Target Information

Target General Infomation
Target ID
T33489
Former ID
TTDC00149
Target Name
Steryl-sulfatase
Gene Name
STS
Synonyms
ASC; Arylsulfatase C; Estrone sulfatase; Steroid sulfatase; Steryl-sulfate sulfohydrolase; STS
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Endometriosis [ICD9: 617; ICD10: N80]
Prostate cancer [ICD9: 185; ICD10: C61]
Function
Conversion of sulfated steroid precursors to estrogens during pregnancy.
BioChemical Class
Sulfuric ester hydrolase
Target Validation
T33489
UniProt ID
P08842
EC Number
EC 3.1.6.2
Sequence
MPLRKMKIPFLLLFFLWEAESHAASRPNIILVMADDLGIGDPGCYGNKTIRTPNIDRLAS
GGVKLTQHLAASPLCTPSRAAFMTGRYPVRSGMASWSRTGVFLFTASSGGLPTDEITFAK
LLKDQGYSTALIGKWHLGMSCHSKTDFCHHPLHHGFNYFYGISLTNLRDCKPGEGSVFTT
GFKRLVFLPLQIVGVTLLTLAALNCLGLLHVPLGVFFSLLFLAALILTLFLGFLHYFRPL
NCFMMRNYEIIQQPMSYDNLTQRLTVEAAQFIQRNTETPFLLVLSYLHVHTALFSSKDFA
GKSQHGVYGDAVEEMDWSVGQILNLLDELRLANDTLIYFTSDQGAHVEEVSSKGEIHGGS
NGIYKGGKANNWEGGIRVPGILRWPRVIQAGQKIDEPTSNMDIFPTVAKLAGAPLPEDRI
IDGRDLMPLLEGKSQRSDHEFLFHYCNAYLNAVRWHPQNSTSIWKAFFFTPNFNPVGSNG
CFATHVCFCFGSYVTHHDPPLLFDISKDPRERNPLTPASEPRFYEILKVMQEAADRHTQT
LPEVPDQFSWNNFLWKPWLQLCCPSTGLSCQCDREKQDKRLSR
Drugs and Mode of Action
Drug(s) COUMATE Drug Info Phase 2 Breast cancer [1]
PGL-2 Drug Info Phase 2 Endometriosis [2]
PGL-2001 Drug Info Phase 2 Endometriosis [3]
STX 64 Drug Info Phase 1 Prostate cancer [4]
Inhibitor 2',4'-dicyanobiphenyl-4-yl sulfamate Drug Info [5]
2-(4-cyclohexylthiosemicarbazono)methyl-phenol Drug Info [6]
2-Adamantan-2-ylidenemethyl-benzooxazol-6-ol Drug Info [7]
2-Amino-3-Oxo-4-Sulfo-Butyric Acid Drug Info [8]
2-ethylestradiol 3,17-O,O-bis-sulfamate Drug Info [9]
2-methoxyestradiol 3,17-O,O-bis-sulfamate Drug Info [9]
2-methylsulfanylestradiol 3,17-O,O-bis-sulfamate Drug Info [9]
3-(4-cyclohexylthiosemicarbazono)methyl-phenol Drug Info [6]
3-(4-hexylthiosemicarbazono)methyl-benzoic acid Drug Info [6]
3-{3-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Drug Info [10]
3-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Drug Info [10]
4-(4-cyclohexylthiosemicarbazono)methyl-phenol Drug Info [6]
4-Sulfamoyloxy-benzoic acid butyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid cycloheptyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid cyclohexyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid cyclooctyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid cyclopentyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid heptyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid hexyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid nonyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid octyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid pentyl ester Drug Info [11]
4-Sulfamoyloxy-benzoic acid propyl ester Drug Info [11]
4-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Drug Info [12]
B-Octylglucoside Drug Info [8]
Benzomate Drug Info [13]
COUMATE Drug Info [5]
EMATE Drug Info [6]
Estradiol 17-O-sulfamate Drug Info [9]
Estradiol 3,17-O,O-bis-sulfamate Drug Info [9]
MHL cyclohexylthiosemicarbazone Drug Info [6]
Molecule 20 Drug Info [14]
Nortropinyl-arylsulfonylurea 3 Drug Info [15]
PGL-2 Drug Info [16]
PGL-2001 Drug Info [16]
STX 64 Drug Info [17]
Sulfamic acid 2-nonyl-4-oxo-4H-chromen-6-yl ester Drug Info [18]
Sulfamic acid 3-(3-hydroxy-benzoyl)-phenyl ester Drug Info [10]
Sulfamic acid 3-(3-methoxy-benzoyl)-phenyl ester Drug Info [10]
Sulfamic acid 3-(4-hydroxy-benzoyl)-phenyl ester Drug Info [10]
Sulfamic acid 3-(4-methoxy-benzoyl)-phenyl ester Drug Info [10]
Sulfamic acid 3-benzoyl-phenyl ester Drug Info [10]
Sulfamic acid 4-(2-hydroxy-benzoyl)-phenyl ester Drug Info [10]
Sulfamic acid 4-(2-methoxy-benzoyl)-phenyl ester Drug Info [10]
Sulfamic acid 4-(3-methoxy-benzoyl)-phenyl ester Drug Info [10]
Sulfamic acid 4-benzoyl-phenyl ester Drug Info [10]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Steroid hormone biosynthesis
PathWhiz Pathway Androgen and Estrogen Metabolism
Reactome Glycosphingolipid metabolism
WikiPathways Estrogen metabolism
Vitamin D Receptor Pathway
Sphingolipid metabolism
References
REF 1Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83.
REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026648)
REF 3ClinicalTrials.gov (NCT01631981) PGL2001 Proof of Concept Study in Symptomatic Endometriosis. U.S. National Institutes of Health.
REF 4Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020388)
REF 5J 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 6J 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 7Bioorg Med Chem Lett. 2004 Oct 4;14(19):4999-5002.Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase.
REF 8How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 9J 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 10Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.
REF 11Bioorg 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 12J 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 13Synthesis, in vitro and in vivo activity of benzophenone-based inhibitors of steroid sulfatase. Bioorg Med Chem. 2004 May 15;12(10):2759-72.
REF 14Review of estrone sulfatase and its inhibitors--an important new target against hormone dependent breast cancer. Curr Med Chem. 2002 Jan;9(2):263-73.
REF 15Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase. Bioorg Med Chem Lett. 2003 Nov 3;13(21):3673-7.
REF 16Synergistic effects of E2MATE and norethindrone acetate on steroid sulfatase inhibition: a randomized phase I proof-of-principle clinical study in women of reproductive age. Reprod Sci. 2014 Oct;21(10):1256-65.
REF 17Phase I study of STX 64 (667 Coumate) in breast cancer patients: the first study of a steroid sulfatase inhibitor. Clin Cancer Res. 2006 Mar 1;12(5):1585-92.
REF 18J 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.

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