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Structural and mechanistic studies on the inhibition of the hypoxia-inducible transcription factor hydroxylases by tricarboxylic acid cycle intermediates.

Abstract:

In humans both the levels and activity of the alpha-subunit of the hypoxia-inducible transcription factor (HIF-alpha) are regulated by its post-translation hydroxylation as catalyzed by iron- and 2-oxoglutarate (2OG)-dependent prolyl and asparaginyl hydroxylases (PHD1-3 and factor-inhibiting HIF (FIH), respectively). One consequence of hypoxia is the accumulation of tricarboxylic acid cycle intermediates (TCAIs). In vitro assays were used to assess non-2OG TCAIs as inhibitors of purified PHD2...

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Publication status:
Published

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Publisher copy:
10.1074/jbc.m608337200

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Journal:
Journal of biological chemistry More from this journal
Volume:
282
Issue:
5
Pages:
3293-3301
Publication date:
2007-02-01
DOI:
EISSN:
1083-351X
ISSN:
0021-9258
Language:
English
Keywords:
Pubs id:
pubs:33684
UUID:
uuid:09d28232-edab-450f-a5ba-785662b0a990
Local pid:
pubs:33684
Source identifiers:
33684
Deposit date:
2012-12-19

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