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Literature summary for 1.14.11.29 extracted from

  • Kwon, H.S.; Choi, Y.K.; Kim, J.W.; Park, Y.K.; Yang, E.G.; Ahn, D.R.
    Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides (2011), Bioorg. Med. Chem. Lett., 21, 4325-4328.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of GST-tagged PHD2 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
DLDLEALA-L-3,4-dehydroproline-YIPADDDFQLR
-
Homo sapiens
DLDLEALA-L-4-thioproline-YIPADDDFQLR
-
Homo sapiens
DLDLEALA-L-piperidine-2-carboxylic acid-YIPADDDFQLR
-
Homo sapiens
DLDLEALA-L-trans-4-fluoroproline-YIPADDDFQLR
-
Homo sapiens
DLDLEALA-L-trans-4-hydroxyproline-YIPADDDFQLR
-
Homo sapiens
additional information the peptide inhibitors consist of amino acids identical to those in the CODD556-575 except the 564 proline residue, and target the C-terminal oxygen-dependent degradation domain binding site in the PHD2 active pocket. Specific inhibition of PHD2, no inhibition of FIH, EC 1.14.11.30 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Fe2+ dependent on Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
hypoxia-inducible factor-proline + 2-oxoglutarate + O2 Homo sapiens HIF-1alpha hypoxia-inducible factor-(3S)-3-hydroxy-proline + succinate + CO2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme PHD2
-

Purification (Commentary)

Purification (Comment) Organism
recombinant GST-tagged PHD2 by glutathione affinity chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
hypoxia-inducible factor-proline + 2-oxoglutarate + O2 HIF-1alpha Homo sapiens hypoxia-inducible factor-(3S)-3-hydroxy-proline + succinate + CO2
-
?

Synonyms

Synonyms Comment Organism
PHD
-
Homo sapiens
PHD2
-
Homo sapiens
proline hydroxylase domain 2
-
Homo sapiens
prolyl hydroxylase domain
-
Homo sapiens