國家衛生研究院 NHRI:Item 3990099045/16276
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    题名: Discovery of novel TANK-Binding Kinase 1 (TBK1) inhibitor against pancreatic ductal adenocarcinoma
    作者: Shih, WH;Huang, HL;HuangFu, WC;Lin, TE;Sung, TY;Li, MC;Huang, GL;Chang, YW;Yen, SC;Hsieh, HP;Hsu, KC;Pan, SL
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Pancreatic ductal adenocarcinoma (PDAC) has limited treatment options, underscoring the urgent need for developing new therapies. The upregulation of TBK1 activity plays a crucial role in multiple pancreatic cancer-related signaling pathways, suggesting that inhibiting the kinase activity of TBK1 could be a promising strategy. Herein, we discovered a novel TBK1 inhibitor, LIB3S0280, using a structure-based virtual screening (SBVS) strategy. In the anti-proliferative and viability assays, LIB3S0280 showed significant inhibition against pancreatic cancer cell lines that highly express TBK1 with the GI(50) values of 2.24 and 4.71 μM and IC(50) values of 6.64 and 10.98 μM at 96 h. For the downstream targets, LIB3S0280 can inhibit TBK1 downstream signaling by decreasing the phosphorylation of IκBα and AKT better than a known TBK1 inhibitor, BX-795. Furthermore, PDAC cells were arrested in G(2)/M and underwent apoptosis or senescence with the treatment of LIB3S0280. These findings suggest that TBK1 inhibitor LIB3S0280 has great potential as a lead compound in the further development of a novel treatment for PDAC.
    日期: 2024-12
    關聯: International Journal of Biological Macromolecules. 2024 Dec;283(Part 1):Article number 137296.
    Link to: http://dx.doi.org/10.1016/j.ijbiomac.2024.137296
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0141-8130&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:001361985000001
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85209147177
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