医学
放射治疗
效应器
前药
限制
癌症研究
缺氧(环境)
癌症
肿瘤科
肿瘤缺氧
内科学
提拉帕扎明
药理学
化疗
细胞毒性
氧气
免疫学
化学
生物化学
体外
机械工程
有机化学
工程类
标识
DOI:10.1016/s1470-2045(00)00006-1
摘要
Tumour hypoxia, a deficiency of oxygen due to an inefficient vasculature, is a limiting factor in both the radiotherapy and chemotherapy of solid tumours. Paradoxically, it is also an attractive therapeutic target, because severe hypoxia occurs only in solid tumour tissue. Hypoxic cells can be exploited for therapy by non-toxic, hypoxia-activated prodrugs. Conceptually, 'trigger' units in these drugs are selectively activated in hypoxic cells to release or activate a toxic 'effector', capable of killing surrounding oxygenated tumour cells. Useful triggers include nitroaromatics, quinones, N-oxides, and transition metals. The N-oxide tirapazamine is in phase III clinical trials.
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