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Stefan Gutwinski, Thorsten Kienast, Johannes Lindenmeyer, Martin Löb, Sabine Löber, Andreas Heinz: Alkoholabhängigkeit – Ein Leitfaden zur Gruppentherapie
2017
Swiss Archives of Neurology, Psychiatry and Psychotherapy
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Hyperphosphorylation induces structural modification of tau-protein
1998
FEBS Letters
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The effect of hyperphosphorylation on the structural properties and conformational stability of bovine tau-protein was studied by means of circular dichroism and fluorescence lifetime techniques. Normal protein contains unusual secondary structure elements: extended left-handed helices. The structure of this protein was assumed to be of a'tadpole' type^a globular Cterminal part with a long and rigid tail included in the extended left-handed helix. Either a decrease or an increase of pH induced
doi:10.1016/s0014-5793(98)01303-9
pmid:9849869
fatcat:7ncivqtxafeu7dpt73lc5v6t44
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... nly minor changes of the normal tau-protein surface. Hyperphosphorylation affected the extended part of the protein molecule; the decrease of pH in this case induced considerable structural rearrangements, and the conformation of the Cterminal part of the protein molecule was transformed into a molten globule-like state. z 1998 Federation of European Biochemical Societies.
Structure-based development of caged dopamine D2/D3 receptor antagonists
2020
Scientific Reports
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Dopamine is a neurotransmitter of great physiological relevance. Disorders in dopaminergic signal transduction are associated with psychiatric and neurological pathologies such as Parkinson's disease, schizophrenia and substance abuse. Therefore, a detailed understanding of dopaminergic neurotransmission may provide access to novel therapeutic strategies for the treatment of these diseases. Caged compounds with photoremovable groups represent molecular tools to investigate a biological target
doi:10.1038/s41598-020-57770-9
pmid:31965029
pmcid:PMC6972920
fatcat:wt4hfycucnbnnikzh4ft62772e
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... th high spatiotemporal resolution. Based on the crystal structure of the D3 receptor in complex with eticlopride, we have developed caged D2/D3 receptor ligands by rational design. We initially found that eticlopride, a widely used D2/D3 receptor antagonist, was photolabile and therefore is not suitable for caging. Subtle structural modification of the pharmacophore led us to the photostable antagonist dechloroeticlopride, which was chemically transformed into caged ligands. Among those, the 2-nitrobenzyl derivative 4 (MG307) showed excellent photochemical stability, pharmacological behavior and decaging properties when interacting with dopamine receptor-expressing cells.
Functional distinction of human EAG1 and EAG2 potassium channels
2002
FEBS Letters
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Human ether a © go-go potassium channel 2 (hEAG2) was cloned and its properties were compared with the previously characterized isoform hEAG1. In the Xenopus oocyte expression system the time course of activation was about four times slower and the voltage required for half-maximal subunit activation was about 10 mV greater for hEAG2 channels. However, its voltage dependence was smaller and, therefore, hEAG2 channels start to open at more negative voltages than hEAG1. Coexpression of both
doi:10.1016/s0014-5793(02)02365-7
pmid:11943152
fatcat:r7llxvv4a5frressbnnzg7iiue
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... ms and kinetic analysis of the resulting currents indicated that they can form heteromeric channel complexes in which the slow activation phenotype of hEAG2 is dominant. Upon expression in mammalian cells, quinidine blocked hEAG1 channels (IC 50 1.4 W WM) more potently than hEAG2 channels (IC 50 152 W WM), thus providing a useful tool for the functional distinction between hEAG1 and hEAG2 potassium channels. ß 2002 Published by Elsevier Science B.V. on behalf of the Federation of European Biochemical Societies.
Subtype Selective Tetracycline Agonists and their Application for a Two-Stage Regulatory System
2006
ChemBioChem
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General: All reactions were carried out in air unless otherwise indicated. Doxycycline hydrate, tetracycline hydrochloride and tetracycline hydrate for chemical synthesis were aquired from Heumann Pharma, Synopharm GmbH and Fluka, respectively. All chemicals were used as purchased. Doxycycline and anhydrotetrycycline for biological testing were purchased as hydrochlorides from Sigma and Acros Organics (Geel, Belgium), respectively. D-luciferin and coelenterazine were purchased from P.J.K.
doi:10.1002/cbic.200600226
pmid:16871602
fatcat:gnouaa5i2ndopkgtlr7pd5pt6e
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... blittersdorf, Germany). 1 H and 13 C NMR spectra were recorded at 300 K on a Bruker Avance 360 (360 MHz) or a Bruker Avance 600 (600 MHz). LC-MS analyses were performed with an Agilent 1100 HPLC combined with a Bruker Esquire 2000 mass spectrometer. HR-EIMS spectra were recorded on a Jeol GCmateII. Preparative HPLC was performed on an Agilent 1100 system using RP-18 colums (Agilent Zorbax 300SB, 7µm or CS-Chromatographie Eurospher C-18, 7µm) and CH 3 CN/ 0.1% aq. TFA or MeOH/0,1% aq. TFA as solvent systems. MPLC separation was performed on a Büchi Chromatography System (binary pump B-688, gradient former B-687 and glass columns B-685) with UV detection at 254 nm using Europrep 60-30 C18 (Eurochrom®, Knauer) RP silica gel and CH 3 CN / 0.1 % aq. TFA as a solvent system. In all cases HPLC grade solvents were used.
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy
2002
Bioorganic & Medicinal Chemistry Letters
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Based on the lead molecule FAUC 113, a series of di-and trisubstituted pyrazolo[1,5-a]pyridine derivatives was synthesized and investigated for their dopamine receptor binding profile. The carbonitrile 11a (FAUC 327) showed excellent pharmacological properties combining high D4 affinity (K i =1.5 nM) and selectivity with significant intrinsic activity (31%) in low nanomolar concentrations (EC 50 =1.5 nM). #
doi:10.1016/s0960-894x(01)00814-9
pmid:11844688
fatcat:jydpndwcjzhpxacpoikfchos64
Quinpramine Ameliorates Rat Experimental Autoimmune Neuritis and Redistributes MHC Class II Molecules
2011
PLoS ONE
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Activation of inflammatory cells is central to the pathogenesis of autoimmune demyelinating diseases of the peripheral nervous system. The novel chimeric compound quinpramine-generated from imipramine and quinacrine-redistributes cholesterol rich membrane domains to intracellular compartments. We studied the immunological and clinical effects of quinpramine in myelin homogenate induced Lewis rat experimental autoimmune neuritis (EAN), a model system for acute human inflammatory neuropathies,
doi:10.1371/journal.pone.0021223
pmid:21698177
pmcid:PMC3116892
fatcat:yd4asbiymfeorlsichyfi56rei
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... h as the Guillain-Barré syndrome. EAN animals develop paresis of all limbs due to autoimmune inflammation of peripheral nerves. Quinpramine treatment ameliorated clinical disease severity of EAN and infiltration of macrophages into peripheral nerves. It reduced expression of MHC class II molecules on antigen presenting cells and antigen specific T cell proliferation both in vitro and in vivo. Quinpramine exerted its anti-proliferatory effect on antigen presenting cells, but not on responder T cells. Our data suggest that quinpramine represents a candidate pharmaceutical for inflammatory neuropathies.
Syntheses and radiofluorination of two derivatives of 5-cyano-indole as selective ligands for the dopamine subtype-4 receptor
2006
Journal of labelled compounds & radiopharmaceuticals
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Two fluoroethoxy substituted derivatives, namely 2-[4-(2-(2-fluoroethoxy)phenyl)piperazin-l-ylmethyl]indole-5-carbonitrile (5a) and 2-[4-(4-(2-fluoroethoxy)-phenyl) piperazin-l-ylmethyl]indole-5-carbonitrile (5b) were synthesized as analogs of the selective D4 receptor ligand 2-[4-(4-fluorophenyl)piperazin-l-ylmethyl]indole-5-carbonitrile (FADC 316). In vitro characterization using CRO-cells expressing different dopamine receptor subtypes gave K; values of 2.1 (5a) and 9.9 nM (5b) for the
doi:10.1002/jlcr.1026
fatcat:6iig6xa4qnbvpj2aw725yytmry
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... ne D4 subtype and displayed a 420-fold D4-selectivity over D2 receptors for 5b. The para-fluoroethoxy substituted candidate 5b revealed substantially reduced (Xl and serotoninergic binding affinities in comparison to the ortho-fluoroethoxy substituted compound. In order to provide potential positron emission tomography (PET) imaging probes for the dopamine D4 receptor, 18F-labelling conditions using C 8 F]fluoroethyl tosylate were optimized and led to radiochemical yields of 81 ± 5% ([ 18 F]5a) and 47 ± 4% ([ 18 F]5b) (n = 3, decay-corrected and referred to labelling agent), respectively. Thus, 18F-fluoroethylation favourably at the para position of the phenylpiperazine moiety of the 5-cyano-indole framework proved to be tolerated by D4 receptors and could also be applied to alternative scaffolds in order to develop D4 radioligand candidates for PET with improved D4 receptor affinity and selectivity.
Conformational transitions provoked by organic solvents in β-lactoglobulin: can a molten globule like intermediate be induced by the decrease in dielectric constant?
1997
Folding & design
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It is known that nonnative states of protein molecules can exist in living cells and can be involved in a number of physiological processes. It has also been established that the membrane surface can be responsible for the partial denaturation of proteins due to negative charges on it. The local decrease in the effective dielectric constant of water near the organic surface has been suggested to be an additional driving force for protein denaturation in the membrane field, but data to confirm
doi:10.1016/s1359-0278(97)00023-0
pmid:9218954
fatcat:jo4wa7udardshafijevhtb3xt4
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... is suggestion were lacking. Results: Conformational transitions induced in -lactoglobulin by methanol, ethanol, isopropanol, dimethylformamide and dioxane were studied by near and far UV circular dichroism, steady-state tryptophan fluorescence and fluorescence decay of 8-anilinonaphthalene-1-sulfonate (8-ANS). The existence of at least two noncoinciding cooperative transitions has been established in all solvent systems studied. The first of these transitions describes the disruption of rigid tertiary structure in protein molecules, while the second reflects the formation of an expanded helical conformation typical of proteins in concentrated organic solvents. This means that the organic solvents provoke the formation of a denatured intermediate state with pronounced secondary structure and native-like compactness. We show that the positions of maxima in f I versus dielectric constant dependence virtually coincide for all five solvent systems studied. Conclusions: The decrease in the dielectric constant of the solvent induces in -lactoglobulin an equilibrium intermediate state. This state, being denatured, is relatively compact and has pronounced secondary structure and high affinity for the hydrophobic fluorescent probe 8-ANS, i.e. possesses all the properties of the molten globule intermediate state. Addresses:
sj-pdf-1-jop-10.1177_0269881120965908 – Supplemental material for Presynaptic vesicular accumulation is required for antipsychotic efficacy in psychotic-like rats
2020
Figshare
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Löber, Peter Gmeiner, Teja W Grömer and Christian P Müller in Journal of Psychopharmacology ...
in psychotic-like rats by Taygun C Uzuneser, Eva-Maria Weiss, Jana Dahlmanns, Liubov S Kalinichenko, Davide Amato, Johannes Kornhuber, Christian Alzheimer, Jan Hellmann, Jonas Kaindl, Harald Hübner, Stefan ...
doi:10.25384/sage.13337216.v1
fatcat:vjsapndrffbk7iqsxu7njbpufy
Exploring the SZE brightness of MUSIC proto-clusters to calibrate the Y-M scaling law
unpublished
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Page 994 of Economic Development and Cultural Change Vol. 51, Issue 4
[page]
2003
Economic Development and Cultural Change
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Lober, “International Ecotourism and the Valuation of Tropical Rainforests in Costa Rica,” Journal of Environmental Management 47 (1996): 1-10; Lisa C. Chase, David R. Lee, William D. ...
Stefan Géssling, “Ecotourism: A Means to Safeguard Biodiversity and Eco- system Functions,” Ecological Economics 29 (1999): 303-20; Sven Wunder, “Eco- tourism and Economic Incentives: An Empirical Approach ...
Estimating Stream Temperature from Air Temperature: Implications for Future Water Quality
2005
Journal of environmental engineering
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et al. 1998; Erickson and Stefan, 2000) . ...
The narrowest average CI's (2.7ºC, 2.9ºC) occurred at Lober River and Opatawicki River, sites with moderate NSC's (0.87,0.83, respectively). ...
doi:10.1061/(asce)0733-9372(2005)131:1(139)
fatcat:kmyveq24mzgqjbjfrclb52bdia
Neue Begriffe oder alte wissenssoziologische Perspektiven? Bericht vom Sommerworkshop des Arbeitskreises "Politik, Wissenschaft und Technik" der DVPW. Darmstadt, 15.–16. Juni 2010
2010
TATuP - Journal for Technology Assessment in Theory and Practice
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Stefan Böschen beleuchtete in seinem Beitrag die regulative Dimension des Verhältnisses von Politik und Wissenschaft am Beispiel der Ökologischen Chemie. ...
Dass Wissen auch eine Kategorie zur Analyse von Policy-Instrumenten sein könne, versuchte Sonja Löber in ihrem Vortrag am Beispiel der Umweltpolitik vorzustellen. ...
doi:10.14512/tatup.19.3.116
fatcat:qzqq3qd6avau3fhk5j2yczufam
Jensen mellem gengangere
2018
Passage
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Anmeldelse af Stefan Iversen: Den uhyggelige fortælling – unaturlig narratologi og Johannes V. Jensens tidlige forfatterskab. Aarhus: Aarhus Universitetsforlag 2018, 374 sider, 299 kr. ...
Men da han løber tør for analyseredskaber, henlaegges den. ...
doi:10.7146/pas.v33i80.111730
fatcat:ml2vkqgkbfg5hp5cyv6ix2snwm
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