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  1. Article ; Online: Preclinical Evaluation of the Reversible Monoacylglycerol Lipase PET Tracer (R)-[

    He, Yingfang / Delparente, Aro / Jie, Caitlin V M L / Keller, Claudia / Humm, Roland / Heer, Dominik / Collin, Ludovic / Schibli, Roger / Gobbi, Luca / Grether, Uwe / Mu, Linjing

    Chembiochem : a European journal of chemical biology

    2024  Volume 25, Issue 7, Page(s) e202300819

    Abstract: Monoacylglycerol lipase (MAGL) plays a crucial role in the degradation of 2-arachidonoylglycerol (2-AG), one of the major endocannabinoids in the brain. Inhibiting MAGL could lead to increased levels of 2-AG, which showed beneficial effects on pain ... ...

    Abstract Monoacylglycerol lipase (MAGL) plays a crucial role in the degradation of 2-arachidonoylglycerol (2-AG), one of the major endocannabinoids in the brain. Inhibiting MAGL could lead to increased levels of 2-AG, which showed beneficial effects on pain management, anxiety, inflammation, and neuroprotection. In the current study, we report the characterization of an enantiomerically pure (R)-[
    MeSH term(s) Rats ; Mice ; Animals ; Monoacylglycerol Lipases/metabolism ; Neurodegenerative Diseases/diagnostic imaging ; Neurodegenerative Diseases/drug therapy ; Positron-Emission Tomography/methods ; Inflammation ; Drug Development ; Enzyme Inhibitors/pharmacology
    Chemical Substances Monoacylglycerol Lipases (EC 3.1.1.23) ; Enzyme Inhibitors
    Language English
    Publishing date 2024-03-05
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2020469-3
    ISSN 1439-7633 ; 1439-4227
    ISSN (online) 1439-7633
    ISSN 1439-4227
    DOI 10.1002/cbic.202300819
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Journal: Holzheizkessel im Vergleich

    Humm, Roland

    Wohnung und Gesundheit : Fachzeitschrift fuer oekologisches Bauen und Leben

    1992  Volume 14, Page(s) 38–41

    Abstract: Der staendige CO2-Anstieg in unserer Atmosphaere und die daraus resultierenden zukuenftigen Naturkatastrophen sind uns in den Medien jeden Tag gegenwaertig. Die Loesungsmoeglichkeiten heissen Einschraenkung des Energieverbrauchs und Verwendung ... ...

    Abstract Der staendige CO2-Anstieg in unserer Atmosphaere und die daraus resultierenden zukuenftigen Naturkatastrophen sind uns in den Medien jeden Tag gegenwaertig. Die Loesungsmoeglichkeiten heissen Einschraenkung des Energieverbrauchs und Verwendung regenerativer Energiequellen. Dazu gehoert der Einsatz moderner Holz-Zentralheizkessel, mit denen eine wesentliche Reduzierung der Schadstoff-Emission erreicht wird. Aufgrund der tabellarischen Marktuebersicht kann sich der Interessent ein Bild ueber das derzeitige Angebot von Holz-Heizkesseln bezueglich Leistung, Wirkungsgrad, Abgaswerten, Preis etc. machen.
    Keywords Alternative Energie ; Kessel ; Heizung ; Kohlendioxid ; Schadstoffemission ; Reaktionstemperatur ; Verbrennung ; Verfahrenstechnik ; Verfahrensparameter ; Verfahrensvergleich ; Wirkungsgrad ; Abgaszusammensetzung ; Erneuerbare Ressourcen ; Marktuebersicht ; Energieverbrauch
    Language German
    Document type Journal
    Database OPAC and Environmental database (ULIDAT) of The Federal Environment Agency (UBA)

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  3. Article ; Online: Identification of potent and selective cathepsin S inhibitors containing different central cyclic scaffolds.

    Hilpert, Hans / Mauser, Harald / Humm, Roland / Anselm, Lilli / Kuehne, Holger / Hartmann, Guido / Gruener, Sabine / Banner, David W / Benz, Joerg / Gsell, Bernard / Kuglstatter, Andreas / Stihle, Martine / Thoma, Ralf / Sanchez, Rubén Alvarez / Iding, Hans / Wirz, Beat / Haap, Wolfgang

    Journal of medicinal chemistry

    2013  Volume 56, Issue 23, Page(s) 9789–9801

    Abstract: Starting from the weakly active dual CatS/K inhibitor 5, structure-based design supported by X-ray analysis led to the discovery of the potent and selective (>50,000-fold vs CatK) cyclopentane derivative 22 by exploiting specific ligand-receptor ... ...

    Abstract Starting from the weakly active dual CatS/K inhibitor 5, structure-based design supported by X-ray analysis led to the discovery of the potent and selective (>50,000-fold vs CatK) cyclopentane derivative 22 by exploiting specific ligand-receptor interactions in the S2 pocket of CatS. Changing the central cyclopentane scaffold to the analogous pyrrolidine derivative 57 decreased the enzyme as well as the cell-based activity significantly by 24- and 69-fold, respectively. The most promising scaffold identified was the readily accessible proline derivative (e.g., 79). This compound, with an appealing ligand efficiency (LE) of 0.47, included additional structural modifications binding in the S1 and S3 pockets of CatS, leading to favorable in vitro and in vivo properties. Compound 79 reduced IL-2 production in a transgenic DO10.11 mouse model of antigen presentation in a dose-dependent manner with an ED50 of 5 mg/kg.
    MeSH term(s) Animals ; Cathepsins/antagonists & inhibitors ; Cyclopentanes/chemistry ; Cysteine Proteinase Inhibitors/chemical synthesis ; Cysteine Proteinase Inhibitors/pharmacokinetics ; Humans ; Mice ; Proline/analogs & derivatives ; Structure-Activity Relationship
    Chemical Substances Cyclopentanes ; Cysteine Proteinase Inhibitors ; Proline (9DLQ4CIU6V) ; Cathepsins (EC 3.4.-) ; cathepsin S (EC 3.4.22.27)
    Language English
    Publishing date 2013-12-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm401528k
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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  4. Article: Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists.

    Kuhn, Bernd / Hilpert, Hans / Benz, Jörg / Binggeli, Alfred / Grether, Uwe / Humm, Roland / Märki, Hans Peter / Meyer, Markus / Mohr, Peter

    Bioorganic & medicinal chemistry letters

    2006  Volume 16, Issue 15, Page(s) 4016–4020

    Abstract: In the quest for novel PPARalpha/gamma co-agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we have used a structure-based design approach to identify propionic acids with a 1,5-disubstituted indole scaffold as potent ... ...

    Abstract In the quest for novel PPARalpha/gamma co-agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we have used a structure-based design approach to identify propionic acids with a 1,5-disubstituted indole scaffold as potent PPARalpha/gamma activators. Compounds 13, 24, and 28 are examples of submicromolar dual agonists with different alpha/gamma EC50 ratios that are selective against the delta-isoform. Analysis of the X-ray complex structure of PPARgamma with the indole propionic acid 13 provides a rationalization for some of the observed SAR.
    MeSH term(s) Drug Design ; Indoles/chemistry ; Indoles/pharmacology ; Molecular Structure ; PPAR alpha/agonists ; PPAR gamma/agonists ; Structure-Activity Relationship ; X-Ray Diffraction
    Chemical Substances Indoles ; PPAR alpha ; PPAR gamma ; indolepropionic acid (830-96-6)
    Language English
    Publishing date 2006-08-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2006.05.007
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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  5. Article ; Online: β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.

    Hilpert, Hans / Guba, Wolfgang / Woltering, Thomas J / Wostl, Wolfgang / Pinard, Emmanuel / Mauser, Harald / Mayweg, Alexander V / Rogers-Evans, Mark / Humm, Roland / Krummenacher, Daniela / Muser, Thorsten / Schnider, Christian / Jacobsen, Helmut / Ozmen, Laurence / Bergadano, Alessandra / Banner, David W / Hochstrasser, Remo / Kuglstatter, Andreas / David-Pierson, Pascale /
    Fischer, Holger / Polara, Alessandra / Narquizian, Robert

    Journal of medicinal chemistry

    2013  Volume 56, Issue 10, Page(s) 3980–3995

    Abstract: An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and highly brain ... ...

    Abstract An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and highly brain penetrant BACE1 inhibitor, was able to reduce significantly CSF Aβ40 and 42 in rats at oral doses as low as 1 mg/kg. The effect was long lasting, showing a significant reduction of Aβ40 and 42 even after 24 h. In contrast to 89, compound 1b lacking the CF3 group was virtually inactive in vivo.
    MeSH term(s) Alzheimer Disease/drug therapy ; Amyloid Precursor Protein Secretases/antagonists & inhibitors ; Animals ; Aspartic Acid Endopeptidases/antagonists & inhibitors ; Brain Chemistry ; Enzyme Inhibitors/pharmacokinetics ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Female ; Fluorine/chemistry ; Humans ; Indicators and Reagents ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Transgenic ; Models, Molecular ; Oxazines/chemical synthesis ; Oxazines/pharmacology ; Rats ; Rats, Wistar ; Structure-Activity Relationship ; X-Ray Diffraction
    Chemical Substances Enzyme Inhibitors ; Indicators and Reagents ; Oxazines ; Fluorine (284SYP0193) ; Amyloid Precursor Protein Secretases (EC 3.4.-) ; Aspartic Acid Endopeptidases (EC 3.4.23.-) ; Bace1 protein, mouse (EC 3.4.23.46)
    Language English
    Publishing date 2013-05-23
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm400225m
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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