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Please use this identifier to cite or link to this item:
http://ir.nhri.org.tw/handle/3990099045/12995
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| Title: | BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy |
| Authors: | 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 |
| Contributors: | Institute of Biotechnology and Pharmaceutical Research |
| Abstract: | 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. |
| Date: | 2021-01 |
| Relation: | 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 |
| Appears in Collections: | [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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| SCP85092472758.pdf | | 2507Kb | Adobe PDF | 311 | View/Open |
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