• Pioneering technique could unlock target

    From ScienceDaily@1:317/3 to All on Thursday, March 17, 2022 22:30:44
    Pioneering technique could unlock targeted treatments for cancer

    Date:
    March 17, 2022
    Source:
    University of Leicester
    Summary:
    Researchers have described application of a pioneering chemical
    technique which could unlock ground-breaking new treatments for
    cancer and other diseases.



    FULL STORY ========================================================================== Leicester researchers have described application of a pioneering chemical technique which could unlock ground-breaking new treatments for cancer
    and other diseases.


    ========================================================================== Members of the Leicester Institute of Structural and Chemical Biology,
    based at the University of Leicester, used proteolysis targeting chimeras (PROTACs) as a 'bridge' to degrade proteins implicated in cancer.

    Scientists can manipulate the effectiveness of treatments by making
    changes to elements of this PROTAC bridge.

    This new study, published in the Journal of Medicinal Chemistry,
    describes how Leicester researchers applied a previously-described protein degradation technique known as PROTACs to degrade histone deacetylation
    enzymes (HDACs) in a more targeted way than ever before.

    HDACs play an important role in gene regulation, in which genes are
    switched 'on' and 'off', and are associated with a range of diseases,
    including cancer as well as various neurodegenerative disorders including Alzheimer's disease.

    Using this pioneering technique to target specific structures within
    cancerous cells could increase the potency and selectivity of new and
    existing drugs, meaning patients would require lower systemic exposure
    to drug treatments leading to a reduction in harmful side-effects to
    patients.



    ==========================================================================
    The group have been granted a patent by the European Patent Office for
    the pioneering technique.

    Dr James Hodgkinson is an Associate Professor in Organic Chemistry
    and Chemical Biology at the University of Leicester and one of the corresponding authors for the study. He said: "We are really excited
    about what these new molecules are capable of in cancer cells and their potential future development into medicines.

    "Our next steps will involve optimising their chemical structure and
    biological properties so that one day they could be used to improve
    the lives of cancer patients." John Schwabe is Professor of Structural
    Biology and Director of the Leicester Institute of Structural and Chemical Biology, and also a corresponding author on the study. Professor Schwabe
    added: "The potential of using specific degraders of therapeutic targets
    is very powerful.

    "This work has been the result of a productive three-way collaboration
    between chemists, biologists and biophysicists -- an exciting combination
    to deliver interdisciplinary research." The Leicester Institute of
    Structural and Chemical Biology leads interdisciplinary research across
    22 separate research groups at the University of Leicester.

    Other work includes innovative research to create a potential vaccine
    against Alzheimer's disease.


    ========================================================================== Story Source: Materials provided by University_of_Leicester. Note:
    Content may be edited for style and length.


    ========================================================================== Journal Reference:
    1. Joshua P. Smalley, India M. Baker, Wiktoria A. Pytel, Li-Ying
    Lin, Karen
    J. Bowman, John W. R. Schwabe, Shaun M. Cowley, James T. Hodgkinson.

    Optimization of Class I Histone Deacetylase PROTACs Reveals that
    HDAC1/ 2 Degradation is Critical to Induce Apoptosis and Cell
    Arrest in Cancer Cells. Journal of Medicinal Chemistry, 2022; DOI:
    10.1021/ acs.jmedchem.1c02179 ==========================================================================

    Link to news story: https://www.sciencedaily.com/releases/2022/03/220317143733.htm

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