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Literature summary for 1.14.11.16 extracted from

  • Brewitz, L.; Tumber, A.; Zhang, X.; Schofield, C.J.
    Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-beta-hydroxylase (2020), Bioorg. Med. Chem., 28, 115675 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
N-terminally His6-tagged human AspH315-758 (His6-AspH315-758) is produced in Escherichia coli BL21 (DE3) cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(R)-gossypol
-
Homo sapiens
belinostat
-
Homo sapiens
bleomycin A2
-
Homo sapiens
midostaurin
-
Homo sapiens
mithramycin A
-
Homo sapiens
navitoclax
-
Homo sapiens
obatoclax
-
Homo sapiens
plicamycin
-
Homo sapiens
pyridine-2,4-dicarboxylic acid
-
Homo sapiens
tubacin
-
Homo sapiens
vemurafenib
-
Homo sapiens
venetoclax
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Fe2+ Fe2+-dependent enzyme Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q12797
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
peptide-L-aspartate + 2-oxoglutarate + O2 the substrate is the synthetic thioether linked cyclic peptide hFX-CP101-119. It is designed based on 19 EGFD1 amino acid residues of the sequence of human coagulation factor X (hFX amino acids 101-119) Homo sapiens peptide-3-hydroxy-L-aspartate + succinate + CO2
-
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Synonyms

Synonyms Comment Organism
aspartate/asparagine-beta-hydroxylase
-
Homo sapiens
ASPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
pH 7.5, 20°C Homo sapiens pyridine-2,4-dicarboxylic acid
0.00025
-
pH 7.5, 20°C Homo sapiens (R)-gossypol
0.00103
-
pH 7.5, 20°C Homo sapiens navitoclax
0.0014
-
pH 7.5, 20°C Homo sapiens venetoclax
0.00147
-
pH 7.5, 20°C Homo sapiens bleomycin A2
0.00338
-
pH 7.5, 20°C Homo sapiens vemurafenib
0.00412
-
pH 7.5, 20°C Homo sapiens tubacin
0.00749
-
pH 7.5, 20°C Homo sapiens belinostat
0.00943
-
pH 7.5, 20°C Homo sapiens midostaurin
0.0095
-
pH 7.5, 20°C Homo sapiens mithramycin A
0.0129
-
pH 7.5, 20°C Homo sapiens obatoclax
0.0132
-
pH 7.5, 20°C Homo sapiens plicamycin

Expression

Organism Comment Expression
Homo sapiens upregulated on the cell surface of invasive cancer cells up

General Information

General Information Comment Organism
physiological function the enzyme catalyses the hydroxylation of Asp/Asn-residues of epidermal growth factor-like domains Homo sapiens