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Literature summary for 2.7.1.91 extracted from

  • Paugh, S.W.; Paugh, B.S.; Rahmani, M.; Kapitonov, D.; Almenara, J.A.; Kordula, T.; Milstien, S.; Adams, J.K.; Zipkin, R.E.; Grant, S.; Spiegel, S.
    A selective sphingosine kinase 1 inhibitor integrates multiple molecular therapeutic targets in human leukemia (2008), Blood, 112, 1382-1391.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(2R,3S,4E)-N-methyl-5-(4'-pentylphenyl)-2-aminopent-4-ene-1,3-diol potent, water-soluble, isoenzyme-specific inhibitor of SphK1. The inhibitor decreases growth and survival of human leukemia U937 and Jurkat cells, and enhances apoptosis and cleavage of Bcl-2. Lethality of SK1-I is reversed by caspase inhibitors and by expression of Bcl-2. The specific inhibitor of SphK1 warrants attention as potential addition to the therapeutic armamentarium in leukemia Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
sphingosine kinase 1
-
Homo sapiens
SPHK1
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.01
-
(2R,3S,4E)-N-methyl-5-(4'-pentylphenyl)-2-aminopent-4-ene-1,3-diol
-
Homo sapiens