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Literature summary for 1.13.11.31 extracted from

  • Tsai, W.C.; Aleem, A.M.; Whittington, C.; Cortopassi, W.A.; Kalyanaraman, C.; Baroz, A.; Iavarone, A.T.; Skrzypczak-Jankun, E.; Jacobson, M.P.; Offenbacher, A.R.; Holman, T.
    Mutagenesis, hydrogen-deuterium exchange, and molecular docking investigations establish the dimeric interface of human platelet-type 12-lipoxygenase (2021), Biochemistry, 60, 802-812 .
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
modeling of the protein dimer Homo sapiens

Protein Variants

Protein Variants Comment Organism
F174A/W176A/L183E/L187E/Y191A quintuple mutant disrupts both the hydrophobic and pi-pi interactions of the dimer interface, generating an 12-LOX monomer Homo sapiens
L183E/L187E mutant mostly forms monomers, product ratio of 12S:15S-enantiomer is 78:22, strong decrease in inhibition by ML355 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
ML355
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0026
-
arachidonate wild-type, pH 8,23°C Homo sapiens
0.011
-
arachidonate mutant L183E/L187E, pH 8,23°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P18054
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonate + O2
-
Homo sapiens (5Z,8Z,10E,14Z)-(12S)-12-hydroperoxyeicosa-5,8,10,14-tetraenoate
-
?

Subunits

Subunits Comment Organism
dimer modeling of the protein dimer shows a TOP-to-TOP dimeric arrangement with the alpha-helices containing a Leu-rich region (L172, L183, L187, and L194). Four nonoverlapping peptides within helix alpha2 of the TOP subdomain of wild-type are stabilizing, consistent with the dimer interface Homo sapiens

Synonyms

Synonyms Comment Organism
ALOX12
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.4
-
arachidonate mutant L183E/L187E, pH 8,23°C Homo sapiens
7
-
arachidonate wild-type, pH 8,23°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00043
-
wild-type, pH 8,23°C Homo sapiens ML355
0.1
-
above 0.1 mM, mutant L183E/L187E, pH 8,23°C Homo sapiens ML355

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
200
-
arachidonate mutant L183E/L187E, pH 8,23°C Homo sapiens
2700
-
arachidonate wild-type, pH 8,23°C Homo sapiens