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On September 14, 2022, the Journal of Medicinal Chemistry, an authoritative journal of international medicinal chemistry, published online, "Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr705/Ser727 Inhibitory Activity.
Figure 1.
In recent years, targeted transcription regulators have become one
of the hot research areas for the development of novel antitumor drugs.
Figure 2.
In this study, the authors established a new high-throughput screening experiment for STAT3 bisphosphorylation inhibitors based on the important role of STAT3 bilosite phosphorylation in the development of gastric cancer cells in the development of gastric cancer cells, namely the STAT3 p-Tyr705 inhibitor STAT3 dependent luciferase experiment (Luciferase reporter) based on the different biological functions of STAT3 bilosite phosphorylation in tumor cells assay) and ATP inhibition assay for characterizing p-Ser727 inhibition activity
.
Figure 3: Structural optimization process from seedling compound to lead compound
Figure 4.
In the following work, the authors conducted systematic target validation and in vivo anti-tumor activity evaluation
of the lead compound HP590.
Figure 5.
Finally, the authors evaluated
HP590's proliferative activity of anti-gastric cancer cells in vivo and abroad.
Summary: This study reports a new high-throughput screening strategy for STAT3 biphosphorylation inhibitors, elaborates the research process from the discovery of the seedling compound to the transformation of the lead compound and the structure-activity relationship, and determines that HP590 can be used as a new class of selective STAT3 bi-site phosphorylation inhibitors through target verification and in vivo anti-tumor activity studies, providing new ideas
for the development of the next generation of STAT3 inhibitors.
Figure 6.
Figure 7.
The article features Researcher Chen Yihua and Researcher Yi Zhengfang of East China Normal University as co-corresponding authors, He Peng and doctoral student Miao Ying of East China Normal University as co-authors, and the research is strongly supported
by Professor Liu Mingyao of East China Normal University.
Original link: https://pubs.
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