受天然产物启发的荧光探针用于肿瘤组织中 NQO1 活性的成像。
Natural product-inspired profluorophores for imaging NQO1 activity in tumour tissues.
机构信息
Centre for Inflammation Research, The University of Edinburgh, EH16 4TJ Edinburgh, UK.
Institute of Exact Sciences, Department of Chemistry, Federal University of Minas Gerais, Belo Horizonte 31270-901, MG, Brazil.
出版信息
Bioorg Med Chem. 2019 Sep 1;27(17):3938-3946. doi: 10.1016/j.bmc.2019.07.017. Epub 2019 Jul 15.
Herein we designed a collection of trimethyl-lock quinone profluorophores as activity-based probes for imaging NAD(P)H:quinone oxidoreductase (NQO1) in cancer cells and tumour tissues. Profluorophores were prepared via synthetic routes from naturally-occurring quinones and characterised in vitro using recombinant enzymes, to be further validated in cells and fresh frozen canine tumour tissues as potential new tools for cancer detection and imaging.
在这里，我们设计了一系列三甲基锁醌类荧光探针作为基于活性的探针，用于在癌细胞和肿瘤组织中成像 NAD(P)H:醌氧化还原酶 (NQO1)。荧光探针是通过天然醌类化合物的合成路线制备的，并使用重组酶进行了体外表征，进一步在细胞和新鲜冷冻的犬肿瘤组织中进行了验证，作为癌症检测和成像的潜在新工具。
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