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

BRENDA support

Literature summary for 2.7.1.91 extracted from

  • Lim, K.G.; Tonelli, F.; Li, Z.; Lu, X.; Bittman, R.; Pyne, S.; Pyne, N.J.
    FTY720 analogues as sphingosine kinase 1 inhibitors: enzyme inhibition kinetics, allosterism, proteasomal degradation, and actin rearrangement in MCF-7 breast cancer cells (2011), J. Biol. Chem., 286, 18633-18640.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.91

Cloned(Commentary)

Cloned (Comment) Organism
expression in HEK-293 cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-FTY720 vinylphosphonate uncompetitive, binds to a putative allosteric site in the enzyme contingent on formation of the enzyme-sphingosine complex. (S)-FTY720 vinylphosphonate binding to and stabilization of the allosteric site might enhance the autoinhibitory effect on the enzymic activity Homo sapiens
2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole mixed type inhibition Homo sapiens
FTY720 competitive Homo sapiens
additional information enzyme is an oligomeric protein containing noncooperative catalytic sites, the allosteric site exerts an autoinhibition of the catalytic site Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information enzyme is an oligomeric protein containing noncooperative catalytic sites, the allosteric site exerts an autoinhibition of the catalytic site Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NYA1
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MCF-7 cell
-
 Homo sapiens
-

Subunits

Subunits Comment Organism
More oligomeric protein containing noncooperative catalytic sites, the allosteric site exerts an autoinhibition of the catalytic site Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.002
-
 FTY720 pH 7.4, 30°C Homo sapiens
0.0145
-
 (S)-FTY720 vinylphosphonate pH 7.4, 30°C Homo sapiens
0.017
-
 2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole pH 7.4, 30°C, competitive inhibition Homo sapiens
0.048
-
 2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole pH 7.4, 30°C, uncompetitive inhibition Homo sapiens