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  1. AU="Gafuik, Christopher J"
  2. AU="Lubsandorzhiev, B K"
  3. AU="Ni, Connie W"
  4. AU="Halpern, Allan C"
  5. AU=Ratner Nancy
  6. AU="Lynch, Jeremy"
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  11. AU="Nawrocki, Eric P."
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  21. AU="Vasconcellos, Silvio A"
  22. AU="Etenko, A."
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  1. Article ; Online: Utilising the intrinsic fluorescence of pomalidomide for imaging applications.

    Brownsey, Duncan K / Gafuik, Christopher J / Kim, Dae-Sun / O'Sullivan, Leonie / Gorobets, Evgueni / Krukowski, Samuel / Turk, Madison / Jenne, Craig N / Mahoney, Douglas J / Derksen, Darren J

    Chemical communications (Cambridge, England)

    2023  Volume 59, Issue 98, Page(s) 14532–14535

    Abstract: Optimisation of protein degraders requires balancing multiple factors including potency, cell permeability and solubility. Here we show that the fluorescence of pomalidomide can be used in high-throughput screening assays to rapidly assess cellular ... ...

    Abstract Optimisation of protein degraders requires balancing multiple factors including potency, cell permeability and solubility. Here we show that the fluorescence of pomalidomide can be used in high-throughput screening assays to rapidly assess cellular penetration of degrader candidates. In addition, this technique can be paired with endocytosis inhibitors to gain insight into potential mechanisms of candidates entering a target cell. A model library of pomalidomide conjugates was synthesised and evaluated using high-throughput fluorescence microscopy. This technique based on intrinsic fluorescence can be used to guide rational design of pomalidomide conjugates without the need for additional labels or tags.
    MeSH term(s) Thalidomide/pharmacology ; Microscopy, Fluorescence
    Chemical Substances pomalidomide (D2UX06XLB5) ; Thalidomide (4Z8R6ORS6L)
    Language English
    Publishing date 2023-12-07
    Publishing country England
    Document type Journal Article
    ZDB-ID 1472881-3
    ISSN 1364-548X ; 1359-7345 ; 0009-241X
    ISSN (online) 1364-548X
    ISSN 1359-7345 ; 0009-241X
    DOI 10.1039/d3cc04314b
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: macroH2A2 antagonizes epigenetic programs of stemness in glioblastoma.

    Nikolic, Ana / Maule, Francesca / Bobyn, Anna / Ellestad, Katrina / Paik, Seungil / Marhon, Sajid A / Mehdipour, Parinaz / Lun, Xueqing / Chen, Huey-Miin / Mallard, Claire / Hay, Alexander J / Johnston, Michael J / Gafuik, Christopher J / Zemp, Franz J / Shen, Yaoqing / Ninkovic, Nicoletta / Osz, Katalin / Labit, Elodie / Berger, N Daniel /
    Brownsey, Duncan K / Kelly, John J / Biernaskie, Jeff / Dirks, Peter B / Derksen, Darren J / Jones, Steven J M / Senger, Donna L / Chan, Jennifer A / Mahoney, Douglas J / De Carvalho, Daniel D / Gallo, Marco

    Nature communications

    2023  Volume 14, Issue 1, Page(s) 3062

    Abstract: Self-renewal is a crucial property of glioblastoma cells that is enabled by the choreographed functions of chromatin regulators and transcription factors. Identifying targetable epigenetic mechanisms of self-renewal could therefore represent an important ...

    Abstract Self-renewal is a crucial property of glioblastoma cells that is enabled by the choreographed functions of chromatin regulators and transcription factors. Identifying targetable epigenetic mechanisms of self-renewal could therefore represent an important step toward developing effective treatments for this universally lethal cancer. Here we uncover an epigenetic axis of self-renewal mediated by the histone variant macroH2A2. With omics and functional assays deploying patient-derived in vitro and in vivo models, we show that macroH2A2 shapes chromatin accessibility at enhancer elements to antagonize transcriptional programs of self-renewal. macroH2A2 also sensitizes cells to small molecule-mediated cell death via activation of a viral mimicry response. Consistent with these results, our analyses of clinical cohorts indicate that high transcriptional levels of this histone variant are associated with better prognosis of high-grade glioma patients. Our results reveal a targetable epigenetic mechanism of self-renewal controlled by macroH2A2 and suggest additional treatment approaches for glioblastoma patients.
    MeSH term(s) Humans ; Histones/genetics ; Histones/metabolism ; Glioblastoma/metabolism ; Gene Expression Regulation, Neoplastic ; Chromatin/metabolism ; Epigenesis, Genetic ; Cell Line, Tumor ; Neoplastic Stem Cells/metabolism ; Brain Neoplasms/genetics ; Brain Neoplasms/metabolism
    Chemical Substances Histones ; Chromatin
    Language English
    Publishing date 2023-05-27
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2553671-0
    ISSN 2041-1723 ; 2041-1723
    ISSN (online) 2041-1723
    ISSN 2041-1723
    DOI 10.1038/s41467-023-38919-2
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

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