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Biotinylated platinum(IV) complexes designed to target cancer cells.

Abstract：

:Three biotinylated platinum(IV) complexes (1-3) were designed and synthesized. The resulting platinum(IV) complexes exhibited effective cytotoxicity against the tested cancer cell lines, especially complex 1, which was 2.0-9.6-fold more potent than cisplatin. These complexes were found to be rapidly reduced to their activated platinum(II) counterparts by glutathione or ascorbic acid under biologically relevant condition. Additional molecular docking studies revealed that the biotin moieties of all Pt(IV) complexes can effectively bind with the streptavidin through the noncovalent interactions. Besides, introduction of the biotin group can obviously promote the cancer cell uptake of platinum when treated with complex 1, particularly in cisplatin-resistant SGC-7901/Cis cancer cells. Further mechanistic studies on complex 1 indicated that it activated the expression of Bax, and induced cytochrome c release from the mitochondria, and finally activated caspase-3.

journal_name

J Inorg Biochem

journal_title

Journal of inorganic biochemistry

authors

Zhao J,Hua W,Xu G,Gou S

doi

10.1016/j.jinorgbio.2017.08.017

subject

Has Abstract

pub_date

2017-11-01 00:00:00

pages

175-180

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(17)30411-7

journal_volume

176

pub_type

杂志文章

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