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血红素，一种酪蛋白激酶 II 抑制剂，可抑制小鼠异种移植模型中的肺癌肿瘤生长。

Hematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograft model.

机构信息

Thoracic Oncology Laboratory, Department of Surgery, Comprehensive Cancer Center, University of California, San Francisco, CA 94115, USA.

出版信息

Int J Oncol. 2013 Nov;43(5):1517-22. doi: 10.3892/ijo.2013.2087. Epub 2013 Sep 4.

DOI:10.3892/ijo.2013.2087
PMID:24008396
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3823374/
Abstract

Casein kinase II (CK2) inhibitors suppress cancer cell growth. In this study, we examined the inhibitory effects of a novel CK2 inhibitor, hematein, on tumor growth in a murine xenograft model. We found that in lung cancer cells, hematein inhibited cancer cell growth, Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increased apoptosis. In a murine xenograft model of lung cancer, hematein inhibited tumor growth without significant toxicity to the mice tested. Molecular docking showed that hematein binds to CK2α in durable binding sites. Collectively, our results suggest that hematein is an allosteric inhibitor of protein kinase CK2 and has antitumor activity to lung cancer.

摘要

酪蛋白激酶 2（CK2）抑制剂抑制癌细胞生长。在这项研究中，我们研究了一种新型 CK2 抑制剂血褐素对荷瘤鼠模型中肿瘤生长的抑制作用。我们发现，在肺癌细胞中，血褐素抑制癌细胞生长，抑制 Akt/PKB Ser129 磷酸化，抑制 Wnt/TCF 通路并促进细胞凋亡。在肺癌的荷瘤鼠模型中，血褐素抑制肿瘤生长，而对实验小鼠无明显毒性。分子对接显示血褐素与 CK2α 在持久结合位点结合。综上所述，我们的研究结果表明血褐素是蛋白激酶 CK2 的别构抑制剂，对肺癌具有抗肿瘤活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/3016b1d418e3/IJO-43-05-1517-g04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/8a79509094fb/IJO-43-05-1517-g00.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/4b69060617bb/IJO-43-05-1517-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/7cc785694324/IJO-43-05-1517-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/53c4ae870bd6/IJO-43-05-1517-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/3016b1d418e3/IJO-43-05-1517-g04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/8a79509094fb/IJO-43-05-1517-g00.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/4b69060617bb/IJO-43-05-1517-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/7cc785694324/IJO-43-05-1517-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/53c4ae870bd6/IJO-43-05-1517-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab53/3823374/3016b1d418e3/IJO-43-05-1517-g04.jpg

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