Department of Chemistry, Manipal Institute of Technology, Manipal Academy of Higher Education, Manipal 576 104, Karnataka, India.
Department of Chemistry, Manipal Institute of Technology, Manipal Academy of Higher Education, Manipal 576 104, Karnataka, India.
Bioorg Chem. 2019 Jul;88:102979. doi: 10.1016/j.bioorg.2019.102979. Epub 2019 May 8.
Hypoxia is a distinctive characteristic of advanced solid malignancies that results from a disparity between oxygen supply and its consumption. The degree of hypoxia is believed to have adverse prognostic significance. Therefore detecting cellular hypoxia can potentially offer insights into the grade of tumour as well as its evolution towards a progressive malignant phenotype, which clinically translates to greater metastatic potential and treatment resistance. Fluorescence imaging to visualize hypoxia in biological systems is a minimally-invasive method. Recently there are several reports on interdisciplinary research that aims at developing functional probes that can be efficiently used for non-invasive imaging of hypoxic tumours. Upregulated levels of nitroreductase (NTR) is detected in hypoxic solid malignancies, and this characteristic feature is increasingly utilized in the development of NTR-targeted fluorescent molecules to selectively sense hypoxia in vivo. The present review summarizes various reports published on the design concepts of nitro naphthalimide-based bio-reductive fluorescent sensors that can be applied noninvasively to image hypoxia in cancer.
缺氧是高级实体恶性肿瘤的一个显著特征,是由氧气供应和消耗之间的差异造成的。缺氧程度被认为具有不良的预后意义。因此,检测细胞缺氧可能有助于了解肿瘤的分级及其向进行性恶性表型的演变,这在临床上意味着更大的转移潜力和治疗抵抗。荧光成像是一种用于可视化生物系统中缺氧的微创方法。最近有一些关于跨学科研究的报道,旨在开发功能探针,这些探针可有效地用于无创性成像缺氧肿瘤。在缺氧的实体恶性肿瘤中检测到硝基还原酶 (NTR) 的上调水平,这一特征特征越来越多地用于开发针对 NTR 的荧光分子,以选择性地在体内感知缺氧。本综述总结了各种关于基于硝基萘二甲酰亚胺的生物还原荧光传感器的设计概念的报道,这些传感器可用于非侵入性地成像癌症中的缺氧。