Literature summary for 2.8.2.1 extracted from

Meng, L.H.; Shankavaram, U.; Chen, C.; Agama, K.; Fu, H.Q.; Gonzalez, F.J.; Weinstein, J.; Pommier, Y.
Activation of aminoflavone (NSC 686288) by a sulfotransferase is required for the antiproliferative effect of the drug and for induction of histone gamma-H2AX (2006), Cancer Res., 66, 9656-9664.

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Activating Compound

Activating Compound	Comment	Organism	Structure
additional information	5-amino-2-(4-amino-3-fluorophenyl)-6,8-difluoro-7-methyl-4H-1-benzopyran-4-one induces the expression of SULT1A1 via the aryl hydrocarbon receptor, AhR, signaling pathway, mechanism, overview	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
additional information	downregulation of SULT1A1 by specific siRNA, transfection of SULT1A1 into MDA-MB-231 cells restores formation of DNA-protein cross-links and histone gamma-H2AX foci in response to aminoflavone	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
apigenin	antagonizes aminoflavone by inhibiting SULT1A1	Homo sapiens
daidzein	antagonizes aminoflavone by inhibiting SULT1A1	Homo sapiens
genistein	antagonizes aminoflavone by inhibiting SULT1A1	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
3'-phosphoadenylyl sulfate + 5-amino-2-(4-amino-3-fluorophenyl)-6,8-difluoro-7-methyl-4H-1-benzopyran-4-one	Homo sapiens	i.e. aminoflavone, diaminoflavone analogues with potent growth-inhibitory activity against human breast and renal cancer cells in vitro and antitumor activity in mice bearing human tumor xenografts, aminoflavone binds to DNA in tumor cells and induces DNA-protein cross-links	adenosine 3',5'-bisphosphate + ?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P50225	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
MCF-7 cell	-	Homo sapiens	-
MDA-MB-231 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
3'-phosphoadenylyl sulfate + 5-amino-2-(4-amino-3-fluorophenyl)-6,8-difluoro-7-methyl-4H-1-benzopyran-4-one	i.e. aminoflavone, diaminoflavone analogues with potent growth-inhibitory activity against human breast and renal cancer cells in vitro and antitumor activity in mice bearing human tumor xenografts, aminoflavone binds to DNA in tumor cells and induces DNA-protein cross-links	Homo sapiens	adenosine 3',5'-bisphosphate + ?	-	?
3'-phosphoadenylyl sulfate + 5-amino-2-(4-amino-3-fluorophenyl)-6,8-difluoro-7-methyl-4H-1-benzopyran-4-one	i.e. aminoflavone	Homo sapiens	adenosine 3',5'-bisphosphate + ?	-	?

Synonyms

Synonyms	Comment	Organism
SULT1A1	-	Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.4	-	assay at	Homo sapiens

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Release 2023.1 (January 2023)