine
- Dermatology and Skin Diseases
- CRISPR and Genetic Engineering
- Creativity in Education and Neuroscience
Brain (Germany)
2005-2021
University of Wuppertal
2017-2020
Leibniz-Institut für Naturstoff-Forschung und Infektionsbiologie e. V. - Hans-Knöll-Institut (HKI)
2005
Max Planck Institute of Immunobiology and Epigenetics
1997
Heinrich Heine University Düsseldorf
1992-1996
From Penicillium janczewskii, obtained from a marine sample, two new diastereomeric quinolinones, 3S*,4R*-dihydroxy-4-(4'-methoxyphenyl)-3,4-dihydro-2(1H)-quinolinone (1) and 3R*,4R*-dihydroxy-4-(4'-methoxyphenyl)-3,4-dihydro-2(1H)-quinolinone (2), were identified, along with known alkaloids, peniprequinolone (3) 3-methoxy-4-hydroxy-4-(4'-methoxyphenyl)-3,4-dihydro-2(1H)-quinolinone (4). Cytotoxicity testing on eight tumor cell lines revealed moderate specificity of 2 SKOV-3 cells.
Please cite this paper as: Inhibition of TRPV1 for the treatment sensitive skin. Experimental Dermatology 2010; 19 : 980–986. Abstract: During past years, topic skin became one most important fields in dermatology. The tremendous interest is based on several studies showing that about 50% population declares to have human thermoreceptor hTRPV1 was previously identified contribute condition while facilitating neurogenic inflammation leading hyperalgesia. Furthermore, sensitivity towards...
Both in-house human genetic and literature data have converged on the identification of leukotriene 4 hydrolase (LTA4H) as a key target for treatment cardiovascular disease. We combined fragment-based crystallography screening with an iterative medicinal chemistry effort to optimize inhibitors LTA4H. Ligand efficiency was followed throughout our structure−activity studies. As applied within context LTA4H inhibitor design, team able design potent compound 20 (DG-051) (Kd = 26 nM) high aqueous...
The E-cadherin-catenin adhesion complex has been the subject of many structural and functional studies because its importance in development, normal tissue function carcinogenesis. It is well established that cytoplasmic domain E-cadherin binds either beta-catenin or plakoglobin, which both can assemble alpha-catenin into complex. Recently we have identified an binding site plakoglobin postulated, based on sequence analysis, these protein-protein interactions are mediated by a hydrophobic...
Brazzein is a small sweet-tasting protein found in the red berries of West African evergreen shrub, Pentadiplandra brazzeana Baillon. highly soluble and stable over large pH range at high temperatures, which are characteristics that suggest its use as natural sweetener. However, culture difficult scale, limiting source brazzein. Heterologous expression brazzein has been established numerous systems, including bacteria, yeast, transgenic plants. requires four disulfide bonds to be active...
Investigating molecular mechanisms underlying human taste sensation requires functionally dedicated and at the same time proliferating cells. Here, we isolated viable fungiform papillae cells from biopsy samples, adenovirally transduced proliferation promoting genes, obtained stably cell lines. Analysis of gene expression 1 line termed HTC-8 revealed that these express 13 TAS2R bitter receptor CD36, OXTR encoding oxytocin receptor, as well genes implicated with signal transduction fate...
We have studied the response of effector molecule guanosine 3′,5′-bisdiphosphate (ppGpp) on RNA polymerase pausing during in vitro transcription elongation. Pausing was followed single round extension stalled ternary complexes excluding possible ppGpp effects initiation. The dependences early sites within different systems controlled by promoters with known to enhanced levels vivo were quantitatively characterized. Transcription stable RNAs and mRNA genes analyzed. In addition, behavior two...
Sweating is an important physiological process to regulate body temperature in humans, and various disorders are associated with dysregulated sweat formation. Primary secretion human eccrine glands involves Ca(2+) -activated Cl(-) channels (CaCC). Recently, members of the TMEM16 family were identified as CaCCs secretory epithelia; however, their molecular identity remained elusive. Here, we investigated function TMEM16A glands. Gene expression analysis revealed that expressed NCL-SG3 gland...
The products of the cytochrome P450 monooxygenase (CYP)-catalyzed oxidation arachidonic acid (AA), that is, epoxy- and hydroxy-fatty acids, play a crucial role in homeostasis several physiological processes. In liver microsome-based multienzyme assay using AA as natural substrate, we investigated how polyphenols inhibit different oxylipin-forming CYP parallel but independently from each other. ω-hydroxylating CYP4F2 CYP4A11 were investigated, well epoxidizing CYP2C-subfamily CYP3A4 along...
DG-051B is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention heart attack. Process optimization led from linear seven-step synthetic procedure to convergent four-step manufacturing sequence that has been used manufacture at 100-kg scale. The entire process can be telescoped due high conversion reactions, low impurity levels, efficient separations, and very effective final purification. Two key aspects...
Although resveratrol exerts manifold antitumorigenic effects in vitro, its efficacy against malignancies vivo seems limited. This has been increasingly recognized recent years and prompted scientists to search for structurally related compounds with more promising anticarcinogenic and/or pharmacokinetic properties. A class of modified derivatives, so-called imine analogs (IRA's), might meet these requirements. Therefore, the biological activity five was examined compared that resveratrol....
Summary Transcription elongation catalysed by DNA‐dependent RNA polymerase does not occur at a constant rate. Instead, during the transcription of many genes pausing occurs defined template positions. Pausing is known to be influenced intracellular NTP concentration, secondary structure growing transcript or factors like NusA. We have investigated effects topology transcriptional pauses in presence and absence on purified NusA protein. Taking advantage method for quantifying we studied...
Abstract Bei der Untersuchung Rückstände auf Scherben eines bei Ausgrabungen in Ägypten gefundenen Kruges, wahrscheinlich aus dem 6. Jh. v. Chr. stammt, wurden noch intakte langkettige, gesättigte n‐, iso‐ und anteiso‐Fettsäuren sowie Wachsester gefunden. Daneben fanden sich den Relikten Oxidationsprodukte ungesättigten Fettsäuren von Terpenen. Die Ergebnisse nach chromatographischer Vortrennung durch GC‐MS‐Kopplung ausgeführten Analysen lassen das ursprüngliche Vorliegen Gemisches...