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通过设计合理的小分子抑制剂靶向 Janus 激酶 3 预防结直肠癌。

Chemoprevention of colorectal cancer by targeting Janus kinase 3 with a rationally designed small molecule inhibitor.

机构信息

Division of Hematology-Oncology, Department of Pediatrics, University of Southern California Keck School of Medicine, Children's Hospital Los Angeles, Los Angeles, CA, USA.

出版信息

Nutr Cancer. 2010;62(7):968-72. doi: 10.1080/01635581.2010.513471.

Abstract

The effects of the rationally designed JAK3 inhibitor JANEX-1 on the development of intestinal tumors in the APC(min) mouse model of familial adenomatous polyposis were examined. At a non-toxic dose level, >4 times lower than its day 30 LD(10), JANEX-1 was highly effective in preventing intestinal tumor development in Min mice, resulting in markedly improved survival outcomes. JAK3 inhibitors may, therefore, be useful in the chemoprevention of colorectal cancer. Here, an overview regarding the potential of JANEX-1 as a chemopreventive agent is provided.

摘要

研究了合理设计的 JAK3 抑制剂 JANEX-1 对家族性腺瘤性息肉病 APC(min)小鼠模型中肠道肿瘤发展的影响。在非毒性剂量水平下,JANEX-1 比其第 30 天 LD(10)高 4 倍以上,可有效预防 Min 小鼠的肠道肿瘤发生,显著改善生存结果。因此,JAK3 抑制剂可能对结直肠癌的化学预防有用。本文提供了 JANEX-1 作为化学预防剂的潜力概述。

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