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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...
Wiley-VCH Verlag
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Publication: Book Item (Buchkap., Lexikonartikel, jur. Kommentierung, Beiträge in Sammelbänden etc.)
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Year
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Abstract
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Affiliated organization
Stöckli, Andreas; Studer, M.; Cutting, Brian; Ernst, Beat
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)
In many fields, most notably medicine and molecular biology, the understanding of the structure and function of carbohydrates and glycoconjugates remains vital. This new volume contains critical reviews covering the latest findings in both chemical and biological sciences, and demonstrates the interdisciplinary nature of modern carbohydrate research. This book addresses diverse applications that...
The Royal Society of Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Publication: JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
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Year
Title
Abstract
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Affiliated organization
K. Lichtsteiner, Salome; Vögtli, Alexander; Weber, Christina; Burkhart, Helmar; Rizzotti, Sven; Folkers, Gerd; Khov-Tran, Van Van; Neier, Reinhard; Ernst, Beat
Departement Mathematik und Informatik / High Performance and Web Computing (Burkhart), Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Carbohydrates are the most abundant natural products. Besides their role in metabolism and as structural building blocks, they are fundamental constituents of every cell surface, where they are involved in vital cellular recognition processes. Carbohydrates are a relatively untapped source of new drugs and therefore offer exciting new therapeutic opportunities. Advances in the functional...
Nature Reviews. Drug Discovery
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Carbohydrates are ubiquitous and represent the most abundant class of molecules in nature. All cell surfaces are coated with complex carbohydrates where they act as recognition molecules for other cells, functional molecules, and pathogens. Consequently, they are involved in disease indications as diverse as inflammation, cancer, and infectious disease. In general, native carbohydrates lack the...
Discovery Medicine
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
The effect of metal ions on the activity, the donor substrate specificity, and the stability in organic solvents of Helicobacter pylori alpha-1,4 fucosyltransferase were studied. The recombinant enzyme was expressed as soluble form in E. coli strain AD494 and purified in a one step affinity chromatography. Its activity was highest in cacodylate buffer at pH 6.5 in the presence of 20 mM Mn(2+) ions...
Biometals
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Knecht, Steven; Ricklin, Daniel; Eberle, Alex N; Ernst, Beat
Since immobilized metal ion affinity chromatography (IMAC) was first reported, several modifications have been developed. Among them, Ni(2+) immobilized by chelation with nitrilotriacetic acid (NTA) bound to a solid support has become the most common method for the purification of proteins carrying either a C- or N-terminal histidine (His) tag. Despite its broad application in protein...
Journal of Molecular Recognition
Departement Biomedizin / Department of Biomedicine, University Hospital Basel, Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
The glucocorticoid receptor (GR) is a member of the nuclear receptor superfamily that affects immune response, development, and metabolism in target tissues. Glucocorticoids ore widely used to treat diverse pathophysiological conditions, but their clinical applicability is limited by side effects. A prediction of the binding affinity toward the GR would be beneficial for identifying...
ChemMedChem
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
We present a computational study on the human mineralocorticoid receptor (hMR) that is based on multidimensional quantitative structure-activity relationships (mQSAR). Therein, we identified the binding mode of 48 steroid and non-steroid homologues by flexible docking to the crystal structure (software Yeti) and quantified it using 6D-QSAR (software Quasar). The receptor surrogate, evolved using a...
Toxicology Letters
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Su, Z.; Wagner, Bea; Cocinero, E. J.; Ernst, Beat; Simons, J.
The tetrasaccharide 1, a substructure of ganglioside GQ1b alpha, shows a remarkable affinity for the myelin-associated glycoprotein (MAG) and was therefore selected as starting point for a lead optimization program. In our search for structurally simplified and pharmacokinetically improved mimics of 1, modifications of the core disaccharide, the alpha(2 -> 3)- and the alpha(2 -> 6)-linked sialic...
Journal of Medicinal Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
A series of novel aryl-substituted triazolyl D-galactosamine derivatives was synthesized as ligands for the carbohydrate recognition domain of the major subunit H1 (H1-CRD) of the human asialoglycoprotein receptor (ASGP-R). The compounds were biologically evaluated with a newly developed competitive binding assay, surface plasmon resonance and by a competitive NMR binding experiment. With compound...
Bioorganic & Medicinal Chemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Perchuc, A. M.; Menin, L.; Favreau, P.; Bühler, B.; Bulet, P.; Schöni, R.; Wilmer, M.; Ernst, Beat; Stöcklin, R.
Among the proteins and peptides already characterized in Bothrops moojeni venom, two novel phospholipases A(2) (PLA(2)) have been purified and fully sequenced by ESI-MS/MS techniques. Both of them belong to the enzymatically non-active Lys49 variants of PLA(2). They consist of 122 amino acids and share a characteristic sequence in their C-terminal region composed of clusters of basic amino acids...
Toxicon
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Chang, J.; Patton, J. T.; Sarkar, A.; Ernst, Beat; Magnani, J. L.; Frenette, P. S.
Leukocyte adhesion in the microvasculature influences blood rheology and plays a key role in vaso-occlusive manifestations of sickle cell disease. Notably, polymorphonuclear neutrophils (PMNs) can capture circulating sickle red blood cells (sRBCs) in inflamed venules, leading to critical reduction in blood flow and vasoocclusion. Recent studies have suggested that E-selectin expression by...
Blood
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Dutzler, R.; Ernst, Beat; Hediger, M. A.; Keppler, D.; Mohr, P.; Neidhart, W.; Märki, H. P.
The objective of the present study was an investigation of the crude Bothrops moojent venom, aiming at the identification of new compounds with platelet-activating or -inhibiting activity. The venom was separated by gel filtration chromatography into 18 fractions, which were tested by means of whole blood aggregometry for their activities affecting the aggregation of blood platelets. In order to...
Platelets
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Duthaler, R. O.; Ernst, B.; Fischer, R.; Katopodis, A. G.; Kinzy, W.; Marterer, W.; Oehrlein, R.; Streiff, M. B.; Thoma, G.
Pig-to-human xenotransplantation of islet cells or of vascularized organs would offer a welcome treatment alternative for the ever-increasing number of patients with end-stage organ failure who are waiting for a suitable allograph. The main hurdle are preexisting antibodies, most of which are specific for 'Linear-B', carbohydrate epitopes terminated by the unbranched Gal-alpha(1,3)Gal...
Chimia
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)
Uropathogenic Escherichia coli (UPEC) is the primary cause of urinary tract infections (UTIs). In the first step of this infective process, the virulence factor FimH located on type 1 pili allows UPEC to specifically adhere to oligosaccharides, which are part of glycoproteins on the urinary bladder mucosa. This initial step prevents the clearance of E. coli from the urinary tract and enables the...
Analytical Biochemistry
Departement Pharmazeutische Wissenschaften / Molekulare Pharmazie (Ernst)