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Literature summary for 2.7.1.91 extracted from

  • Lim, K.G.; Tonelli, F.; Berdyshev, E.; Gorshkova, I.; Leclercq, T.; Pitson, S.M.; Bittman, R.; Pyne, S.; Pyne, N.J.
    Inhibition kinetics and regulation of sphingosine kinase 1 expression in prostate cancer cells: functional differences between sphingosine kinase 1a and 1b (2012), Int. J. Biochem. Cell Biol., 44, 1457-1464.
    View publication on PubMed

Application

Application Comment Organism
medicine the expression level and properties of N-terminal 86 amino-acid isoform variant of sphingosine kinase 1, SK1b, in prostate cancer cells reduce its sensitivity to proteasomal degradation induced by 2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole in comparison to isoform SK1a. The reduced sensitivity of SK1b to proteasomal degradation in response to 2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole results in specific changes in ceramide and S1P levels that lead to apoptosis of androgen-sensitive but not androgen-independent LNCaP prostate cancer cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-FTY720 vinylphosphonate uncompetitive with sphingosine and is a mixed inhibitor with respect to ATP Homo sapiens
2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole i.e. SKi, or SKI-II. Mixed inhibitor of sphingosine and ATP binding. N-terminal 86 amino-acid isoform variant SK1b shows reduced sensitivity to proteasomal degradation induced by 2-(p-hydroxyanilino)-4-(p-chlorophenyl)thiazole in comparison to isoform SK1a Homo sapiens
FTY720 i.e. fingolimod, competitive with sphingosine and uncompetitive with ATP Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NYA1 enzyme is expressed as isoform SK1a of 42.5 kDa, and isoform SK1b, a 51 kDa protein identical to SK1a, but with an 86 amino acid N-terminal extension
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