Identification of chemical compounds regulating PD‐L1 by introducing HiBiT‐tagged cells,FEBS Letters

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Identification of chemical compounds regulating PD‐L1 by introducing HiBiT‐tagged cells
FEBS Letters ( IF 3.0 ) Pub Date : 2021-01-20 , DOI: 10.1002/1873-3468.14032
Yutaro Uchida ₁ , Takahide Matsushima ₁ , Ryota Kurimoto ₁ , Tomoki Chiba ₁ , Yuki Inutani ₁ , Hiroshi Asahara _{1,

2}

Affiliation

Programmed death-ligand 1 (PD-L1) is a co-inhibitory molecule expressed on tumor cells. Immune checkpoint inhibitors focusing on the PD-L1 mechanism are now being studied for the treatment of various cancer types. However, the regulatory mechanism of PD-L1 is yet to be fully clarified, and a high-throughput system for comparing the abilities of small compounds in regulating PD-L1 has not yet been established. Therefore, we created a HiBiT-tagged lung adenocarcinoma cell line, PC9-KI, for easier and faster detection of changes in PD-L1 protein expression. Using PC9-KI cells, we screened 1,280 chemical compounds from the Library of Pharmacologically Active Compounds (LOPAC) and identified microtubule polymerization inhibitors and thapsigargin as PD-L1 upregulators and a p97 inhibitor as a PD-L1 downregulator.

中文翻译：

通过引入 HiBiT 标记的细胞鉴定调节 PD-L1 的化合物

程序性死亡配体 1 (PD-L1) 是一种在肿瘤细胞上表达的共抑制分子。专注于 PD-L1 机制的免疫检查点抑制剂目前正在研究用于治疗各种癌症类型。然而，PD-L1的调控机制尚未完全阐明，用于比较小分子化合物对PD-L1的调控能力的高通量体系尚未建立。因此，我们创建了一个带有 HiBiT 标记的肺腺癌细胞系 PC9-KI，以便更轻松、更快速地检测 PD-L1 蛋白表达的变化。使用 PC9-KI 细胞，我们从药理活性化合物库 (LOPAC) 中筛选了 1,280 种化合物，并确定了微管聚合抑制剂和毒胡萝卜素作为 PD-L1 上调剂和 p97 抑制剂作为 PD-L1 下调剂。

更新日期：2021-01-20

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