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  1. Article ; Online: Chitosan-assisted permeabilization of ATP–biotin for live cell kinase-catalyzed biotinylation

    Ahmed E Fouda / D Maheeka Embogama / Vindya Ramanayake-Mudiyanselage / Mary Kay H Pflum

    BioTechniques, Vol 65, Iss 3, Pp 143-

    2018  Volume 148

    Abstract: Kinases are essential cell signaling enzymes that phosphorylate protein substrates using ATP as the universal cosubstrate. A wide variety of ATP analogs have been used in kinase research, although the studies are limited by the cell impermeability of ATP. ...

    Abstract Kinases are essential cell signaling enzymes that phosphorylate protein substrates using ATP as the universal cosubstrate. A wide variety of ATP analogs have been used in kinase research, although the studies are limited by the cell impermeability of ATP. Here we describe the use of the cationic polymer deacetylated chitosan to permeabilize ATP analogs for live cell applications, including kinase-catalyzed biotinylation.
    Keywords Biology (General) ; QH301-705.5
    Language English
    Publishing date 2018-09-01T00:00:00Z
    Publisher Future Science Ltd
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Rational design of metabolically stable HDAC inhibitors: An overhaul of trifluoromethyl ketones.

    Riddhidev, Banerjee / Endri, Karaj / Sabitri, Lamichhane / Kotsull Lauren, N / Nishanth, Kuganesan / Dragan, Isailovic / Mary Kay H, Pflum / James, Slama / William, Taylor / L M Viranga, Tillekeratne

    European journal of medicinal chemistry

    2022  Volume 244, Page(s) 114807

    Abstract: Epigenetic regulation of gene expression using histone deacetylase (HDAC) inhibitors is a promising strategy for developing new anticancer agents. The most common HDAC inhibitors are hydroxamates, which, though highly potent, have limitations due to ... ...

    Abstract Epigenetic regulation of gene expression using histone deacetylase (HDAC) inhibitors is a promising strategy for developing new anticancer agents. The most common HDAC inhibitors are hydroxamates, which, though highly potent, have limitations due to their poor pharmacokinetic properties and lack of isoform selectivity. Trifluoromethylketones (TFMK) developed as alternatives to hydroxamates are rapidly metabolized to inactive trifluoromethyl alcohols in vivo, which prevented their further development as potential drug candidates. In order to overcome this limitation, we designed trifluoropyruvamides (TFPAs) as TFMK surrogates. The presence of an additional electron withdrawing group next to the ketone carbonyl group made the hydrate form of the ketone more stable, thus preventing its metabolic reduction to alcohol in vivo. In addition, this structural modification reduces the potential of the TFMK group to act as a covalent warhead to eliminate off-target effects. Additional structural changes in the cap group of the inhibitors gave analogues with IC
    MeSH term(s) Histone Deacetylase Inhibitors/pharmacology ; Histone Deacetylase Inhibitors/chemistry ; Ketones/pharmacology ; Epigenesis, Genetic ; Repressor Proteins/metabolism ; Hydroxamic Acids/chemistry ; Protein Isoforms/metabolism
    Chemical Substances Histone Deacetylase Inhibitors ; Ketones ; Repressor Proteins ; Hydroxamic Acids ; Protein Isoforms
    Language English
    Publishing date 2022-10-05
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2022.114807
    Database MEDical Literature Analysis and Retrieval System OnLINE

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