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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Research Article

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 and Qiang Yu*

Volume 18, Issue 3, 2018

Page: [422 - 427] Pages: 6

DOI: 10.2174/1871520617666171106123226

Price: $65

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.

Graphical Abstract

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