國家衛生研究院 NHRI:Item 3990099045/12995
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    题名: BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy
    作者: Chen, YY;Lo, CF;Chiu, TY;Hsu, CY;Yeh, TK;Chen, CP;Huang, CL;Huang, CY;Wang, MH;Huang, YC;Ho, HH;Chao, YS;Shih, JC;Tsou, LK;Chen, CT
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Zinc(II)-dipicolylamine (Zn-DPA) has been shown to specifically identify and bind to phosphatidylserine (PS), which exists in bulk in the tumor microenvironment. BPRDP056, a Zn-DPA-SN38 conjugate was designed to provide PS-targeted drug delivery of a cytotoxic SN38 to the tumor microenvironment, thereby allowing a lower dosage of SN38 that induces apoptosis in cancer cells. Micro-Western assay showed that BPRDP056 exhibited apoptotic signal levels similar to those of CPT-11 in the treated tumors growing in mice. Pharmacokinetic study showed that BPRDP056 has excellent systemic stability in circulation in mice and rats. BPRDP056 is accumulated in tumors and thus increases the cytotoxic effects of SN38. The in vivo antitumor activities of BPRDP056 have been shown to be significant in subcutaneous pancreas, prostate, colon, liver, breast, and glioblastoma tumors, included an orthotopic pancreatic tumor, in mice. BPRDP056 shrunk tumors at a lower (~20% only) dosing intensity of SN38 compared to that of SN38 conjugated in CPT-11 in all tumor models tested. A wide spectrum of antitumor activities is expected to treat all cancer types of PS-rich tumor microenvironments. BPRDP056 is a first-in-class small molecule drug conjugate for cancer therapy.
    日期: 2021-01
    關聯: Translational Oncology. 2021 Jan;14(1):Article number 100897.
    Link to: http://dx.doi.org/10.1016/j.tranon.2020.100897
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1936-5233&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000608422100006
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85092472758
    显示于类别:[鄒倫] 期刊論文
    [陳炯東] 期刊論文
    [石全(2014-2017)] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [葉燈光] 期刊論文

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