國家衛生研究院 NHRI:Item 3990099045/12018
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    题名: Linker optimization and therapeutic evaluation of phosphatidylserine-targeting zinc dipicolylamine-based drug conjugates
    作者: Liu, YW;Chen, YY;Hsu, CY;Chiu, TY;Liu, KL;Lo, CF;Fang, MY;Huang, YC;Yeh, TK;Pak, KY;Gray, BD;Hsu, TA;Huang, KH;Shih, C;Shia, KS;Chen, CT;Tsou, LK
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: We report that compound 13, a novel phosphatidylserine-targeting zinc(II) dipicolylamine drug conjugate, readily triggers a positive feedback therapeutic loop through the in situ generation of phosphatidylserine in the tumor microenvironment. Linker modifications, pharmacokinetics profiling, in vivo antitumor studies, and micro-Western array of treated-tumor tissues were employed to show that this class of conjugates induced regeneration of apoptotic signals, which facilitated subsequent recruitment of the circulating conjugates through the zinc(II) dipicolylamine-phosphatidylserine association and resulted in compounding antitumor efficacy. Compared to the marketed compound 17, compound 13 not only induced regressions in colorectal and pancreatic tumor models, it also exhibited at least 5-fold enhancement in antitumor efficacy with only 40% of the drug employed during treatment, culminating in a >12.5-fold increase in therapeutic potential. Our study discloses a chemically distinct apoptosis-targeting theranostic, with built-in complementary functional moieties between the targeting module and the drug mechanism to expand the arsenal of antitumor therapy.
    日期: 2019-07-11
    關聯: Journal of Medicinal Chemistry. 2019 Jul 11;62(13):6047-6062.
    Link to: http://dx.doi.org/10.1021/acs.jmedchem.9b00173
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000475543300007
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85068148444
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