EC Number   |
Inhibitors |
Structure |
|---|
    2.3.1.24 | 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate |
- |
   |
| 2.3.1.24 | 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid |
- |
|
| 2.3.1.24 | Ca2+ |
- |
|
| 2.3.1.24 | 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 |
|
| 2.3.1.24 | fumonisin |
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 |
|
| 2.3.1.24 | fumonisin B1 |
- |
|
| 2.3.1.24 | fumonisin B1 |
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 |
|
| 2.3.1.24 | fumonisin B1 |
enzyme inhibition in vivo and in vitro |
|
| 2.3.1.24 | fumonisin B1 |
mixed mode of inhibition with respect to the long-chain base |
|
| 2.3.1.24 | fumonisin B1 |
a ceramide synthase inhibitor |
|
