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

ChemMedChem Wiley

Book Volume: 14

Pages Range: 94-99

Journal Issue: 1

DOI: 10.1002/cmdc.201800483

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

University of Oxford GB 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://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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