Prolyl hydroxylation domain (PHD) enzymes catalyze the hydroxylation of the transcription factor hypoxia-inducible factor (HIF) and serve as cellular oxygen sensors. HIF and the PHD enzymes regulate numerous potentially tissue-protective target genes which can adapt cells to metabolic and ischemic stress. We describe a fluorescent PHD inhibitor (1-chloro-4-hydroxybenzo[g]isoquinoline-3-carbonyl)glycine which is suited to fluorescence-based detection assays and for monitoring PHD inhibitors in biological systems. In cell-based assays, application of the fluorescent PHD inhibitor allowed co-localization with a cellular PHD enzyme and led to live cell imaging of processes involved in cellular oxygen sensing.

中文翻译：

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一种基于荧光苯并[g]异喹啉的HIF脯氨酰羟化酶抑制剂，用于细胞成像。

脯氨酰羟化域（PHD）酶催化转录因子缺氧诱导因子（HIF）的羟化作用，并用作细胞氧传感器。HIF和PHD酶调节着许多潜在的组织保护性靶基因，这些基因可以使细胞适应新陈代谢和缺血性应激。我们描述了一种荧光PHD抑制剂（1-氯-4-羟基苯并[g]异喹啉-3-羰基）甘氨酸，适用于基于荧光的检测方法和监测生物系统中的PHD抑制剂。在基于细胞的测定中，荧光PHD抑制剂的应用允许与细胞PHD酶共定位，并导致涉及细胞氧传感的过程的活细胞成像。