Target Information
Target General Infomation | |||||
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Target ID |
T33489
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Former ID |
TTDC00149
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Target Name |
Steryl-sulfatase
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Gene Name |
STS
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Synonyms |
ASC; Arylsulfatase C; Estrone sulfatase; Steroid sulfatase; Steryl-sulfate sulfohydrolase; STS
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
Sulfuric ester hydrolase
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Target Validation |
T33489
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UniProt ID | |||||
EC Number |
EC 3.1.6.2
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Sequence |
MPLRKMKIPFLLLFFLWEAESHAASRPNIILVMADDLGIGDPGCYGNKTIRTPNIDRLAS
GGVKLTQHLAASPLCTPSRAAFMTGRYPVRSGMASWSRTGVFLFTASSGGLPTDEITFAK LLKDQGYSTALIGKWHLGMSCHSKTDFCHHPLHHGFNYFYGISLTNLRDCKPGEGSVFTT GFKRLVFLPLQIVGVTLLTLAALNCLGLLHVPLGVFFSLLFLAALILTLFLGFLHYFRPL NCFMMRNYEIIQQPMSYDNLTQRLTVEAAQFIQRNTETPFLLVLSYLHVHTALFSSKDFA GKSQHGVYGDAVEEMDWSVGQILNLLDELRLANDTLIYFTSDQGAHVEEVSSKGEIHGGS NGIYKGGKANNWEGGIRVPGILRWPRVIQAGQKIDEPTSNMDIFPTVAKLAGAPLPEDRI IDGRDLMPLLEGKSQRSDHEFLFHYCNAYLNAVRWHPQNSTSIWKAFFFTPNFNPVGSNG CFATHVCFCFGSYVTHHDPPLLFDISKDPRERNPLTPASEPRFYEILKVMQEAADRHTQT LPEVPDQFSWNNFLWKPWLQLCCPSTGLSCQCDREKQDKRLSR |
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Drugs and Mode of Action | |||||
Inhibitor | 2',4'-dicyanobiphenyl-4-yl sulfamate | Drug Info | [530712] | ||
2-(4-cyclohexylthiosemicarbazono)methyl-phenol | Drug Info | [528905] | |||
2-Adamantan-2-ylidenemethyl-benzooxazol-6-ol | Drug Info | [527199] | |||
2-Amino-3-Oxo-4-Sulfo-Butyric Acid | Drug Info | [551393] | |||
2-ethylestradiol 3,17-O,O-bis-sulfamate | Drug Info | [528582] | |||
2-methoxyestradiol 3,17-O,O-bis-sulfamate | Drug Info | [528582] | |||
2-methylsulfanylestradiol 3,17-O,O-bis-sulfamate | Drug Info | [528582] | |||
3-(4-cyclohexylthiosemicarbazono)methyl-phenol | Drug Info | [528905] | |||
3-(4-hexylthiosemicarbazono)methyl-benzoic acid | Drug Info | [528905] | |||
3-{3-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate | Drug Info | [526379] | |||
3-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate | Drug Info | [526379] | |||
4-(4-cyclohexylthiosemicarbazono)methyl-phenol | Drug Info | [528905] | |||
4-Sulfamoyloxy-benzoic acid butyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid cycloheptyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid cyclohexyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid cyclooctyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid cyclopentyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid heptyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid hexyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid nonyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid octyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid pentyl ester | Drug Info | [526939] | |||
4-Sulfamoyloxy-benzoic acid propyl ester | Drug Info | [526939] | |||
4-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate | Drug Info | [529570] | |||
B-Octylglucoside | Drug Info | [551393] | |||
Benzomate | Drug Info | [535953] | |||
COUMATE | Drug Info | [530712] | |||
EMATE | Drug Info | [528905] | |||
Estradiol 17-O-sulfamate | Drug Info | [528582] | |||
Estradiol 3,17-O,O-bis-sulfamate | Drug Info | [528582] | |||
MHL cyclohexylthiosemicarbazone | Drug Info | [528905] | |||
Molecule 20 | Drug Info | [535375] | |||
Nortropinyl-arylsulfonylurea 3 | Drug Info | [535851] | |||
PGL-2 | Drug Info | [532697] | |||
PGL-2001 | Drug Info | [532697] | |||
STX 64 | Drug Info | [536200] | |||
Sulfamic acid 2-nonyl-4-oxo-4H-chromen-6-yl ester | Drug Info | [526867] | |||
Sulfamic acid 3-(3-hydroxy-benzoyl)-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 3-(3-methoxy-benzoyl)-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 3-(4-hydroxy-benzoyl)-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 3-(4-methoxy-benzoyl)-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 3-benzoyl-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 4-(2-hydroxy-benzoyl)-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 4-(2-methoxy-benzoyl)-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 4-(3-methoxy-benzoyl)-phenyl ester | Drug Info | [526379] | |||
Sulfamic acid 4-benzoyl-phenyl ester | Drug Info | [526379] | |||
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 523963 | ClinicalTrials.gov (NCT01631981) PGL2001 Proof of Concept Study in Symptomatic Endometriosis. U.S. National Institutes of Health. | ||||
Ref 531371 | Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83. | ||||
Ref 526379 | Bioorg Med Chem Lett. 2002 Aug 19;12(16):2093-5.4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase. | ||||
Ref 526867 | J 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 526939 | Bioorg 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 527199 | Bioorg Med Chem Lett. 2004 Oct 4;14(19):4999-5002.Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase. | ||||
Ref 528582 | J 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 528905 | J 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 529570 | J 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 530712 | J 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 532697 | Synergistic 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 535375 | Review 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 535851 | Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase. Bioorg Med Chem Lett. 2003 Nov 3;13(21):3673-7. | ||||
Ref 535953 | Synthesis, in vitro and in vivo activity of benzophenone-based inhibitors of steroid sulfatase. Bioorg Med Chem. 2004 May 15;12(10):2759-72. |
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