Search results for publications (keywords "beat ernst"")

Showing records 1 - 20 (of 123) Next page Next page

Publication: Authored Book (Verfasser eines eigenständigen Buches)

Author  Year  Title  Abstract  Publisher  Affiliated organization 
Vögtli, Alexander; Ernst, Beat
2010
Im Rahmen einer biopharmazeutischen Synopse erläutert es mit den physikochemischen Eigenschaften verschiedener Arzneistoffmoleküle in Zusammenhang stehende Aspekte der Arzneimittelwirkung, die anderswo kaum auf diesem eingängigen und leicht verständlichen Niveau beschrieben sind. Die Autoren verstehen es zu abstrahieren und den Leser durch eine Vielzahl konkreter Beispiele bei Laune zu halten, was...
Wiley-VCH Verlag
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)

Publication: Book Item (Buchkap., Lexikonartikel, jur. Kommentierung, Beiträge in Sammelbänden etc.)

Author  Year  Title  Abstract  Publisher  Affiliated organization 
Pang, Lijuan; Bezençon, Jacqueline; Kleeb, Simon; Rabbani, Said; Sigl, Anja; Smiesko, Martin; Sager, Christoph P.; Eris, Deniz; Schwardt, Oliver; Ernst, Beat
2017
Urinary tract infections (UTIs) caused by uropathogenic Escherichia coli (UPEC) are among the most prevalent infections worldwide. Since frequent antibiotic treatment favors the emergence of antibiotic resistance, efficient non-antibiotic strategies are urgently needed. The first step of the pathogenesis of UTI is the bacterial adherence to urothelial host cells, a process mediated by the...
Royal Society of Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Stöckli, Andreas; Studer, M.; Cutting, Brian; Ernst, Beat
2009
Wiley-Blackwell
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)

Publication: JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)

Author  Year  Title  Abstract  Publisher  Affiliated organization 
Ernst, Beat; Zihlmann, Pascal; Slbermann, Marleen; Sharpe, Timothy; Jiang, Xiaohua; Mühlethaler, Tobias; Jakob, Roman P; Rabbani, Said; Sager, Christoph P; Frei, Priska; Maier, Timm
2018
Affinity data, such as dissociation constants (KD) or inhibitory concentrations (IC50), are widely used in drug discovery. However, these parameters describe an equilibrium state, which is often not established in vivo due to pharmacokinetic effects and they are therefore not necessarily sufficient for evaluating drug efficacy. More accurate indicators for pharmacological activity are the kinetics...
Chemistry (Weinheim an der Bergstrasse, Germany)
Departement Biozentrum / Structural Biology (Maier), Departement Biozentrum / Biophysics Facility (Sharpe)
Rabbani, Said; Fiege, Brigitte; Eris, Deniz; Silbermann, Marleen; Jakob, Roman Peter; Navarra, Giulio; Maier, Timm; Ernst, Beat
2018
For many biological processes such as ligand binding, enzymatic catalysis, or protein folding, allosteric regulation of protein conformation and dynamics is fundamentally important. One example is the bacterial adhesin FimH, where the C-terminal pilin domain exerts negative allosteric control over binding of the N-terminal lectin domain to mannosylated ligands on host cells. When the lectin and...
Journal of Biological Chemistry
Departement Biozentrum / Structural Biology (Maier), Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Sager, Christoph P.; Fiege, Brigitte; Zihlmann, Pascal; Vannam, Raghu; Rabbani, Said; Jakob, Roman P.; Preston, Roland C.; Zalewski, Adam; Maier, Timm; Peczuh, Mark W.; Ernst, Beat
2018
Seven-membered ring mimetics of mannose were studied as ligands for the mannose-specific bacterial lectin FimH, which plays an essential role in the first step of urinary tract infections (UTI). A competitive binding assay and isothermal titration calorimetry (ITC) experiments indicated an approximately ten-fold lower affinity for the seven-membered ring mannose mimetic...
Chemical Science
Departement Biozentrum / Structural Biology (Maier)
Aeschbacher, Thomas; Zierke, Mirko; Smieško, Martin; Collot, Mayeul; Mallet, Jean-Maurice; Ernst, Beat; Allain, Frédéric H.-T.; Schubert, Mario
2017
The increasing understanding of the essential role of carbohydrates in development, and in a wide range of diseases fuels a rapidly growing interest in the basic principles governing carbohydrate-protein interactions. A still heavily debated issue regarding the recognition process is the degree of flexibility or rigidity of oligosaccharides. Combining NMR structure determination based on extensive...
Chemistry - A European Journal
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Frei, Priska; Pang, Lijuan; Silbermann, Marleen; Eriş, Deniz; Mühlethaler, Tobias; Schwardt, Oliver; Ernst, Beat
2017
Target-directed dynamic combinatorial chemistry (DCC) is an emerging technique for the efficient identification of inhibitors of pharmacologically relevant targets. In this contribution, we present an application for a bacterial target, the lectin FimH, a crucial virulence factor of uropathogenic E. coli being the main cause of urinary tract infections. A small dynamic library of acylhydrazones...
Chemistry - A European Journal
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Herrendorff, Ruben; Hänggi, Pascal; Pfister, Hélène; Yang, Fan; Demeestere, Delphine; Hunziker, Fabienne; Frey, Samuel; Schaeren-Wiemers, Nicole; Steck, Andreas J.; Ernst, Beat
2017
Anti-MAG (myelin-associated glycoprotein) neuropathy is a disabling autoimmune peripheral neuropathy caused by monoclonal IgM autoantibodies that recognize the carbohydrate epitope HNK-1 (human natural killer-1). This glycoepitope is highly expressed on adhesion molecules, such as MAG, present in myelinated nerve fibers. Because the pathogenicity and demyelinating properties of anti-MAG...
Proceedings of the National Academy of Sciences
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Mayer, Katharina; Eris, Deniz; Schwardt, Oliver; Sager, Christoph P.; Rabbani, Said; Kleeb, Simon; Ernst, Beat
2017
Frequent antibiotic treatment of urinary tract infections has resulted in the emergence of antimicrobial resistance, necessitating alternative treatment options. One such approach centers around FimH antagonists that block the bacterial adhesin FimH, which would otherwise mediate binding of uropathogenic Escherichia coli to the host urothelium to trigger the infection. Although the FimH lectin can...
Journal of Medicinal Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Navarra, Giulio; Zihlmann, Pascal; Jakob, Roman P.; Stangier, Katia; Preston, Roland C.; Rabbani, Said; Smiesko, Martin; Wagner, Bea; Maier, Timm; Ernst, Beat
2017
Uropathogenic E. coli exploit the PapG-II adhesin for infecting host cells of the kidney; moreover, the expression of PapG-II located at the tip of bacterial pili has been correlated with the onset of pyelonephritis in humans, a potentially life-threatening condition. It was envisaged that the blocking of PapG-II, and thus bacterial adhesion, embodies a viable therapeutic alternative to...
ChemBioChem
Departement Biozentrum / Structural Biology (Maier), Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Rabbani, Said; Krammer, Eva-Maria; Goedele, Roos; Zalewski, Adam; Preston, Roland; Eid, Sameh; Zihlmann, Pascal; Prévost, Martine; Lensink, Marc F.; Thompson, Andrew; Ernst, Beat; Bouckaert, Julie
2017
The most prevalent diseases manifested by Escherichia coli are acute and recurrent bladder infections and chronic inflammatory bowel diseases such as Crohn's disease. E. coli clinical isolates express the FimH adhesin, which consists of a mannose-specific lectin domain connected via a pilin domain to the tip of type 1 pili. Although the isolated FimH lectin domain has affinities in the nanomolar...
IU Cr J
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Sager, Christoph P.; Eriş, Deniz; Smieško, Martin; Hevey, Rachel; Ernst, Beat
2017
In general, carbohydrate-lectin interactions are characterized by high specificity but also low affinity. The main reason for the low affinities are desolvation costs, due to the numerous hydroxy groups present on the ligand, together with the typically polar surface of the binding sites. Nonetheless, nature has evolved strategies to overcome this hurdle, most prominently in relation to...
Beilstein Journal of Organic Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Schönemann, Wojciech; Lindegger, Marcel; Rabbani, Said; Zihlmann, Pascal
2017
Urinary tract infections (UTIs), which are among the most prevalent bacterial infections worldwide, are mainly attributed to uropathogenic Escherichia coli (UPEC). Because of frequent antibiotic treatment, antimicrobial resistance constitutes an increasing therapeutic problem. Antagonists of the mannose-specific bacterial lectin FimH, a key protein mediating the adhesion of UPEC to human bladder...
Perspectives in Science
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Eris, Deniz; Preston, Roland C.; Scharenberg, Meike; Hulliger, Fabian; Abgottspon, Daniela; Pang, Lijuan; Jiang, Xiaohua; Schwardt, Oliver; Ernst, Beat
2016
FimH is a bacterial lectin found at the tips of type 1 pili of uropathogenic Escherichia coli (UPEC). It mediates shear-enhanced adhesion to mannosylated surfaces. Binding of UPEC to urothelial cells initiates the infection cycle leading to urinary tract infections (UTIs). Antiadhesive glycomimetics based on α-d-mannopyranose offer an attractive alternative to the conventional...
ChemBioChem
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Kleeb, Simon; Jiang, Xiaohua; Frei, Priska; Sigl, Anja; Bezençon, Jacqueline; Bamberger, Karen; Schwardt, Oliver; Ernst, Beat
2016
The widespread occurrence of urinary tract infections has resulted in frequent antibiotic treatment, contributing to the emergence of antimicrobial resistance. Alternative approaches are therefore required. In the initial step of colonization, FimH, a lectin located at the tip of bacterial type 1 pili, interacts with mannosylated glycoproteins on the urothelial mucosa. This initial pathogen/host...
Journal of Medicinal Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Preston, Roland C.; Jakob, Roman P.; Binder, Florian P. C.; Sager, Christoph P.; Ernst, Beat; Maier, Timm
2016
E-selectin is a cell-adhesion molecule of the vascular endothelium that promotes essential leukocyte rolling in the early inflammatory response by binding to glycoproteins containing the tetrasaccharide sialyl Lewis(x) (sLe(x)). Efficient leukocyte recruitment under vascular flow conditions depends on an increased lifetime of E-selectin/ligand complexes under tensile force in a so-called...
Journal of Molecular Cell Biology
Departement Biozentrum / Structural Biology (Maier)
Pröpster, Johannes M.; Yang, Fan; Rabbani, Said; Ernst, Beat; Allain, Frédéric H.-T.; Schubert, Mario
2016
Siglec-8 is a human immune-inhibitory receptor that, when engaged by specific self-glycans, triggers eosinophil apoptosis and inhibits mast cell degranulation, providing an endogenous mechanism to down-regulate immune responses of these central inflammatory effector cells. Here we used solution NMR spectroscopy to dissect the fine specificity of Siglec-8 toward different sialylated and sulfated...
Proceedings of the National Academy of Sciences of the United States of America
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Sauer, Maximilian M; Jakob, Roman P; Eras, Jonathan; Baday, Sefer; Eriş, Deniz; Navarra, Giulio; Bernèche, Simon; Ernst, Beat; Maier, Timm; Glockshuber, Rudi
2016
Ligand-receptor interactions that are reinforced by mechanical stress, so-called catch-bonds, play a major role in cell-cell adhesion. They critically contribute to widespread urinary tract infections by pathogenic Escherichia coli strains. These pathogens attach to host epithelia via the adhesin FimH, a two-domain protein at the tip of type I pili recognizing terminal mannoses on epithelial...
Nature communications
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst), Departement Biozentrum / Structural Biology (Maier)
Schönemann, Wojciech; Kleeb, Simon; Dätwyler, Philipp; Schwardt, Oliver; Ernst, Beat
2016
The bacterial lectin FimH is a promising therapeutic target for the nonantibiotic prevention and treatment of urinary tract infections. In this communication, an ester prodrug approach is described to achieve oral bioavailability for FimH antagonists. By introducing short-chain acyl promoieties at the C-6 position of a biphenyl α- d -mannopyranoside, prodrugs with an excellent absorption...
Canadian Journal of Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
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17/07/2018