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Literature summary extracted from

  • Zhao, W.; Wang, Y.; Hao, W.; Zhao, M.; Peng, S.
    In vitro inhibition of fatty acid synthase by 1,2,3,4,6-penta-O-galloyl-beta-D-glucose plays a vital role in anti-tumour activity (2014), Biochem. Biophys. Res. Commun., 445, 346-351.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.100 1,2,3,4,6-penta-O-galloyl-beta-D-glucose compound is transported across cancer cell membrane to further down-regulate FAS and activate caspase-3 in MDA-MB-231 cells. Compared with other FAS inhibitors, including catechin gallate and morin, 1,2,3,4,6-penta-O-galloyl-beta-D-glucose involves a higher reversible fast-binding inhibition with an irreversible slow-binding inhibition, i.e. saturation kinetics with a dissociation constant of 0.59 microM and a limiting rate constant of 0.16 per min. The major reacting site of PGG is on the beta-ketoacyl reduction domain of FAS. Compound exhibits different types of inhibitions against the three substrates in the FAS overall reaction Homo sapiens
2.3.1.85 1,2,3,4,6-penta-O-galloyl-beta-D-glucose compound is transported across cancer cell membrane to further down-regulate FAS and activate caspase-3 in MDA-MB-231 cells. Compared with other FAS inhibitors, including catechin gallate and morin, 1,2,3,4,6-penta-O-galloyl-beta-D-glucose involves a higher reversible fast-binding inhibition with an irreversible slow-binding inhibition, i.e. saturation kinetics with a dissociation constant of 0.59 microM and a limiting rate constant of 0.16 per min. The major reacting site of PGG is on the beta-ketoacyl reduction domain of FAS. Compound exhibits different types of inhibitions against the three substrates in the FAS overall reaction Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.100 Homo sapiens
-
-
-
2.3.1.85 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.100 MDA-MB-231 cell
-
 Homo sapiens
-
1.1.1.100 U-251 cell
-
 Homo sapiens
-
2.3.1.85 MDA-MB-231 cell
-
 Homo sapiens
-
2.3.1.85 U-251 cell
-
 Homo sapiens
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.85 0.0016
-
 37°C, pH not specified in the publication Homo sapiens 1,2,3,4,6-penta-O-galloyl-beta-D-glucose