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替凡替尼(ARQ - 197)在口腔鳞状细胞癌中具有抗肿瘤活性,并能下调黏着斑激酶(FAK)。

Tivantinib (ARQ-197) exhibits anti-tumor activity with down-regulation of FAK in oral squamous cell carcinoma.

作者信息

Xi Wei-Hong, Yang Li-Yun, Cao Zhong-Yi, Qian Yong

机构信息

Department of Oral and Maxillofacial Surgery, First Affiliated Hospital, Nanchang University, Nanchang 330006, China.

Department of Blood Transfusion, First Affiliated Hospital, Nanchang University, Nanchang 330006, China.

出版信息

Biochem Biophys Res Commun. 2015 Feb 20;457(4):723-9. doi: 10.1016/j.bbrc.2015.01.062. Epub 2015 Jan 24.

DOI:10.1016/j.bbrc.2015.01.062
PMID:25623532
Abstract

Oral squamous cell carcinoma (OSCC) is one of the most common cancers worldwide and the 5 years survival rate of the patients is about 60% in the USA, due to acquired chemotherapeutic resistance and metastasis of the disease. In this study, we found that tivantinib, a selective MET inhibitor, suppresses OCSS cell proliferation and colony formation, however, anti-tumor activities induced by tivantinib are independent of the inhibition of MET signaling pathway. In addition, tivantinib cause G2/M cell cycle arrest and caspases-dependent apoptosis in OSCC cell lines. We also found that tivantinib dose-dependently suppressed the activation and expression of FAK. In all, these data suggested that tivantinib may be developed as a chemotherapeutic agent to effectively treat certain cancers including OSCC.

摘要

口腔鳞状细胞癌(OSCC)是全球最常见的癌症之一,在美国,由于疾病获得性化疗耐药和转移,患者的5年生存率约为60%。在本研究中,我们发现选择性MET抑制剂替万替尼可抑制OSCC细胞增殖和集落形成,然而,替万替尼诱导的抗肿瘤活性与MET信号通路的抑制无关。此外,替万替尼可导致OSCC细胞系发生G2/M期细胞周期阻滞和半胱天冬酶依赖性凋亡。我们还发现替万替尼剂量依赖性地抑制FAK的激活和表达。总之,这些数据表明,替万替尼可能被开发为一种化疗药物,以有效治疗包括OSCC在内的某些癌症。

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Tivantinib (ARQ-197) exhibits anti-tumor activity with down-regulation of FAK in oral squamous cell carcinoma.替凡替尼(ARQ - 197)在口腔鳞状细胞癌中具有抗肿瘤活性,并能下调黏着斑激酶(FAK)。
Biochem Biophys Res Commun. 2015 Feb 20;457(4):723-9. doi: 10.1016/j.bbrc.2015.01.062. Epub 2015 Jan 24.
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