Poly(ADP-ribose)polymerase (PARP) inhibition and anticancer activity of simmiparib, a new inhibitor undergoing clinical trials

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• 作者：Bo Yuan^a ; ^b ; ¹ ; Na Ye^b ; ^c ; ¹ ; Shan-Shan Song^a ; ^b ; Yu-Ting Wang^a ; ^b ; Zilan Song^b ; ^c ; Hua-Dong Chen^a ; ^b ; Chuan-Huizi Chen^a ; ^b ; Xia-Juan Huan^a ; ^b ; Ying-Qing Wang^a ; ^b ; Yi Su^a ; ^b ; Yan-Yan Shen^a ; ^b ; Yi-Ming Sun^a ; ^b ; Xin-Ying Yang^a ; ^b ; Yi Chen^a ; ^b ; Shi-Yan Guo^d ; Yong Gan^d ; Zhi-Wei Gao^d ; Xiao-Yan Chen^d ; Jian Ding^a ; ^b ; Jin-Xue He^a ; ^b ; ^{jxhe@simm.ac.cn} ; Ao Zhang^b ; ^c ; ^{aozhang@simm.ac.cn} ; Ze-Hong Miao^a ; ^b ; ^{zhmiao@simm.ac.cn}
• 关键词：Homologous recombination repair defects ; Olaparib ; Growth inhibition ; Patient-derived xenografts ; Pharmacokinetics
• 刊名：Cancer Letters
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：386
• 期：Complete
• 页码：47-56
• 全文大小：3327 K
• 卷排序：386

文摘

Simmiparib potently inhibits PARP 1/2 and traps PARP 1-DNA complexes. Simmiparib induces DSB accumulation and G2/M arrest in HR-deficient cells. Simmiparib selectively induces apoptosis in HR-deficient cells. Simmiparib exhibits remarkable anticancer activities both in vitro and in vivo. Simmiparib sensitizes HR-proficient cancer cells to anticancer drugs.