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Literature summary for 2.4.1.80 extracted from

  • Alam, S.; Fedier, A.; Kohler, R.S.; Jacob, F.
    Glucosylceramide synthase inhibitors differentially affect expression of glycosphingolipids (2015), Glycobiology, 25, 351-356.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
DL-erythro-1-phenyl-2-decanoylamino-3-morpholino-1-propanol the enzyme GCS inhibitor causes cytotoxic, antiproliferative, antiangiogenic and tumor-volume-reducing effects, modulating drug responses in cell lines both cytodestructive (as a drug sensitizer) and cytoprotective, effect on cell survival, overview. The inhibitor is not suitable to deplete cells of the neolacto glycosphingolipid series Homo sapiens
DL-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol the enzyme GCS inhibitor causes cytotoxic, antiproliferative, antiangiogenic and tumor-volume-reducing effects, modulating drug responses in cell lines both cytodestructive (as a drug sensitizer) and cytoprotective, effect on cell survival, overview. The inhibitor is not suitable to deplete cells of the neolacto glycosphingolipid series Homo sapiens
additional information GCS enzyme inhibitors affect the expression of lactosylceramide, neolacto, ganglio, and globo series glycosphingolipids in a panel of human breast cancer cell lines using flow cytometry, a commonly applied method investigating cell-surface glycosphingolipids after enzyme inhibition, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-glucose + an N-acylsphingosine Homo sapiens
-
UDP + a D-glucosyl-N-acylsphingosine
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16739
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-glucose + an N-acylsphingosine
-
Homo sapiens UDP + a D-glucosyl-N-acylsphingosine
-
?

Synonyms

Synonyms Comment Organism
GCS
-
Homo sapiens
glucosylceramide synthase
-
Homo sapiens

General Information

General Information Comment Organism
malfunction enzyme inhibitors affect the expression of lactosylceramide, neolacto, ganglio, and globo series glycosphingolipids in a panel of human cancer cell lines. Their cell-surface glycosphingolipid expression considerably varies among cell lines and sublethal concentrations (IC10) of both inhibitors preferentially and significantly reduce the expression of globo Gb3 glycosphingolipids in the cancer cell lines IGROV1, BG1, HT29 and T47D, whereas globo SSEA3 glycosphingolipid expression is only reduced in BG1 cells. The neolacto and ganglio glycosphingolipid series is not affected. Lactosylceramider, the precursor of all GlcCer-related glycosphingolipids, is significantly reduced only in BG1 cells treated with DL-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol, overview Homo sapiens
metabolism glucosylceramide synthase catalyzes the first committed step in the biosynthesis of glucosylceramide-related glycosphingolipids, pathway overview Homo sapiens