Selective ERK inhibitor ulixertinib inhibits proliferation and induces apoptosis in lymphoma cell lines

作者：Ding, Wan-Jun^*; Tao, Wei-Ping; Zeng, Tao; Deng, Jun-Jian; Lei, Hong-Bo; Ge, Wei

来源：International Journal of Clinical and Experimental Medicine, 2016, 9(6): 10955-10962.

• Lymphoma
• ulixertinib
• ERK1/2
• proliferation
• apoptosis

Aberrant MAPK pathway signaling and resultant ERK kinase activity is evident in many oncogene-dependent cancers and the intrinsic and acquired drug resistance is often associated with activated ERK signaling. Here, we reported ulixertinib, an ERK1/2 kinase inhibitor, potently and selectively inhibits ERK1 and ERK2 kinases in a reversible, ATP-competitive fashion. Consistent with its mechanism of action, ulixertinib inhibited ERK1/2 activation and cell proliferation, and induced cell cycle arrest and apoptosis in human lymphoma cell lines SUDHL-10 and Raji cells. Furthermore, the expression of VEGFA, VEGFR2 and Bcl-2 was significantly decreased in SUDHL-10 and Raji cells treated with ulixertinib, but the expression of Bax and caspase-3 was notably increased. In total, in vitro studies will help elucidate how ulixertinib may be used as a novel agent in therapeutic strategies for human lymphoma.

• 出版日期2016
• 单位武汉大学