Identification of benzo[b]thiophene-1,1-dioxide derivatives as novel PHGDH covalent inhibitors

[Display omitted] •The benzo[b]thiophene-1,1-dioxide derivative B12 was identified as a novel covalent inhibitor of PHGDH.•B12 has potential PHGDH inhibitory activity and anti-proliferative activities against PHGDH overexpression cancer cell lines.•B12 was shown to inhibit de novo serine synthesis i...

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Veröffentlicht in:Bioorganic chemistry 2024-05, Vol.146, p.107330-107330, Article 107330
Hauptverfasser: Cao, Xin-Yu, Li, Xinge, Wang, Feng, Duan, Yichen, Wu, Xingmei, Lin, Guo-Qiang, Geng, Meiyu, Huang, Min, Tian, Ping, Tang, Shuai, Gao, Dingding
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Sprache:eng
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