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HASPIN抑制剂CHR-6494对BxPC-3-Luc（一种表达荧光素酶的胰腺癌细胞系）的抑制作用。

Inhibitory Effect of the HASPIN Inhibitor CHR-6494 on BxPC-3-Luc, A Luciferase-Expressing Pancreatic Cancer Cell Line.

作者信息

Tanaka Hiromitsu, Nishida-Fukuda Hisayo, Wada Morimasa, Tokuhiro Keizo, Matsushita Hiroaki, Ando Yukio

机构信息

Faculty of Pharmaceutical Sciences, Nagasaki International University, Huis Ten Bosch, Sasebo, Nagasaki, Japan. Email:

Department of Genome Editing, Institute of Biomedical Science, Kansai Medical University, Shin-machi, Hirakata City, Osaka, Japan.

出版信息

Cell J. 2022 Apr;24(4):212-214. doi: 10.22074/cellj.2022.7796. Epub 2022 Apr 27.

DOI:10.22074/cellj.2022.7796
PMID:35674022
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9124445/
Abstract

HASPIN acts in chromosome segregation via histone phosphorylation. Recently, HASPIN inhibitors have been shown to suppress growth of various cancer cells. Pancreatic cancer has no symptom in the early stages and may progress before detection. So, the 5-year survival rate is low. Here, we reported that administration of the HASPIN inhibitor, CHR-6494, to mice bearing pancreatic BxPC-3-Luc cancer cells significantly suppressed growth of BxPC-3-Luc cells. CHR-6494 might be a useful agent for treating pancreatic cancer.

摘要

HASPIN通过组蛋白磷酸化作用于染色体分离。最近，HASPIN抑制剂已被证明可抑制多种癌细胞的生长。胰腺癌在早期没有症状，可能在被发现之前就已进展。因此，其5年生存率较低。在此，我们报道了给携带胰腺BxPC-3-Luc癌细胞的小鼠施用HASPIN抑制剂CHR-6494可显著抑制BxPC-3-Luc细胞的生长。CHR-6494可能是一种治疗胰腺癌的有效药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3192/9124445/b30bc7bdfb34/Cell-J-24-212-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3192/9124445/e14f08b9b527/Cell-J-24-212-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3192/9124445/56f3b10622e9/Cell-J-24-212-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3192/9124445/b30bc7bdfb34/Cell-J-24-212-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3192/9124445/e14f08b9b527/Cell-J-24-212-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3192/9124445/56f3b10622e9/Cell-J-24-212-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3192/9124445/b30bc7bdfb34/Cell-J-24-212-g03.jpg

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本文引用的文献

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Cancer Res. 2020 Feb 15;80(4):798-810. doi: 10.1158/0008-5472.CAN-19-2330. Epub 2019 Dec 27.
2
HASPIN kinase inhibitor CHR-6494 suppresses intestinal polyp development, cachexia, and hypogonadism in Apcmin/+ mice.HASPIN 激酶抑制剂 CHR-6494 抑制 Apcmin/+ 小鼠的肠道息肉发育、恶病质和性腺功能减退。
Eur J Cancer Prev. 2020 Nov;29(6):481-485. doi: 10.1097/CEJ.0000000000000562.
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Sangivamycin and its derivatives inhibit Haspin-Histone H3-survivin signaling and induce pancreatic cancer cell death.
桑吉霉素及其衍生物抑制 Haspin-Histone H3-survivin 信号通路并诱导胰腺癌细胞死亡。
Sci Rep. 2019 Nov 12;9(1):16588. doi: 10.1038/s41598-019-53223-0.
4
Current Clinical Strategies of Pancreatic Cancer Treatment and Open Molecular Questions.当前胰腺癌治疗的临床策略和未解决的分子问题。
Int J Mol Sci. 2019 Sep 13;20(18):4543. doi: 10.3390/ijms20184543.
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Haspin knockdown can inhibit progression and development of pancreatic cancer in vitro and vivo.组蛋白去乙酰化酶 6 抑制剂抑制胰腺癌细胞的体外和体内生长
Exp Cell Res. 2019 Dec 1;385(1):111605. doi: 10.1016/j.yexcr.2019.111605. Epub 2019 Sep 4.
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Bioorg Chem. 2018 Aug;78:418-426. doi: 10.1016/j.bioorg.2018.03.031. Epub 2018 Apr 17.
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