Article
Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition.
BMC cancer - 21 May 2015
Meng Fanying, Bhupathi Deepthi, Sun Jessica D, Liu Qian, Ahluwalia Dharmendra, Wang Yan, Matteucci Mark D, Hart Charles P
Abstract excerpt
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. METHODS: We employed in vitro cell viability, DNA damage, cellular signaling assays and the in vivo HT29 human tumor...
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