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Literature summary for 2.3.1.85 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

Inhibitors Comment Organism Structure
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

Organism UniProt Comment Textmining
Homo sapiens
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-
-

Source Tissue

Source Tissue Comment Organism Textmining
MDA-MB-231 cell
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Homo sapiens
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U-251 cell
-
Homo sapiens
-

IC50 Value

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