B. Turnover[28] Sphingosine-1-phosphate lyase
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Agonist-induced activation of the S1P receptor 2 constitutes a novel osteoanabolic therapy for the treatment of osteoporosis in mice
2019, BoneCitation Excerpt :We also identified clear associations of serum S1P and bone health in over 4000 human subjects [4]. The pharmacological S1P lyase inhibitor 4-deoxypyridoxine (DOP) that we employed but also several others of this group such as 2-acetyl-4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)imidazole (THI) and the novel LX2931 ((1E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone oxime) that is tested as candidate drug for rheumatoid arthritis in a phase 2 clinical trial, block S1P lyase activity by competing with vitamin B6 at the pyridoxal-5′-phosphate binding domain of the enzyme [11,12]. Accordingly, side effects from interference with a number of other vitamin B6-dependent enzymes are expected.
Epigenetic regulation of pro-inflammatory cytokine secretion by sphingosine 1-phosphate (S1P) in acute lung injury: Role of S1P lyase
2017, Advances in Biological RegulationBacterial versus human sphingosine-1-phosphate lyase (S1PL) in the design of potential S1PL inhibitors
2016, Bioorganic and Medicinal ChemistryA facile stable-isotope dilution method for determination of sphingosine phosphate lyase activity
2016, Chemistry and Physics of LipidsDeficiency of sphingosine-1-phosphate lyase impairs lysosomal metabolism of the amyloid precursor protein
2014, Journal of Biological Chemistry
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