Synthesis of Biotinylated 2-methoxystypandrone and Identification of JAK2 and IKK as its Targets

Author(s): Shan Kuang, Zhenhua Sima, Jiawei Liu*, Wuguo Li, Qiaoling Song, Qing Zhang, Qiang Yu*

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 18 , Issue 3 , 2018

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Graphical Abstract:


Background: 2-Methoxystypandrone (2-MS), isolated from the roots of Polygonum cuspidatum, is a potent dual inhibitor of the STAT3 and NF-κB pathways.

Objective: To investigate the molecular targets and mechanisms of 2-MS.

Method: A biotin-conjugated 2-MS analog, named 2-MS-Biotin, was designed and synthesized. The effects of 2-MS-Biotin on the STAT3 and NF-κB pathways were examined by Western blotting. The cytotoxicity of 2- MS-Biotin was evaluated using real-time cell analysis system. Proteins directly bound to 2-MS-Biotin were pulled down through streptavidin agarose beads and were detected using Western blotting.

Results: 2-MS-Biotin retained the inhibition activities of the parent compound 2-MS on the STAT3 and NF-κB pathways as well as on cancer cell growth. Also, JAK2 and IKK proteins can be effectively pulled down by 2- MS-Biotin.

Conclusion: Using 2-MS-Biotin as a tool, both JAK2 and IKK were identified as the targets of 2-MS.

Keywords: 2-Methoxystypandrone, natural compound, biotin-tagged probe, anticancer drug, JAK2, IKK.

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Article Details

Year: 2018
Published on: 04 June, 2018
Page: [422 - 427]
Pages: 6
DOI: 10.2174/1871520617666171106123226
Price: $65

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