Target Validation Information
Target ID T33489
Target Name Steryl-sulfatase
Target Type
Clinical Trial
Drug Potency against Target 2-ethylestradiol 3,17-O,O-bis-sulfamate Drug Info IC50 = 1000 nM [528582]
Estradiol 3,17-O,O-bis-sulfamate Drug Info IC50 = 18 nM [528582]
STX 64 Drug Info IC50 = 8 nM [552230]
EMATE Drug Info IC50 = 80 nM [528905]
2-(4-cyclohexylthiosemicarbazono)methyl-phenol Drug Info IC50 = 8000 nM [528905]
2-methoxyestradiol 3,17-O,O-bis-sulfamate Drug Info IC50 = 39 nM [528582]
Sulfamic acid 4-(2-hydroxy-benzoyl)-phenyl ester Drug Info IC50 = 4600 nM [526379]
Sulfamic acid 3-(3-hydroxy-benzoyl)-phenyl ester Drug Info IC50 = 6900 nM [526379]
4-Sulfamoyloxy-benzoic acid cyclooctyl ester Drug Info IC50 = 170 nM [526939]
4-Sulfamoyloxy-benzoic acid heptyl ester Drug Info IC50 = 3400 nM [526939]
4-Sulfamoyloxy-benzoic acid cyclohexyl ester Drug Info IC50 = 1700 nM [526939]
4-Sulfamoyloxy-benzoic acid nonyl ester Drug Info IC50 = 4800 nM [526939]
4-Sulfamoyloxy-benzoic acid cycloheptyl ester Drug Info IC50 = 500 nM [526939]
4-Sulfamoyloxy-benzoic acid pentyl ester Drug Info IC50 = 5900 nM [526939]
4-Sulfamoyloxy-benzoic acid octyl ester Drug Info IC50 = 5000 nM [526939]
4-Sulfamoyloxy-benzoic acid cyclopentyl ester Drug Info IC50 = 9300 nM [526939]
3-(4-cyclohexylthiosemicarbazono)methyl-phenol Drug Info IC50 = 4000 nM [528905]
MHL cyclohexylthiosemicarbazone Drug Info IC50 = 460 nM [528905]
3-{3-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Drug Info IC50 = 3200 nM [526379]
Sulfamic acid 3-benzoyl-phenyl ester Drug Info IC50 = 5700 nM [526379]
3-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Drug Info IC50 = 780 nM [526379]
Sulfamic acid 4-(3-methoxy-benzoyl)-phenyl ester Drug Info IC50 = 5200 nM [526379]
Sulfamic acid 3-(3-methoxy-benzoyl)-phenyl ester Drug Info IC50 = 7100 nM [526379]
Sulfamic acid 4-(2-methoxy-benzoyl)-phenyl ester Drug Info IC50 = 4800 nM [526379]
2-methylsulfanylestradiol 3,17-O,O-bis-sulfamate Drug Info IC50 = 320 nM [528582]
Sulfamic acid 3-(4-hydroxy-benzoyl)-phenyl ester Drug Info IC50 = 5000 nM [526379]
2-Adamantan-2-ylidenemethyl-benzooxazol-6-ol Drug Info IC50 = 260 nM [527199]
Sulfamic acid 2-nonyl-4-oxo-4H-chromen-6-yl ester Drug Info IC50 = 403 nM [526867]
4-Sulfamoyloxy-benzoic acid propyl ester Drug Info IC50 = 13200 nM [526939]
4-Sulfamoyloxy-benzoic acid hexyl ester Drug Info IC50 = 3800 nM [526939]
4-(4-cyclohexylthiosemicarbazono)methyl-phenol Drug Info IC50 = 2300 nM [528905]
Sulfamic acid 3-(4-methoxy-benzoyl)-phenyl ester Drug Info IC50 = 6900 nM [526379]
Sulfamic acid 4-benzoyl-phenyl ester Drug Info IC50 = 5100 nM [526379]
4-Sulfamoyloxy-benzoic acid butyl ester Drug Info IC50 = 10500 nM [526939]
4-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Drug Info IC50 = 190 nM [529570]
COUMATE Drug Info IC50 = 1.5 nM [530712]
2',4'-dicyanobiphenyl-4-yl sulfamate Drug Info IC50 = 16.3 nM [530712]
3-(4-hexylthiosemicarbazono)methyl-benzoic acid Drug Info IC50 = 12000 nM [528905]
Action against Disease Model STX 64 The IC50 value of STX64, a potent STS inhibitor, against STS activity in JEG-3 cell line is 0.5 nmol/L. [552873] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The effects of modulating the murine steroid sulfatase axis pharmacologically (through administration of the substrate dehydroepiandrosterone sulfate [DHEAS], 0-40 mg/kg, or acute inhibition of the enzyme by CO uMATE, 10 mg/kg) or genetically (through loss of the gene in 39,X(Y)*O mice) were assayed using the 5-choice serial reaction time task (5-CSRTT) a test of visuospatial attention and response control, and a locomotor activity paradigm.HEAS administration improved 5-CSRTT performance under attentionally demanding conditions, whereas steroid sulfatase inhibition impaired accuracy under the same conditions. Loss of Sts expression constitutively throughout development in 39,X(Y)*O mice resulted in deficits in 5-CSRTT performance at short stimulus durations and reduced anticipatory responding. Neither the pharmacologic nor the genetic manipulations affected basic locomotor activity.These data provide converging evidence indicating a role for steroid sulfatase indiscrete aspects of attentional functioning and are suggestive of a role in motor impulsivity. The findings provide novel insights into the neurobiology of attention and strengthen the notion of STS as a candidate gene for the attentional component of ADHD [528582]
References
Ref 528582J Med Chem. 2006 Dec 28;49(26):7683-96.2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.
Ref 528582J Med Chem. 2006 Dec 28;49(26):7683-96.2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.
Ref 552230Potent active site-directed inhibition of steroid sulphatase by tricyclic coumarin-based sulphamates. Chem Biol. 2000 Oct;7(10):773-91.
Ref 528905J Med Chem. 2007 Jul 26;50(15):3661-6. Epub 2007 Jun 20.Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.
Ref 528905J Med Chem. 2007 Jul 26;50(15):3661-6. Epub 2007 Jun 20.Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.
Ref 528582J Med Chem. 2006 Dec 28;49(26):7683-96.2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 528905J Med Chem. 2007 Jul 26;50(15):3661-6. Epub 2007 Jun 20.Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.
Ref 528905J Med Chem. 2007 Jul 26;50(15):3661-6. Epub 2007 Jun 20.Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 528582J Med Chem. 2006 Dec 28;49(26):7683-96.2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 527199Bioorg Med Chem Lett. 2004 Oct 4;14(19):4999-5002.Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase.
Ref 526867J Med Chem. 2003 Nov 6;46(23):5091-4.Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 528905J Med Chem. 2007 Jul 26;50(15):3661-6. Epub 2007 Jun 20.Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526379Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
Ref 526939Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Ref 529570J Med Chem. 2008 Jul 24;51(14):4226-38. Epub 2008 Jul 1.Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.
Ref 552873A new therapeutic strategy against hormone-dependent breast cancer: the preclinical development of a dual aromatase and sulfatase inhibitor. Clin Cancer Res. 2008 Oct 15;14(20):6469-77. doi: 10.1158/1078-0432.CCR-08-1027.
Ref 530712J Med Chem. 2010 Mar 11;53(5):2155-70.Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
Ref 530712J Med Chem. 2010 Mar 11;53(5):2155-70.Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
Ref 528905J Med Chem. 2007 Jul 26;50(15):3661-6. Epub 2007 Jun 20.Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.

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