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This approach, although very attractive, has not been feasible for treating brain tumours due to the stringent structural features necessary for pharmaceutical agents to cross the blood\u2013brain barrier (BBB). This study presents the proof of concept in vitro cellular activity of PARP1 (Poly(ADP\u2010ribose) polymerase 1) enzyme inhibitor olaparib conjugated with a known BBB\u2010crossing heptamethine cyanine dye. 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