More sensitive and specific methods for early detection are imperative to improve survival rates in oral cancer. However, oral cancer detection is still largely based on visual examination and histopathology of biopsy material, offering no molecular selectivity or spatial resolution. Intuitively, the addition of optical contrast could improve oral cancer detection and delineation, but so far no molecularly targeted approach has been translated. Our fluorescently labeled small-molecule inhibitor PARPi-FL binds to the DNA repair enzyme poly(ADP-ribose)polymerase 1 (PARP1) and is a potential diagnostic aid for oral cancer delineation. Based on our preclinical work, a clinical phase I/II trial opened in March 2017 to evaluate PARPi-FL as a contrast agent for oral cancer imaging. In this commentary, we discuss why we chose PARP1 as a biomarker for tumor detection and which particular characteristics make PARPi-FL an excellent candidate to image PARP1 in optically guided applications. We also comment on the potential benefits of our molecularly targeted PARPi-FL-guided imaging approach in comparison to existing oral cancer screening adjuncts and mention the adaptability of PARPi-FL imaging to other environments and tumor types.

中文翻译：

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使用PARP1靶向光学成像剂检测和描绘口腔癌。

必须采用更灵敏，更具体的早期检测方法来提高口腔癌的生存率。但是，口腔癌的检测仍主要基于活检材料的视觉检查和组织病理学，没有分子选择性或空间分辨率。直观上，增加光学对比可以改善口腔癌的检测和轮廓，但是到目前为止，还没有翻译出分子靶向的方法。我们的荧光标记小分子抑制剂PARPi-FL与DNA修复酶聚（ADP-核糖）聚合酶1（PARP1）结合，是口腔癌勾画的潜在诊断工具。根据我们的临床前工作，于2017年3月启动了一项I / II期临床试验，以评估PARPi-FL作为口腔癌成像的造影剂。在这篇评论中 我们讨论了为什么我们选择PARP1作为肿瘤检测的生物标志物，以及哪些特殊特性使PARPi-FL成为在光导应用中成像PARP1的极佳候选者。与现有的口腔癌筛查辅助工具相比，我们还对我们的分子靶向PARPi-FL引导成像方法的潜在优势进行了评论，并提及PARPi-FL成像对其他环境和肿瘤类型的适应性。