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Literature summary for 3.1.6.2 extracted from

  • Mostafa, Y.A.; Kralt, B.; Rao, P.P.; Taylor, S.D.
    A-ring substituted 17beta-arylsulfonamides of 17beta-aminoestra-1,3,5(10)-trien-3-ol as highly potent reversible inhibitors of steroid sulfatase (2015), Bioorg. Med. Chem., 23, 5681-5692 .
    View publication on PubMed
Search for more literature for 3.1.6.2

Inhibitors

Inhibitors Comment Organism Structure
4-fluoro-17beta-(3'-trifluoromethylbenzene)sulfonamideestra-1,3,5(10)-trien-3-ol
-
 Homo sapiens
4-nitro-17beta-4'-biphenylsulfonamide-1,3,5(10)-estratrien-3-ol
-
 Homo sapiens
additional information design of sulfated steroid inhibitors. The presence of a NO2 or Br at the 2-position of the A-ring results in a decrease in potency compared to their A-ring-unsubstituted counterparts. The presence of a nitro group or fluorine atom at the 4-position of the A-ring results in an increase in potency Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P08842
-
-

Source Tissue

Source Tissue Comment Organism Textmining
BT-549 cell
-
 Homo sapiens
-
Hs-578T cell
-
 Homo sapiens
-
MDA-MB-231 cell
-
 Homo sapiens
-
MDA-MB-468 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferyl sulfate + H2O
-
 Homo sapiens 4-methylumbelliferone + sulfate
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1
-
 pH 7.4, 24°C Homo sapiens 4-nitro-17beta-4'-biphenylsulfonamide-1,3,5(10)-estratrien-3-ol
2.5
-
 pH 7.4, 24°C Homo sapiens 4-fluoro-17beta-(3'-trifluoromethylbenzene)sulfonamideestra-1,3,5(10)-trien-3-ol