Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition

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• 作者：Fanying Meng ; Deepthi Bhupathi ; Jessica D Sun ; Qian Liu ; Dharmendra Ahluwalia…
• 关键词：Cancer ; Hypoxia ; Chk1 inhibitor ; Hypoxia ; activated prodrug ; DNA damage ; DNA repair ; in vitro cytotoxicity ; in vivo anti ; tumor activity ; Xenograft models
• 刊名：BMC Cancer
• 出版年：2015
• 出版时间：December 2015
• 年：2015
• 卷：15
• 期：1
• 全文大小：4,100 KB
• 刊物主题：Cancer Research; Oncology; Stem Cells; Animal Models; Internal Medicine;
• 出版者：BioMed Central
• ISSN：1471-2407

文摘

Background The hypoxia-activated prodrug TH-302 is reduced at its nitroimidazole group and selectively under hypoxic conditions releases the DNA cross-linker bromo-isophosphoramide mustard (Br-IPM). Here, we have explored the effect of Chk1 inhibition on TH-302-mediated pharmacological activities.