EC Number |
Inhibitors |
Structure |
---|
2.3.1.297 | australifungin |
- |
|
2.3.1.297 | Ca2+ |
- |
|
2.3.1.297 | 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. FTY720 itself and not FTY720-P, is responsible for CerS2 inhibition. 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. Inhibition of CerS2 by FTY720 does not occur via a nonspecific mechanism |
|
2.3.1.297 | FTY720 |
FTY720 is an effective immunomodulatory molecule and is a competitive inhibitor of ceramide synthase 2 toward dihydrosphingosine, it shows interference with sphingolipid de novo biosynthesis, overview. The inhibition of CerS2 activity is reversible as the potency of inhibition diminishes with the dilution of the enzyme-inhibitor preparation |
|
2.3.1.297 | fumonisin B1 |
- |
|
2.3.1.297 | fumonisin B1 |
mixed mode of inhibition with respect to the laong-chain base; mixed mode of inhibition with respect to the long-chain base |
|
2.3.1.297 | fumonisin B1 |
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 |
|
2.3.1.297 | fumonisin B1 |
inhibits the increase in total cellular ceramide induced by UV-C irradiation |
|
2.3.1.297 | Mn2+ |
- |
|
2.3.1.297 | more |
LOH1 is inhibited by most or all divalent cations tested; LOH3 is inhibited by most or all divalent cations tested |
|