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一种铑(III)配合物作为针对TP53突变三阴性乳腺癌细胞的Wee1抑制剂的鉴定。

Identification of a rhodium(iii) complex as a Wee1 inhibitor against TP53-mutated triple-negative breast cancer cells.

作者信息

Yang Guan-Jun, Zhong Hai-Jing, Ko Chung-Nga, Wong Suk-Yu, Vellaisamy Kasipandi, Ye Min, Ma Dik-Lung, Leung Chung-Hang

机构信息

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.

出版信息

Chem Commun (Camb). 2018 Mar 6;54(20):2463-2466. doi: 10.1039/c7cc09384e.

DOI:10.1039/c7cc09384e
PMID:29367998
Abstract

The rhodium(iii) complex 1 was identified as a potent Wee1 inhibitor in vitro and in cellulo. It decreased Wee1 activity and unscheduled mitotic entry, and induced cell damage and death in TP53-mutated triple-negative breast cancer cells. 1 represents a promising scaffold for further development of more potent metal-based Wee1 antagonists.

摘要

铑(III)配合物1在体外和细胞内被鉴定为一种有效的Wee1抑制剂。它降低了Wee1活性和非计划有丝分裂进入,并在TP53突变的三阴性乳腺癌细胞中诱导细胞损伤和死亡。1代表了一个有前景的骨架,可用于进一步开发更有效的金属基Wee1拮抗剂。

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