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Literature summary for 2.5.1.26 extracted from

  • Stazi, G.; Battistelli, C.; Piano, V.; Mazzone, R.; Marrocco, B.; Marchese, S.; Louie, S.M.; Zwergel, C.; Antonini, L.; Patsilinakos, A.; Ragno, R.; Viviano, M.; Sbardella, G.; Ciogli, A.; Fabrizi, G.; Cirilli, R.; Strippoli, R.; Marchetti, A.; Tripodi, M.; Nomura, D.K.; Mattevi, A.; Mai, A.; Valent, V.a.l.e.n.t.e.
    Development of alkyl glycerone phosphate synthase inhibitors Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells (2019), Eur. J. Med. Chem., 163, 722-735 .
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(3S)-3-(2-fluorophenyl)-N-((2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)methyl)butanamide
-
 Cavia porcellus
(3S)-3-(2-fluorophenyl)-N-((2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)methyl)butanamide
-
 Homo sapiens
3-(2,6-difluorophenyl)-N-((2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)methyl)butanamide the inhibitor show higher binding affinity but retains the binding mode observed for (3S)-3-(2-fluorophenyl)-N-((2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)methyl)butanamide with the second fluorine atom likely enhancing the hydrophobic interactions with the aliphatic residues surrounding the substrate tunnel Cavia porcellus
3-(2,6-difluorophenyl)-N-((2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)methyl)butanamide the inhibitor show higher binding affinity but retains the binding mode observed for (3S)-3-(2-fluorophenyl)-N-((2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)methyl)butanamide with the second fluorine atom likely enhancing the hydrophobic interactions with the aliphatic residues surrounding the substrate tunnel Homo sapiens

Organism

Organism UniProt Comment Textmining
Cavia porcellus P97275
-
-
Homo sapiens O00116
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MDA-MB-231 cell
-
 Homo sapiens
-
PC-3 cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
AGPS
-
 Homo sapiens
AGPS
-
 Cavia porcellus

Cofactor

Cofactor Comment Organism Structure
FAD FAD-dependent enzyme Homo sapiens
FAD FAD-dependent enzyme Cavia porcellus

Expression

Organism Comment Expression
Homo sapiens up-regulated across different types of aggressive cancers such as human breast 231MFP, melanoma C8161, and prostate PC-3 cancers up

General Information

General Information Comment Organism
malfunction knockdown of alkylglycerone-phosphate synthase leads to an overall reduction of ether lipid levels, as well as oncogenic signaling molecules, such as LPAe, PAFe and eicosanoids Homo sapiens
malfunction knockdown of alkylglycerone-phosphate synthase leads to an overall reduction of ether lipid levels, as well as oncogenic signaling molecules, such as LPAe, PAFe and eicosanoids, and it shows lower tumor growth rates in xenograft mice Cavia porcellus