Target type: molecularfunction
Catalysis of the reaction: ATP + sphinganine = ADP + sphinganine 1-phosphate. [EC:2.7.1.91]
Sphinganine kinase activity is a key enzymatic step in the biosynthesis of sphingosine-1-phosphate (S1P), a bioactive lipid mediator involved in diverse cellular processes. This activity is catalyzed by sphinganine kinases (SPHKs), which phosphorylate sphinganine at the 1-hydroxyl group, generating sphingosine-1-phosphate (S1P). The reaction requires ATP as a phosphate donor. S1P is a pleiotropic signaling molecule that exerts its effects through binding to five G protein-coupled receptors (S1P1-5) and has been implicated in various physiological and pathological processes, including cell survival, proliferation, migration, inflammation, angiogenesis, and immune regulation. SPHKs exist in multiple isoforms (SPHK1, SPHK2, and SPHK3) with distinct tissue distribution and regulatory mechanisms. They are crucial for maintaining cellular homeostasis and play a role in the development of various diseases. SPHK activity is regulated by a variety of factors, including cellular stress, growth factors, and cytokines. The dysregulation of SPHK activity has been linked to several diseases, including cancer, cardiovascular disease, and neurodegenerative disorders.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Sphingosine kinase 1 | A sphingosine kinase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYA1] | Homo sapiens (human) |
| Sphingosine kinase 2 | A sphingosine kinase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NRA0] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| fingolimod hydrochloride | fingolimod hydrochloride : The hydrochloride salt of 2-amino-2-[2-(4-octylphenyl) ethyl]-1,3-propanediol (fingolimod). Fingolimod Hydrochloride: A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS. | hydrochloride | immunosuppressive agent; prodrug; sphingosine-1-phosphate receptor agonist |
| 4-(4-(4-chloro-phenyl)thiazol-2-ylamino)phenol | substituted aniline | ||
| safingol | safingol: RN given refers to the (R-(R*,S*))-isomer | amino alcohol | |
| sphingosine | 2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4. sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position. sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration. sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds. | sphing-4-enine | human metabolite; mouse metabolite |
| n,n-dimethylsphingenine | N,N-dimethylsphingosine : A sphingoid that is sphingosine in which the two amino hydrogens are replaced by methyl groups. N,N-dimethylsphingosine: a sphingosine kinase inhibitor | aminodiol; sphingoid; tertiary amino compound | EC 2.7.1.91 (sphingosine kinase) inhibitor; metabolite |
| es-285 | 1-deoxysphinganine : A bioactive sphingoid, sphinganine, in which the terminal hydroxy group has been replaced by a hydrogen. spisulosine: from marine organism, Spisula polynyma; structure in first source | amino alcohol; sphingoid | antineoplastic agent |
| 3-(4-chlorophenyl)-adamantane-1-carboxylic acid (pyridin-4-ylmethyl)amide | organochlorine compound | ||
| bml 258 | |||
| pf-543 | PF-543: Sphingosine Kinase 1 Selective Inhibitor; structure in first source | sulfonamide | |
| rome | (2R)-2-amino-2-(methoxymethyl)-4-(4-octylphenyl)butan-1-ol : A 2-amino-2-(methoxymethyl)-4-(4-octylphenyl)butan-1-ol that has R-configuration. It is a sphingosine kinase-2 inhibitor. Rome: The capital city of Italy. | 2-amino-2-(methoxymethyl)-4-(4-octylphenyl)butan-1-ol | EC 2.7.1.91 (sphingosine kinase) inhibitor |