• New tool to accelerate drug discovery

    From ScienceDaily@1:317/3 to All on Tuesday, March 22, 2022 22:30:46
    New tool to accelerate drug discovery
    Simpler, less-expensive method using bioluminescence shines light on
    real-time cellular traffic

    Date:
    March 22, 2022
    Source:
    University of Houston
    Summary:
    New technology will accelerate drug development by allowing
    researchers a better look inside the cell membrane to observe how
    cells react to drugs.



    FULL STORY ========================================================================== Inside your body on the surface of cell membranes, a metaphorical
    communication and traffic network is underway as hormones -- or chemical messengers -- bind to cell membrane receptors to fine tune how the
    cell behaves. Once bound together, this hormone-receptor complex works
    to carry out a variety of functions by ferrying chemical signals from
    outside the cell and translating those signals into action inside the
    cell. The process of moving into the cell is called trafficking.


    ==========================================================================
    Now, for the first time, new technology developed at the University of
    Houston College of Pharmacy will be able to peer inside and get a close
    look at the trafficking in real-time. Bradley McConnell, professor
    of pharmacology, has devised a way to watch the membrane protein
    trafficking using bioluminescence, the production and emission of light
    inside living organisms, replacing the need for complicated protocols,
    methods or highly automated equipment.

    "We describe a powerful unrestricted and universal technology of drug
    discovery that is based on trafficking properties of plasma membrane receptors," reports McConnell in Communications Biology, a Nature
    journal. The paper's lead author is Arfaxad Reyes-Alcaraz, a postdoctoral fellow in McConnell's laboratory.

    "This technology can be applied to monitoring the effectiveness of a
    potential new therapeutic drug that is targeted to a cell receptor and
    then internalized into the cell. It can also be used to monitor the
    SARS-CoV-2 viral entry into the cell." Ultimately, the researchers
    expect the process to be used for drug development for heart disease,
    metabolic disorders, cancer, infectious diseases, COVID-19 and others.

    The process monitors how cell receptors are internalized into the cell as
    part of their normal function in response to a hormone, or a therapeutic
    drug, interacting with its receptor -- a powerful tool to understand how
    the body works. Scientists have successfully studied this process for
    years using complex and expensive biological tools, but highly sensitive
    and versatile technologies have been lacking to study such processes in real-time living systems.

    "Now imagine studying this process simply and inexpensively with a
    method that is even more informative than is currently available," said McConnell. "The ability to selectively generate a bioluminescent signal
    when the membrane receptor is in the early endosome to monitor receptor internalization (i.e., membrane trafficking) is novel."

    ========================================================================== Story Source: Materials provided by University_of_Houston. Original
    written by Laurie Fickman. Note: Content may be edited for style and
    length.


    ========================================================================== Journal Reference:
    1. Arfaxad Reyes-Alcaraz, Emilio Y. Lucero Garcia-Rojas, Elizabeth A.

    Merlinsky, Jae Young Seong, Richard A. Bond, Bradley K. McConnell. A
    NanoBiT assay to monitor membrane proteins trafficking for drug
    discovery and drug development. Communications Biology, 2022; 5
    (1) DOI: 10.1038/ s42003-022-03163-9 ==========================================================================

    Link to news story: https://www.sciencedaily.com/releases/2022/03/220322122817.htm

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