去氯伐替尼诱导人胶质母细胞瘤细胞中 YAP1 的蛋白酶体降解

IF 1.7 4区化学 Q3 CHEMISTRY, ORGANIC

Synlett Pub Date : 2024-05-22 DOI:10.1055/a-2331-6463

Shaonan Wang, Min Sun, Yajuan Su, Zhou Xu, Ang Li, Weiwei He

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引用次数: 0

摘要

Deucravacitinib 是酪氨酸激酶 2 (TYK2) 的一种选择性异位抑制剂，最近被美国食品及药物管理局批准用于治疗斑块型银屑病。我们发现，这种化合物能诱导人胶质母细胞瘤（GBM）细胞（U-87 MG）中希波信号通路下游效应因子 YAP1 蛋白质体降解。这种降解独立于典型的 Hippo 通路，为 YAP1 的替代调控机制提供了线索。

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Deucravacitinib Induces Proteasomal Degradation of YAP1 in Human Glioblastoma Cells

Deucravacitinib is a selective allosteric inhibitor of tyrosine kinase 2 (TYK2) recently approved by the FDA for the treatment of plaque psoriasis. We discovered that this compound induces proteasomal degradation of YAP1, the downstream effector of the Hippo signaling pathway, in human glioblastoma (GBM) cells (U-87 MG). This degradation is independent of the canonical Hippo pathway, which offers clues to alternative mechanisms for YAP1 regulation.

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来源期刊

Synlett 化学-有机化学

CiteScore

3.40

自引率

5.00%

发文量

369

审稿时长

1 months

期刊介绍： SYNLETT is an international journal reporting research results and current trends in chemical synthesis in short personalized reviews and preliminary communications. It covers all fields of scientific endeavor that involve organic synthesis, including catalysis, organometallic, medicinal, biological, and photochemistry, but also related disciplines and offers the possibility to publish scientific primary data.