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

doi:10.1038/srep36044

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

Department of Chemistry

Research output: Contribution to journal › Journal article › peer-review

15 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 language	English
Article number	36044
Journal	Scientific Reports
Volume	6
DOIs	https://doi.org/10.1038/srep36044
Publication status	Published - 17 Nov 2016

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@article{23952e0a252442c6bea69af3ef84f203,

title = "Antagonizing STAT5B dimerization with an osmium complex",

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.",

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

year = "2016",

month = nov,

day = "17",

doi = "10.1038/srep36044",

language = "English",

volume = "6",

journal = "Scientific Reports",

issn = "2045-2322",

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T1 - Antagonizing STAT5B dimerization with an osmium complex

AU - Liu, Li Juan

AU - Wang, Wanhe

AU - Kang, Tian Shu

AU - Liang, Jia Xin

AU - LIU, Chenfu

AU - KWONG, Daniel W J

AU - Wong, Vincent Kam Wai

AU - MA, Edmond Dik Lung

AU - Leung, Chung Hang

PY - 2016/11/17

Y1 - 2016/11/17

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=84995934822&partnerID=8YFLogxK

U2 - 10.1038/srep36044

DO - 10.1038/srep36044

M3 - Journal article

C2 - 27853239

AN - SCOPUS:84995934822

SN - 2045-2322

VL - 6

JO - Scientific Reports

JF - Scientific Reports

M1 - 36044

ER -

Antagonizing STAT5B dimerization with an osmium complex

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