Target Information

Target General Infomation
Target ID
T86014
Former ID
TTDI02179
Target Name
Sphingosine kinase
Gene Name
SPHK1
Synonyms
SK 1; SPK 1; SPHK1
Target Type
Clinical Trial
Disease Arteriosclerosis [ICD9: 440; ICD10: I70]
Late-stage ovarian cancer; Lymphoma [ICD9:140-229, 183, 188, 202.8, 208.9; ICD10: C56, C67, C81-C86]
Vascular disease [ICD9: 325, 430-459; ICD10: G45-G46, I60-I95]
Function
Catalyzes the phosphorylation of sphingosine to form sphingosine 1-phosphate (SPP), a lipid mediator with both intra- and extracellular functions. Also acts on D-erythro-sphingosine and to a lesser extent sphinganine, but not other lipids,such as D,L-threo-dihydrosphingosine, N,N-dimethylsphingosine, diacylglycerol, ceramide, or phosphatidylinositol.
BioChemical Class
Kinase
UniProt ID
Q9NYA1
EC Number
EC 2.7.1.91
Sequence
MDPAGGPRGVLPRPCRVLVLLNPRGGKGKALQLFRSHVQPLLAEAEISFTLMLTERRNHA
RELVRSEELGRWDALVVMSGDGLMHEVVNGLMERPDWETAIQKPLCSLPAGSGNALAASL
NHYAGYEQVTNEDLLTNCTLLLCRRLLSPMNLLSLHTASGLRLFSVLSLAWGFIADVDLE
SEKYRRLGEMRFTLGTFLRLAALRTYRGRLAYLPVGRVGSKTPASPVVVQQGPVDAHLVP
LEEPVPSHWTVVPDEDFVLVLALLHSHLGSEMFAAPMGRCAAGVMHLFYVRAGVSRAMLL
RLFLAMEKGRHMEYECPYLVYVPVVAFRLEPKDGKGVFAVDGELMVSEAVQGQVHPNYFW
MVSGCVEPPPSWKPQQMPPPEEPL
Drugs and Mode of Action
Drug(s) Phenoxodiol Drug Info Phase 1/2 Late-stage ovarian cancer; Lymphoma [521895]
B-5354a Drug Info Terminated Arteriosclerosis [525909]
F-12509A Drug Info Terminated Arteriosclerosis [525833]
Inhibitor B-5354a Drug Info [525910]
F-12509A Drug Info [525833]
PF-543 Drug Info [531834]
SK1-I Drug Info [529501]
VPC-94075 Drug Info [543575]
Modulator Phenoxodiol Drug Info [1572591]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Sphingosine and sphingosine-1-phosphate metabolism
KEGG Pathway Sphingolipid metabolism
Metabolic pathways
Calcium signaling pathway
Sphingolipid signaling pathway
VEGF signaling pathway
Fc gamma R-mediated phagocytosis
Tuberculosis
NetPath Pathway TCR Signaling Pathway
TNFalpha Signaling Pathway
PANTHER Pathway Angiogenesis
VEGF signaling pathway
Pathway Interaction Database Fc-epsilon receptor I signaling in mast cells
Beta3 integrin cell surface interactions
S1P1 pathway
Sphingosine 1-phosphate (S1P) pathway
PDGFR-beta signaling pathway
Reactome Sphingolipid de novo biosynthesis
VEGFR2 mediated cell proliferation
WikiPathways Signal Transduction of S1P Receptor
Protein folding
Sphingolipid Metabolism
References
Ref 521895ClinicalTrials.gov (NCT00382811) OVATURE (OVArian TUmor REsponse) A Phase III Study of Weekly Carboplatin With and Without Phenoxodiol in Patients With Platinum-Resistant, Recurrent Epithelial Ovarian Cancer. U.S. National Institutes of Health.
Ref 525833F-12509A, a new sphingosine kinase inhibitor, produced by a discomycete. J Antibiot (Tokyo). 2000 May;53(5):459-66.
Ref 525909B-535a, b and c, new sphingosine kinase inhibitors, produced by a marine bacterium; taxonomy, fermentation, isolation, physico-chemical properties and structure determination. J Antibiot (Tokyo). 2000 Aug;53(8):753-8.
Ref
Ref 525833F-12509A, a new sphingosine kinase inhibitor, produced by a discomycete. J Antibiot (Tokyo). 2000 May;53(5):459-66.
Ref 525910Characterization of B-5354c, a new sphingosine kinase inhibitor, produced by a marine bacterium. J Antibiot (Tokyo). 2000 Aug;53(8):759-64.
Ref 529501A selective sphingosine kinase 1 inhibitor integrates multiple molecular therapeutic targets in human leukemia. Blood. 2008 Aug 15;112(4):1382-91.
Ref 531834Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88.
Ref 543575(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2204).
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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