A Fluorescent Benzo[g]isoquinoline-based HIF Prolyl Hydroxylase Inhibitor for Cellular Imaging.
Mayer M, Fey K, Heinze E, Wick C, Abboud MI, Yeh TL, Tumber A, Orth N, Schley G, Buchholz B, Clark T, Schofield CJ, Willam C, Burzlaff N (2018)
Publication Status: Published
Publication Type: Journal article
Publication year: 2018
Journal
Book Volume: 14
Pages Range: 94-99
Journal Issue: 1
Abstract
Prolyl hydroxylation domain enzymes (PHD) 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 fluorescent 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.
Authors with CRIS profile
Marleen Mayer
Professur für Anorganische Chemie
Kerstin Fey
Department of Medicine 4 – Nephrology and Hypertension
Eva Waidmann
Lehrstuhl für Anorganische und Metallorganische Chemie
Christian Wick
Computer-Chemie-Centrum
Nicole Orth
Lehrstuhl für Bioanorganische Chemie
Björn Buchholz
Department of Medicine 4 – Nephrology and Hypertension
Timothy Clark
Computer-Chemie-Centrum
Carsten Willam
Department of Medicine 4 – Nephrology and Hypertension
Nicolai Burzlaff
Professur für Anorganische Chemie
Involved external institutions
United Kingdom (GB)How to cite
APA:
Mayer, M., Fey, K., Heinze, E., Wick, C., Abboud, M.I., Yeh, T.L.,... Burzlaff, N. (2018). A Fluorescent Benzo[g]isoquinoline-based HIF Prolyl Hydroxylase Inhibitor for Cellular Imaging. ChemMedChem, 14(1), 94-99. https://dx.doi.org/10.1002/cmdc.201800483
MLA:
Mayer, Marleen, et al. "A Fluorescent Benzo[g]isoquinoline-based HIF Prolyl Hydroxylase Inhibitor for Cellular Imaging." ChemMedChem 14.1 (2018): 94-99.
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