Journal article
A fluorescent benzo[g]isoquinoline-based HIF prolyl hydroxylase inhibitor for cellular imaging
- Abstract:
- 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.
- Publication status:
- Published
- Peer review status:
- Peer reviewed
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- Files:
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(Preview, Accepted manuscript, pdf, 1.8MB, Terms of use)
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- Publisher copy:
- 10.1002/cmdc.201800483
Authors
+ Cancer Research UK
More from this funder
- Funding agency for:
- Abboud, M
- Schofield, C
- Grant:
- 18245
- 18245
+ Wellcome Trust
More from this funder
- Funding agency for:
- Abboud, M
- Schofield, C
- Grant:
- 18245
- 18245
- Publisher:
- Wiley
- Journal:
- ChemMedChem More from this journal
- Volume:
- 14
- Issue:
- 1
- Pages:
- 94-99
- Publication date:
- 2018-12-21
- Acceptance date:
- 2018-10-26
- DOI:
- EISSN:
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1860-7187
- ISSN:
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1860-7179
- Keywords:
- Pubs id:
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pubs:935986
- UUID:
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uuid:09c12867-94e2-435e-b6b3-79cae589126b
- Local pid:
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pubs:935986
- Source identifiers:
-
935986
- Deposit date:
-
2018-11-01
Terms of use
- Copyright holder:
- Wiley‐VCH Verlag GmbH and Co
- Copyright date:
- 2018
- Notes:
- Copyright © 2018 Wiley‐VCH Verlag GmbH and Co. KGaA, Weinheim. This is the accepted manuscript version of the article. The final version is available online from Wiley at: https://doi.org/10.1002/cmdc.201800483
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