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  1. Article: Design, Synthesis, and Biological Evaluation of 4,4'-Difluorobenzhydrol Carbamates as Selective M

    Kilian, Jonas / Ozenil, Marius / Millard, Marlon / Fürtös, Dorka / Maisetschläger, Verena / Holzer, Wolfgang / Wadsak, Wolfgang / Hacker, Marcus / Langer, Thierry / Pichler, Verena

    Pharmaceuticals (Basel, Switzerland)

    2022  Volume 15, Issue 2

    Abstract: Due to their important role in mediating a broad range of physiological functions, muscarinic acetylcholine receptors (mAChRs) have been a promising target for therapeutic and diagnostic applications alike; however, the list of truly subtype-selective ... ...

    Abstract Due to their important role in mediating a broad range of physiological functions, muscarinic acetylcholine receptors (mAChRs) have been a promising target for therapeutic and diagnostic applications alike; however, the list of truly subtype-selective ligands is scarce. Within this work, we have identified a series of twelve 4,4'-difluorobenzhydrol carbamates through a rigorous docking campaign leveraging commercially available amine databases. After synthesis, these compounds have been evaluated for their physico-chemical property profiles, including characteristics such as HPLC-logD, tPSA, logBB, and logPS. For all the synthesized carbamates, these characteristics indicate the potential for BBB permeation. In competitive radioligand binding experiments using Chinese hamster ovary cell membranes expressing the individual human mAChR subtype
    Language English
    Publishing date 2022-02-18
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph15020248
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  2. Book ; Online ; Thesis: Effects of the fungicide mixture mancozeb, metalaxyl-M, and chlorothalonil on the degradation of $^14}C-MCPA$ in soil

    Nguyen, Kim Thu [Verfasser] / Schäffer, Andreas [Akademischer Betreuer] / Dongen, Joost T. van [Akademischer Betreuer] / Smith, Kilian [Akademischer Betreuer]

    2023  

    Author's details Kim Thu Nguyen ; Andreas Schäffer, Joost Thomas van Dongen, Kilian Smith
    Keywords Landwirtschaft, Veterinärmedizin ; Agriculture, Veterinary Science
    Subject code sg630
    Language English
    Publisher Universitätsbibliothek der RWTH Aachen
    Publishing place Aachen
    Document type Book ; Online ; Thesis
    Database Digital theses on the web

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  3. Article: Rechsprechung. MVZ-Gründungsberechtigung eines von ausländischen Finanzinvestoren beherrschten Krankenhausträgers? (SG Dresden, Beschl. v. 9.5.2022 - S 25 KA 20/22 ER [Ls.]) m. Anm. Kilian Friedrich

    Kilian, Friedrich

    Gesundheitsrecht

    2022  Volume 21, Issue 11, Page(s) 725

    Language German
    Document type Article
    ZDB-ID 2092255-3
    ISSN 1610-1197
    Database Current Contents Medicine

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    In stock of ZB MED Cologne/Königswinter

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  4. Article ; Online: Design, Synthesis, and Biological Evaluation of 4,4’-Difluorobenzhydrol Carbamates as Selective M 1 Antagonists

    Jonas Kilian / Marius Ozenil / Marlon Millard / Dorka Fürtös / Verena Maisetschläger / Wolfgang Holzer / Wolfgang Wadsak / Marcus Hacker / Thierry Langer / Verena Pichler

    Pharmaceuticals, Vol 15, Iss 248, p

    2022  Volume 248

    Abstract: ... mAChR subtype h M 1 - h M 5 , the most promising compound 2 displayed a high binding affinitiy towards h ... M 1 R (1.2 nM) while exhibiting modest-to-excellent selectivity versus the h M 2-5 R (4–189-fold ...

    Abstract Due to their important role in mediating a broad range of physiological functions, muscarinic acetylcholine receptors (mAChRs) have been a promising target for therapeutic and diagnostic applications alike; however, the list of truly subtype-selective ligands is scarce. Within this work, we have identified a series of twelve 4,4’-difluorobenzhydrol carbamates through a rigorous docking campaign leveraging commercially available amine databases. After synthesis, these compounds have been evaluated for their physico–chemical property profiles, including characteristics such as HPLC-logD, tPSA, logBB, and logPS. For all the synthesized carbamates, these characteristics indicate the potential for BBB permeation. In competitive radioligand binding experiments using Chinese hamster ovary cell membranes expressing the individual human mAChR subtype h M 1 - h M 5 , the most promising compound 2 displayed a high binding affinitiy towards h M 1 R (1.2 nM) while exhibiting modest-to-excellent selectivity versus the h M 2-5 R (4–189-fold). All 12 compounds were shown to act in an antagonistic fashion towards h M1R using a dose-dependent calcium mobilization assay. The structural eligibility for radiolabeling and their pharmacological and physico–chemical property profiles render compounds 2, 5, and 7 promising candidates for future position emission tomography (PET) tracer development.
    Keywords muscarinic acetylcholine receptors ; subtype selectivity ; drug development ; molecular docking ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Subject code 540
    Language English
    Publishing date 2022-02-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article: The kinetics and regulation of M-xylose transport in Candida utilis.

    Kilian, S G / Prior, B A / du Preez, J C

    World journal of microbiology & biotechnology

    2014  Volume 9, Issue 3, Page(s) 357–360

    Abstract: Low-affinity (K m=67.6±3.2 mM) and high-affinity (K m=1.9±1.2 mM) D-xylose transport occur ... in Candida utilis grown, respectively, on D-glucose or D-xylose. Starvation of glucose-grown cells decreases the K m ...

    Abstract Low-affinity (K m=67.6±3.2 mM) and high-affinity (K m=1.9±1.2 mM) D-xylose transport occur in Candida utilis grown, respectively, on D-glucose or D-xylose. Starvation of glucose-grown cells decreases the K m value (10.5±2.6 mm). The high-affinity system appearing during starvation required protein synthesis and it was inactivated when cells were exposed to glucose, by a process independent of protein synthesis. High-affinity transport was accompanied by transient alkalinization of yeast suspensions, indicating that it is a proton symport, whereas low-affinity transport was not. Both systems, however, were inhibited by metabolic inhibitors and by replacing H2O in the transport assay with D2O, indicating that both may be proton symports. Glucose and acetic acid also inhibited both high-and low-affinity xylose transport.
    Language English
    Publishing date 2014-01-14
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 1499109-3
    ISSN 1573-0972 ; 0959-3993
    ISSN (online) 1573-0972
    ISSN 0959-3993
    DOI 10.1007/BF00383080
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  6. Book ; Thesis: Die räumliche Erreichbarkeit zertifizierter Krebszentren in Deutschland als Grundvoraussetzung adäquater onkologischer Versorgung und deren Auswirking auf die Krankheitsverläufe der vier häufigsten Tumorerkrankungen

    Blome, Lauritz Kilian

    2021  

    Institution Goethe-Universität Frankfurt am Main
    Author's details vorgelegt von Lauritz Kilian Blome
    Language German
    Size 117, XXI Seiten, Diagramme, Karten, 21 cm
    Publishing place Frankfurt am Main
    Publishing country Germany
    Document type Book ; Thesis
    Thesis / German Habilitation thesis Dissertation, Johann Wolfgang Goethe-Universität Frankfurt am Main, 2021
    Note Zusammenfassung auf Deutsch und Englisch ; Literaturverzeichnis: Seite II-XVII
    HBZ-ID HT021131814
    Database Catalogue ZB MED Medicine, Health

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    In stock of ZB MED Cologne/Königswinter

    Shelf markLoan statusLocation
    2021 D 589 order for loan Magazin

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  7. Article ; Online: Nucleotide variability of Tahyna virus (Bunyaviridae, Orthobunyavirus) small (S) and medium (M) genomic segments in field strains differing in biological properties.

    Kilian, Patrik / Růzek, Daniel / Danielová, Vlasta / Hypsa, Václav / Grubhoffer, Libor

    Virus research

    2010  Volume 149, Issue 1, Page(s) 119–123

    Abstract: ... we analyzed complete nucleotide sequences of the small (S) and medium (M) genomic segments of field TAHV ... Within the M segment, the highest variability was observed in the G(C) gene encoding viral envelope protein and ... to a less extent also in the NSm gene. However, 5' and 3' non-coding regions of M segment, as well as in G(N ...

    Abstract Tahyna virus (TAHV), a mosquito-borne bunyavirus (California group), is frequently associated with inapparent or influenza-like (Valtice fever) infections in humans, rarely leading to atypical pneumonia or meningitis. Field TAHV strains exhibit a high variability in their biological properties with respect to virulence for laboratory mouse, temperature-sensitivity or character of plaques in cell culture. In consideration of the variations in the antigenic properties TAHV and its potential genetic variability, we analyzed complete nucleotide sequences of the small (S) and medium (M) genomic segments of field TAHV strains with different combinations of phenotypic markers. S segment was highly conservative in all analyzed TAHV strains. Within the M segment, the highest variability was observed in the G(C) gene encoding viral envelope protein and to a less extent also in the NSm gene. However, 5' and 3' non-coding regions of M segment, as well as in G(N) gene exhibited highly conservative pattern, indicating its functional importance, but minor or no role in the determination of biological properties of TAHV field strains.
    MeSH term(s) 3' Untranslated Regions ; 5' Untranslated Regions ; Animals ; Cluster Analysis ; Conserved Sequence ; Encephalitis Virus, California/genetics ; Encephalitis Virus, California/isolation & purification ; Encephalitis Virus, California/pathogenicity ; Encephalitis, California/virology ; Genetic Variation ; Genome, Viral ; Hot Temperature ; Humans ; Mice ; Molecular Sequence Data ; Phylogeny ; RNA, Viral/genetics ; Sequence Analysis, DNA ; Sequence Homology ; Viral Envelope Proteins/genetics ; Viral Plaque Assay ; Virulence
    Chemical Substances 3' Untranslated Regions ; 5' Untranslated Regions ; RNA, Viral ; Viral Envelope Proteins
    Language English
    Publishing date 2010-04
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 605780-9
    ISSN 1872-7492 ; 0168-1702
    ISSN (online) 1872-7492
    ISSN 0168-1702
    DOI 10.1016/j.virusres.2010.01.005
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    Zs.A 1965: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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  8. Book ; Thesis: Bestimmung und Messung physikalischer und technischer Parameter zur Beschreibung von Laufflächen in Milchviehställen

    Kilian, Michael

    (Schriftenreihe der Bayerischen Landesanstalt für Landwirtschaft ; 2007,10)

    2007  

    Author's details Michael Kilian
    Series title Schriftenreihe der Bayerischen Landesanstalt für Landwirtschaft ; 2007,10
    Collection
    Language German
    Size 251 S. : Ill., graph. Darst.
    Edition 1. Aufl.
    Publisher LfL
    Publishing place Freising-Weihenstephan
    Publishing country Germany
    Document type Book ; Thesis
    Thesis / German Habilitation thesis Gießen, Univ., Diss., 2007
    Note Zsfassung in engl. Sprache
    HBZ-ID HT015271334
    Database Catalogue ZB MED Nutrition, Environment, Agriculture

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    In stock of ZB MED Bonn / Germany

    Shelf markLoan statusLocation
    074/522 available for loan (reading room) Freihandmagazin (U1)

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  9. Book ; Online: Auswirkungen von organischen Bodenzusätzen auf biodiversitätsgefährdende Stoffströme in der Landwirtschaft

    Siedt, Martin / Nabel, Moritz / Roß-Nickoll, Martina / Schäffer, Andreas / Smith, Kilian E. C. / Dongen, Joost T. van

    Einflüsse auf die mikrobielle Diversität, die Nährstoffe, den Abbau von Pestiziden und die Mobilität von Schwermetallen in Ackerböden

    (BfN-Schriften ; 660 (2023))

    2023  

    Author's details Martin Siedt, Moritz Nabel, Martina Roß-Nickoll, Andreas Schäffer, Kilian E.C. Smith, Joost T. van Dongen
    Series title BfN-Schriften ; 660 (2023)
    Collection
    Language German
    Size 1 Online-Ressource (79 Seiten), Illustrationen, Diagramme
    Publisher Bundesamt für Naturschutz
    Publishing place Bonn
    Publishing country Germany
    Document type Book ; Online
    Note Open Access
    HBZ-ID HT030061658
    ISBN 9783896244215 ; 3896244213
    Database ZB MED Catalogue: Medicine, Health, Nutrition, Environment, Agriculture

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  10. Book ; Thesis: Prospektive Studie zur Analyse der klinischen Ergebnisse nach arthroskopischer Arthrolyse des Ellenbogengelenkes

    Borda, Alex / Wegmann, Kilian / Scaal, Martin

    2020  

    Institution Universitätsklinikum Köln / Klinik und Poliklinik für Orthopädie und Unfallchirurgie
    Author's details vorgelegt von Alex Borda ; 1. Gutachter: Privatdozent Dr. med. K. Wegmann, 2. Gutachter: Universitätsprofessor Dr. rer. nat. M. Scaal ; aus der Klinik und Poliklinik für Orthopädie und Unfallchirurgie der Universität zu Köln
    Subject code 610
    Language German
    Size 72 Seiten, Illustrationen, Diagramme
    Publishing place Köln
    Publishing country Germany
    Document type Book ; Thesis
    Thesis / German Habilitation thesis Dissertation, Universität zu Köln, 2020
    HBZ-ID HT020430369
    Database Catalogue ZB MED Medicine, Health

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    In stock of ZB MED Cologne/Königswinter

    Shelf markLoan statusLocation
    2020 D 314 order for loan Magazin

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