國家衛生研究院 NHRI:Item 3990099045/12995

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Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/12995

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:	[Lun Kelvin Tsou] Periodical Articles [Chiung-Tong Chen] Periodical Articles [Chuan Shih(2014-2017)] Periodical Articles [Yu-Sheng Chao(2002-2013)] Periodical Articles [Teng-Kuang Yeh] Periodical Articles

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