Small molecule inhibition of polo-like kinase 1 by volasertib (BI 6727) causes significant melanoma growth delay and regression in vivo

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• 作者：Brian D. Cholewa^a ; Mary A. Ndiaye^a ; Wei Huang^b ; Xiaoqi Liu^c ; Nihal Ahmad^a ; ^d ; ^{nahmad@wisc.edu}
• 关键词：Melanoma ; Plk1 ; BI 6727 ; Volasertib
• 刊名：Cancer Letters
• 出版年：2017
• 出版时间：28 January 2017
• 年：2017
• 卷：385
• 期：Complete
• 页码：179-187
• 全文大小：1867 K
• 卷排序：385

文摘

Plk1 is overexpressed in clinical melanoma samples compared to benign nevi. Plk1 inhibition by BI 6727 has anti-proliferative effects in human melanoma cells. Plk1 inhibition by BI 6727 causes G2/M & S-phase cell cycle arrests in vitro. BI 6727 treatment significantly delays melanoma growth & causes regression in vivo. Anti-melanoma effects of BI 6727 are accompanied by an increase of p53 activity.