Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.14.11.53 extracted from

  • Feng, C.; Liu, Y.; Wang, G.; Deng, Z.; Zhang, Q.; Wu, W.; Tong, Y.; Cheng, C.; Chen, Z.
    Crystal structures of the human RNA demethylase Alkbh5 reveal basis for substrate recognition (2014), J. Biol. Chem., 289, 11571-11583.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
mutants of human Alkbh5 are amplified by PCR and subcloned into a modified pET-28a (Novagen) vector encoding a tobacco etch virus protease recognition site. The final clones are verified by DNA sequencing. All of the recombinant plasmids are transformed into Escherichia coli strain BL21(DE3) Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
crystallizations are performed at 24 and 4°C using both the hanging drop and sitting drop vapor diffusion methods. Five high resolution crystal structures of the catalytic core of Alkbh5 in complex with different ligands. These findings provide a structural basis for understanding the substrate recognition specificity of Alkbh5 and offer a foundation for selective drug design against AlkB members Homo sapiens

Protein Variants

Protein Variants Comment Organism
269A/Q271A double mutation shows no impact on the repair efficiency of Alkbh5 Homo sapiens
F232A/F234A mutant exhibits 41% activity toward m6A-containing ssDNA Homo sapiens
F232D/Q233D/F234E the mutant enzyme displays a severe loss of activity, demonstrating only 13.5% of wild-type activity Homo sapiens
K231A/K235A double mutation shows no impact on the repair capacity of Alkbh5 Homo sapiens
K231E/K235E double mutation shows no impact on the repair capacity of Alkbh5 Homo sapiens
Q146A/K147A/R148A mutant retains 44% of the wild-type activity Homo sapiens
R269E/Q271E mutant with greatly reduced catalytic activity to 50% Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
citrate less effective inhibitor Homo sapiens
N-oxalylglycine
-
Homo sapiens
Pyridine 2,4-dicarboxylate moderate inhibitor Homo sapiens
succinate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q6P6C2 fragment
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N6-methyladenine in single-stranded DNA oligonucleotide + 2-oxoglutarate + O2
-
Homo sapiens adenine in single-stranded DNA oligonucleotide + formaldehyde + succinate + CO2
-
?

Synonyms

Synonyms Comment Organism
ALKBH5
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
21
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.2
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.026
-
pH 7.2, 21°C Homo sapiens N-oxalylglycine
0.03
-
pH 7.2, 21°C Homo sapiens succinate
0.347
-
pH 7.2, 21°C Homo sapiens Pyridine 2,4-dicarboxylate
0.628
-
pH 7.2, 21°C Homo sapiens citrate

General Information

General Information Comment Organism
metabolism N6-methylation of adenosine is the most ubiquitous and abundant modification of nucleoside in eukaryotic mRNA and long non-coding RNA. This modification plays an essential role in the regulation of mRNA translation and RNA metabolism Homo sapiens