A fluorescent benzo[g]isoquinoline-based HIF prolyl hydroxylase inhibitor for cellular imaging

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 s...

全面介紹

書目詳細資料
Main Authors: Mayer, M, Fey, K, Heinze, E, Rainer Wick, C, Abboud, M, Yeh, T, Tumber, A, Orth, N, Schley, G, Buchholz, B, Clark, T, Schofield, C, Willam, C, Burzlaff, N
格式: Journal article
出版: Wiley 2018
實物特徵
總結: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.