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    Home > Active Ingredient News > Antitumor Therapy > 【STTT】Central South University team developed a new FASN inhibitor for the treatment of various tumors!

    【STTT】Central South University team developed a new FASN inhibitor for the treatment of various tumors!

    • Last Update: 2022-09-09
    • Source: Internet
    • Author: User
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    This article is original from Translational Medicine Network, please indicate the source for reprinting 

    Author: TMZHI

    Introduction: Fatty acid synthase (FASN) is a key enzyme in regulating the de novo fatty acid synthesis pathway.


    On August 24, Prof.


    Doi: 10.


    Research Background

     01 

    Reprogramming of tumor lipid metabolism is closely related to multiple biological behaviors such as tumorigenesis, progression, and drug resistance.


    research process

     02 

    In order to screen for specific FASN inhibitors against non-small cell lung cancer, the researchers used KRAS-positive cells A549 and NCI-H1299 to centrally screen the library of laminacin derivatives and found that compared to the developed FASN inhibitor Ollie Lista, TVB-3166, the screened compound 6p has higher sensitivity, stronger proliferation and invasion inhibitory effect, and 6 can specifically bind to FASN and play a targeting role (Figure 1)


    Figure 1.



    In addition, the researchers also discovered the mechanism by which the novel FASN inhibitor 6p exerts its antitumor effect.


    Figure 2.



    To study the in vivo antitumor effect of FASN inhibitor 6p, the researchers constructed a lung cancer cell xenograft model and found that 6p reduced the levels of FASN and p-AKT in tumors, significantly inhibited tumor growth, and had no obvious toxicity


    Figure 3.


    Significance

     03 

    FASN can be used as a target for a variety of tumor therapy, but there are no better targeted therapy drugs in clinical use


    References:


    Cao D, Yang J, Deng Y, et al.


    Note: This article is intended to introduce the progress of medical research and cannot be used as a reference for treatment plans


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