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Literature summary for 1.14.19.17 extracted from

  • Casasampere, M.; Ordonez, Y.F.; Casas, J.; Fabrias, G.
    Dihydroceramide desaturase inhibitors induce autophagy via dihydroceramide-dependent and independent mechanisms (2017), Biochim. Biophys. Acta, 1861, 264-275 .
    View publication on PubMed

Application

Application Comment Organism
pharmacology the cells capacity to biosynthesize dihydroceramides must be taken into account in proautophagic Des1 inhibitors-including therapies Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
celecoxib CCX Homo sapiens
fenretinide
-
Homo sapiens
additional information in T98G and U87MG glioblastoma cell lines different Des1 inhibitory pro-autophagic compounds (DIPACS) exhibiting different cytotoxicities (CCX, PXD, resveratrol, gamma-tocotrienol and XM462), trigger autophagy via different pathways, both dihydroceramide-dependent and independent pathways Homo sapiens
phenoxodiol PXD Homo sapiens
resveratrol
-
Homo sapiens
tetrahydrocannabinol
-
Homo sapiens
XM462 an active-site directed Des1 inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
tetracosanoyl-dihydroceramide + reduced acceptor + O2 + 2 H+ Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
glioblastoma cell
-
Homo sapiens
-
T-98G cell
-
Homo sapiens
-
U-87DND cell
-
Homo sapiens
-
U-87MG cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-[6-[(7-nitro-2-1,3-benzoxadiazol-4-yl)amino]hexanoyl]-D-erythro-sphinganine + reduced acceptor + O2 + 2 H+
-
Homo sapiens ?
-
?
tetracosanoyl-dihydroceramide + reduced acceptor + O2 + 2 H+
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
dihydroceramide desaturase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
in vivo assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
cytochrome b5
-
Homo sapiens

Expression

Organism Comment Expression
Homo sapiens gamma-tocotrienol causes downregulation of Des1 expression but is not inhibitory for the enzyme activity down

General Information

General Information Comment Organism
malfunction dihydroceramide desaturase 1 inhibitors activate autophagy via both dihydroceramide-dependent and independent pathways and the balance between the two pathways influences the final cell fate. Enzyme inhibitors celecoxib, resveratrol, phenoxodiol, and gamma-tocotrienol, but not gamma-tocopherol at 0.05 mM, promote an increase in dihydroceramide, dihydrosphingomyelins, and lactosyldihydroceramides in U-87MG and T-98G cell lines. Similar results are found with the active site-directed Des1 inhibitor XM462 Homo sapiens