A Fluorescent Benzo[g]isoquinoline-based HIF Prolyl Hydroxylase Inhibitor for Cellular Imaging.

Journal article


Publication Details

Author(s): 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
Journal: Chemmedchem
Publication year: 2018
ISSN: 1860-7179


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.


FAU Authors / FAU Editors

Burzlaff, Nicolai Prof. Dr.
Professur für Anorganische Chemie
Clark, Timothy apl. Prof. Dr.
Computer-Chemie-Centrum
Fey, Kerstin
Medizinische Klinik 4 - Nephrologie und Hypertensiologie
Waidmann, Eva
Lehrstuhl für Anorganische und Metallorganische Chemie
Mayer, Marleen
Professur für Anorganische Chemie
Orth, Nicole
Lehrstuhl für Bioanorganische Chemie
Wick, Christian Dr.
Computer-Chemie-Centrum
Willam, Carsten Prof. Dr.
Medizinische Klinik 4 - Nephrologie und Hypertensiologie


External institutions with authors

University of Oxford


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. 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 (2018).

BibTeX: 

Last updated on 2019-20-07 at 07:22

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