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Antagonizing STAT3 dimerization with a rhodium(III) complex
Ma D.-L.1; Liu L.-J.2; Leung K.-H.1; Chen Y.-T.3; Zhong H.-J.2; Chan D.S.-H.2; Wang H.-M.D.3; Leung C.-H.2
2014
Source PublicationAngewandte Chemie - International Edition
ISSN14337851
Volume53Issue:35Pages:9178
Abstract

Kinetically inert metal complexes have arisen as promising alternatives to existing platinum and ruthenium chemotherapeutics. Reported herein, to our knowledge, is the first example of a substitutionally inert, Group9 organometallic compound as a direct inhibitor of signal transducer and activator of transcription3 (STAT3) dimerization. From a series of cyclometalated rhodium(III) and iridium(III) complexes, a rhodium(III) complex emerged as a potent inhibitor of STAT3 that targeted the SH2 domain and inhibited STAT3 phosphorylation and dimerization. Significantly, the complex exhibited potent anti-tumor activities in an invivo mouse xenograft model of melanoma. This study demonstrates that rhodium complexes may be developed as effective STAT3 inhibitors with potent anti-tumor activity. Saving your skin: A rhodium(III) complex is the first example of a substitutionally inert, Group9 organometallic compound which serves as a direct inhibitor of the signal transducer and activator of transcription3 (STAT3) dimerization. The rhodium(III) complex inhibited STAT3 activity invitro and invivo and showed potent and selective anticancer activity against melanoma cell lines and melanoma xenografts in an invivo mouse model. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

KeywordAntitumor Agents Cytotoxicity Dimerization Protein-protein Interactions Rhodium
DOI10.1002/anie.201404686
URLView the original
Indexed BySCI
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000342676100007
The Source to ArticleScopus
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Cited Times [WOS]:87   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorMa D.-L.; Leung C.-H.
Affiliation1.Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong (China)
2.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao (China)
3.Department of Fragrance and Cosmetic Science, Kaohsiung Medical University, Kaohsiung 807, Taiwan (Republic of China)
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Ma D.-L.,Liu L.-J.,Leung K.-H.,et al. Antagonizing STAT3 dimerization with a rhodium(III) complex[J]. Angewandte Chemie - International Edition,2014,53(35):9178.
APA Ma D.-L..,Liu L.-J..,Leung K.-H..,Chen Y.-T..,Zhong H.-J..,...&Leung C.-H..(2014).Antagonizing STAT3 dimerization with a rhodium(III) complex.Angewandte Chemie - International Edition,53(35),9178.
MLA Ma D.-L.,et al."Antagonizing STAT3 dimerization with a rhodium(III) complex".Angewandte Chemie - International Edition 53.35(2014):9178.
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