Mcl-1 Inhibitor Suppresses Tumor Growth of Esophageal Squamous Cell Carcinoma in a Mouse Model

Jianqing Lin, Deqiang Fu, Yijun Dai, Jianguang Lin, Tianwen Xu

Oncotarget. 2017 Jun 28;8(70):114457-114462.

PMID: 29383093

Abstract:

Esophageal squamous cell carcinoma (ESCC) has a high morbidity in China, accounting for 90% of all esophageal carcinoma cases. Hence, identifying drug targets for prevention and treatment of ESCC is essential. Due to its critical role in the regulation of cell apoptosis, Mcl-1 holds great potential as a target for treatment against ESCC. In current study, we used a 4-nitroquinoline-1-oxide (4-NQO)-induced ESCC mouse model of test whether A-1210477, a Mcl-1 small molecular inhibitor, could repress ESCC development. We showed that A-1210477 treatment decreased ESCC formation and animal weight loss in a dose dependent manner. We detected decreased cellular proliferation in A-1210477-treated ESCC tissue by Ki67 expression. Moreover, A-1210477 treatment increased the number of apoptotic cells in ESCC tissues. Our study clearly demonstrates the contribution of Mcl-1 to ESCC development through promoting cell proliferation and inhibition of apoptosis, and provides a strong evidence for further evaluation of A-1210477 for treating ESCC.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1668553261 A-1210477 A-1210477 1668553-26-1 Price
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