1.14.11.30: hypoxia-inducible factor-asparagine dioxygenase

This is an abbreviated version!
For detailed information about hypoxia-inducible factor-asparagine dioxygenase, go to the full flat file.

Reaction

Synonyms

asparaginyl hydroxylase, asparaginyl-hydroxylase, factor inhibiting HIF, factor inhibiting HIF-1, factor inhibiting hypoxia inducible factor-1alpha, factor-inhibiting HIF, factor-inhibiting hypoxia inducible factor, factor-inhibiting hypoxia-inducible factor, FIH, FIH hydroxylase, HIF asparagine hydroxylase, HIF asparaginyl hydroxylase, HIF hydroxylase, HIF1AN, hypoxia-inducible factor 1-alpha inhibitor, hypoxia-inducible factor asparagine hydroxylase

ECTree

     1 Oxidoreductases

         1.14 Acting on paired donors, with incorporation or reduction of molecular oxygen

             1.14.11 With 2-oxoglutarate as one donor, and incorporation of one atom of oxygen into each donor

                1.14.11.30 hypoxia-inducible factor-asparagine dioxygenase

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Results	in table
5	Activating Compound
11	AA Sequence
3	Application
5	Cloned(Commentary)
2	Crystallization (Commentary)
57	Disease/ Diagnostics
1	Expression
19	General Information
13	IC50 Value
29	Inhibitors
6	kcat/KM [mM/s]
8	Ki Value [mM]
15	KM Value [mM]
9	Metals/Ions
15	Natural Substrates/ Products (Substrates)
18	Organism
29	PDB ID
4	pH Optimum
5	Protein Variants
5	Purification (Commentary)
1	Reaction
18	Reference
16	Source Tissue
37	Substrates and Products (Substrate)
1	Subunits
39	Synonyms
1	Systematic Name
4	Temperature Optimum [°C]
7	Turnover Number [1/s]

Inhibitors

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Inhibitors on EC 1.14.11.30 - hypoxia-inducible factor-asparagine dioxygenase

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INHIBITOR

ORGANISM

UNIPROT

COMMENTARY

LITERATURE

IMAGE

1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid

Homo sapiens

-

i.e. JNJ-42041935, 2-oxoglutarate analogue

765338

-

2,3-dihydroxypyridine

Homo sapiens

-

-

725647

2-hydroxypyridine 1-oxide

Homo sapiens

-

-

725647

3,4-dihydroxybenzoate

Homo sapiens

-

-

659445

3-cyano-6-methyl-2(H)-pyridinone

Homo sapiens

-

-

725647

3-hydroxy-1,2-dimethyl-4(1H)-pyridinone

Homo sapiens

-

-

725647

3-hydroxy-2-methyl-4-pyrone

Homo sapiens

-

-

725647

4-methylcatechol

Homo sapiens

-

-

725647

4-nitrocatechol

Homo sapiens

-

-

725647

4-tert-butylcatechol

Homo sapiens

-

-

725647

5-hydroxy-2-hydroxymethyl-4-pyrone

Homo sapiens

-

-

725647

5-hydroxy-4-oxo-4H-pyran-2-carboxylic acid

Homo sapiens

-

-

725647

Co2+

Homo sapiens

-

-

698722

desferrioxamine

Homo sapiens

-

iron chelator

765338

dimethyloxalylglycine

Homo sapiens

-

2-oxoglutarate analogue

765338

FG-4592

Homo sapiens

-

i.e. roxadustat, 2-oxoglutarate analogue

765338

H2O2

Homo sapiens

-

peroxide rapidly inhibits hydroxlation of diverse FIH substrates and inhibits FIH in a range of cell types. Preferential inhibition of N803-hydroxylation compared with P402/P564 hydroxylation by PHDs, EC 1.14.11.29. Cysteine 800 in HIF-1alpha does not regulate N803 or N847 hydroxylation. FIH activity is not restored by exogenous Fe2+

724847

N-(methoxyoxoacetyl)-glycine methyl ester

Homo sapiens

-

a pan-hydroxylase inhibitor, in vitro and in vivo inhibition

725596

N-oxaloylglycine

Homo sapiens

-

-

698722

N-oxalyl-D-phenylalanine

Homo sapiens

-

-

742895

oxalylglycine

Homo sapiens

-

-

659445

Pyridine-2,4-dicarboxylate

Homo sapiens

-

-

659445

Pyridine-2,5-dicarboxylate

Homo sapiens

-

-

659445

Zn2+

Homo sapiens

-

-

698722

additional information

5 entries

-

additional information

Homo sapiens

-

the Ki-value for 3-hydroxypyridine-2-carbonylglycine and N-((3-hydroxy-6-chloroquinolin-2-yl)carbonyl)glycine are above 0.3 mM

659445

-

additional information

Homo sapiens

-

inhibited by limited hypoxia

698722

-

additional information

Homo sapiens

-

construction of peptide inhibitors consist of amino acids identical to those in the HIF1alpha C-terminal oxygen-dependent degradation domain residues 556-575 except for the 564 proline residue: DLDLEALA-L-trans-4-fluoroproline-YIPADDDFQLR, DLDLEALA-L-trans-4-hydroxyproline-YIPADDDFQLR, DLDLEALA-L-piperidine-2-carboxylic acid-YIPADDDFQLR, DLDLEALA-L-3,4-dehydroproline-YIPADDDFQLR, and DLDLEALA-L-4-thioproline-YIPADDDFQLR. All peptide inhibitors show specific inhibition of PHD2, EC 1.14.11.29, and no inhibition of FIH

724523

-

additional information

Homo sapiens

-

temporal dynamics of hydroxylase inhibition, overview

725596

-

additional information

Homo sapiens

-

screening of iron chelators pyridines, hydroxypyrones/hydroxypyridinones, and catechols as inhibitors for FIH, analysis of selectivity of the inhibitors for FIH compared to PHD2, EC 1.14.11.29. Ligand binding kinetics and structural analysis, overview. Representative inhibitors bind to the metal center in both FIH as an 2-oxoglutarate mimic

725647

-