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    Home > Biochemistry News > Biotechnology News > The annual "star" small molecule list is released, including long-acting HIV therapy, PROTAC molecules...

    The annual "star" small molecule list is released, including long-acting HIV therapy, PROTAC molecules...

    • Last Update: 2021-04-19
    • Source: Internet
    • Author: User
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    Recently, the drughunter website announced the annual list of small molecules selected by industry drug developers.


    The top-ranked lenacapavir is one of the key drugs in the recent major research and development cooperation between Gilead Sciences and Merck & Co.


    HIV capsid: closely related to HIV replication but difficult to target

    HIV capsid: closely related to HIV replication but difficult to target

    Speaking of lenacapavir, we must first talk about its target, the capsid protein of HIV.


    This capsid is formed by the self-assembly of thousands of capsid protein monomers.


    Lenacapavir: Make HIV capsid a "fake and shoddy product"

    Lenacapavir: Make HIV capsid a "fake and shoddy product"

    Just as a good Lego model requires every small building block to be stitched together tightly, the normal function of the capsid also requires the precise assembly of the capsid protein monomers.


    This is also the direction of drug research and development.


    Based on this idea, the R&D team of Gilead Sciences screened drugs that affect the capsid assembly process.


    Brings hope for long-acting HIV therapy

    Brings hope for long-acting HIV therapy

    Another difficulty in developing long-acting HIV therapy is to prevent the drug from being cleared by the liver.


    In addition to being a long-acting therapy for people with HIV infection, Gilead Sciences is also conducting clinical trials to evaluate the potential of lenacapavir as a pre-exposure prophylaxis (PrEP) therapy.


    The drug hunter website pointed out that lenacapavir is a classic case of small molecule drug development, and I wish it more good news in the future clinical development and approval process.


    Reference materials:

    [1] Small Molecule of the Year – 2020.


    [2] Gilead's Investigational Lenacapavir DemonstratesSustained Long-Acting Efficacy Through Week 26 in Data Presented at CROI.


    [3] Gilead and Merck Announce Agreement to Jointly Develop and Commercialize Long-Acting, Investigational Treatment Combinations of Lenacapavir and Islatravir in HIV.


    [4] Capsid.


    [5] Quinn et al.


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