Antagonizing STAT5B dimerization with an osmium complex

Li Juan Liu, Wanhe Wang, Tian Shu Kang, Jia Xin Liang, Chenfu LIU, Daniel W J KWONG, Vincent Kam Wai Wong, Edmond Dik Lung MA, Chung Hang Leung*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

13 Citations (Scopus)

Abstract

Targeting STAT5 is an appealing therapeutic strategy for the treatment of hematologic malignancies and inflammation. Here, we present the novel osmium(II) complex 1 as the first metal-based inhibitor of STAT5B dimerization. Complex 1 exhibited superior inhibitory activity against STAT5B DNA binding compared to STAT5A DNA binding. Moreover, 1 repressed STAT5B transcription and blocked STAT5B dimerization via binding to the STAT5B protein, thereby inhibiting STAT5B translocation to the nucleus. Furthermore, 1 was able to selectively inhibit STAT5B phosphorylation without affecting the expression level of STAT5B.

Original languageEnglish
Article number36044
JournalScientific Reports
Volume6
DOIs
Publication statusPublished - 17 Nov 2016

Scopus Subject Areas

  • General

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