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3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate
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4,4'-diisothiocyanostilbene-2,2'-disulfonic acid
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FTY720
inhibits ceramide synthases and upregulates dihydrosphingosine 1-phosphate formation in human lung endothelial cells. FTY720 is a sphingosine analogue and in clinical trials as an immunomodulator. Multifaceted mode of interaction between FTY720 and CerS. Conversion to FTY720-phosphate is necessary for its clinical efficacy. FTY720 inhibits ceramide synthesis using C18-CoA to a greater extent than other acyl-CoAs, dependence on acyl-CoA chain length of inhibition of CerS activity by FTY720. Sphinganine first binds to CerS to form an E-S (CerS-sphinganine) complex, and only after formation of this complex can FTY720 bind. The binding sites of FTY720 and acyl-CoA appear to be distinct, but the interaction between sphinganine binding and FTY720 binding nevertheless impacts the rate of the reaction with respect to acyl-CoA. FTY720 inhibits ceramide synthesis at high sphinganine concentrations in vivo, but not at low concentrations, supporting a complex, possibly allosteric mode of interaction between sphinganine and FTY720 and is consistent with uncompetitive inhibitors being most effective at high substrate concentrations. FTY720 acts as a noncompetitive inhibitor toward C18-CoA. The inhibition of FTY720 toward C18-CoA is allosteric under the normal reaction conditions. Sphingolipid composition of HEK cells treated with FTY720, overview; inhibits ceramide synthases and upregulates dihydrosphingosine 1-phosphate formation in human lung endothelial cells. FTY720 is a sphingosine analogue and in clinical trials as an immunomodulator. Multifaceted mode of interaction between FTY720 and CerS. FTY720 inhibits ceramide synthesis using C18-CoA to a greater extent than other acyl-CoAs. Sphinganine first binds to CerS to form an E-S (CerS-sphinganine) complex, and only after formation of this complex can FTY720 bind. The binding sites of FTY720 and acyl-CoA appear to be distinct, but the interaction between sphinganine binding and FTY720 binding nevertheless impacts the rate of the reaction with respect to acyl-CoA. FTY720 inhibits ceramide synthesis at high sphinganine concentrations in vivo, but not at low concentrations, supporting a complex, possibly allosteric mode of interaction between sphinganine and FTY720 and is consistent with uncompetitive inhibitors being most effective at high substrate concentrations
fumonisin
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nixtamalization and rinsing with water effectively reduce both the concentration and ceramide synthase inhibitory activity of readily extractable fumonisins in masa and tortilla products prepared using a commercial process. The data provided no evidence for the formation of biologically active fumonisin reaction products during nixtamalization, baking, or frying
Ca2+
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fumonisin B1
mixed mode of inhibition with respect to the long-chain base
fumonisin B1
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potent inhibition
fumonisin B1
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a ceramide synthase inhibitor
fumonisin B1
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a natural product of the fungus Fusarium moniliforme that acts as a mycotoxin in mammalian cells
fumonisin B1
inhibits the increase in total cellular ceramide induced by UV-C irradiation; inhibits the increase in total cellular ceramide induced by UV-C irradiation
fumonisin B1
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a natural product of the fungus Fusarium moniliforme that acts as a mycotoxin in mammalian cells. It does not affect the rate of cell proliferation or cell viability of P338 cells during 24 h at 0.1 mM, but inhibits 80% and 60% of the apoptotic lethal effect produced by 200 nM and 300 nM daunorubicin, respectively. Increasing the dose of daunorubicin to greater than 500 nM, it also abrogates the inhibitory effect of fumonisin B1
fumonisin B1
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reversible competitive inhibition, inhibits ceramide synthase in mouse brain microsomes with a competitive-like kinetic behavior with respect to both sphinganine and stearoyl-CoA. Fumonisin B1 inhibits ceramide synthase activity when palmitoyl-CoA, stearoyl-CoA, or lignoceroyl-CoA are used as the co-substrate, cf. EC 2.3.1.297 and 2.3.1.24
fumonisin B1
knockdown using fumonisin B 1 reduces ceramide synthase activity by 78%
fumonisin B1
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specific ceramide synthase inhibitor, suppresses hypoxia-reoxygenation-induced ceramide generation and provides protection against hypoxia-reoxygenation-induced EndoG release, DNA fragmentation, and cell death at 0.025-0.1 mM
fumonisin B1
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enzyme inhibition in vivo and in vitro
fumonisin B1
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complete inhibition in vivo and in vitro
fumonisin B1
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potent inhibition
fumonisin B1
competitive, a refolding of activation loop during fumonisin binding results in catalytic inhibition
fumonisin B1
formation of a stable protein-substrate-inhibitor complex. The three molecules bind at different positions within the conserved active site and during a molecular dynamics simulation run no evident change regarding the substitution of sites with substrates and the inhibitor could be observed
Fumonisin B2
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potent inhibition
Fumonisin B2
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potent inhibition
Mn2+
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additional information
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fumonisins are mycotoxins from Fusarium moniliforme
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additional information
FTY720-P has no effect on CerS5 activity. In contrast to the dual effects of fumonisin B1, which is only observed in cells overexpressing CerS, FTY720 elevates ceramide levels in untransfected cells. Dimethylsphingosine has no effect on CerS5 activity; in contrast to the dual effects of fumonisin B1, which is only observed in cells overexpressing CerS, FTY720 elevates ceramide levels in untransfected cells. Dimethylsphingosine has no effect on CerS4 activity
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additional information
FTY720-P has no effect on CerS5 activity. In contrast to the dual effects of fumonisin B1, which is only observed in cells overexpressing CerS, FTY720 elevates ceramide levels in untransfected cells. Dimethylsphingosine has no effect on CerS5 activity; in contrast to the dual effects of fumonisin B1, which is only observed in cells overexpressing CerS, FTY720 elevates ceramide levels in untransfected cells. Dimethylsphingosine has no effect on CerS4 activity
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additional information
no enzyme inhibition by curcumin
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additional information
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enzyme activitiy does not change by pretreating the endoplasmic reticulum-derived membrane vesicles with detergent
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additional information
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fumonisins block sphingosine biosynthesis by inhibiting the conversion of sphinganine to dihydroceramides, which precedes introduction of the 4,5-trans-double bond of sphingosine. Fumonisins, mycotoxins produced by Fusarium moniliforme and a number of other fungi, cause neuronal degeneration, liver and renal toxicity, cancer, and other injury to animals. Fumonisin Bl inhibits complex sphirqolipid synthesis from galactose and sphinganine, effects on the amounts of free sphingosine and sphinganine and on total complex sphingolipids, overview
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additional information
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fumonisins isolated from Fusarium moniliforme inhibit the conversion of sphinganine to N-acyl-sphinganines and the activity of sphingosine N-acyltransferase (ceramide synthase). No inhibiton of serine palmitoyltransferase by fumonisin B1
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additional information
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fumonisins are mycotoxins from Fusarium moniliforme
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