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BI_2536——靶向有丝分裂激酶Polo样激酶1(Plk1)。

BI_2536--targeting the mitotic kinase Polo-like kinase 1 (Plk1).

作者信息

Wäsch R, Hasskarl J, Schnerch D, Lübbert M

机构信息

Department of Hematology and Oncology, Freiburg University Medical Center, Hugstetterstrasse 55, 79106, Freiburg, Germany.

出版信息

Recent Results Cancer Res. 2010;184:215-8. doi: 10.1007/978-3-642-01222-8_15.

Abstract

Human Polo-like kinase 1 (Plk1) is an essential regulator of mitotic progression. Targeted inhibition of this kinase was effective in killing tumor cells in vitro and in vivo. The Plk1 inhibitor BI_2536 was well tolerated and showed antitumor activity in the first clinical trials enrolling patients with advanced solid tumors and refractory or relapsed acute myeloid leukemia.

摘要

人类Polo样激酶1(Plk1)是有丝分裂进程的重要调节因子。对该激酶的靶向抑制在体外和体内杀死肿瘤细胞方面均有效。Plk1抑制剂BI_2536耐受性良好,并且在首批纳入晚期实体瘤以及难治性或复发性急性髓系白血病患者的临床试验中显示出抗肿瘤活性。

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