Estrone Sulphate ESTRONE ESTROPIPATE BDBM50366524 Estrone 3-sulfate
BDBM17289 Estrone, 15 Estrone (E1) Estrovarin (1S,10R,11S,15S)-5-hydroxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2,4,6-trien-14-one Unigen Kestrone CHEMBL1405 [2,4,6,7-3H]-E1 Estrone folliculin [2,4,6,7-3H]-Estrone Theelin
13-methyl-17-oxo-3-sulfooxy-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene {15-methyl-14-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-trien-5-yl}oxidanesulfonic acid [3H]estrone sulfate [3H]Estrone 3-sulfate BDBM10022 [6,7-3H] E1S Estrone 3-sulfate
cid_92895 SMR000058657 MLS000028621 (8R,9S,13S,14S)-3-methoxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one ESTRONE 3-METHYL ETHER BDBM48630
(15S)-15-methyl-14-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-trien-5-yl sulfamate BDBM11637 estrone-3-O-sulfamate sulfamate compound 4 EMATE
- Howarth, NM; Purohit, A; Reed, MJ; Potter, BV Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential. J Med Chem 37: 219-21 (1994)
- Howarth, NM; Cooper, G; Purohit, A; Duncan, L; Reed, MJ; Potter, BV Phosphonates and thiophosphonates as sulfate surrogates: synthesis of estrone 3-methylthiophosphonate, a potent inhibitor of estrone sulfatase Bioorg Med Chem Lett 3: 313-318 (1993)
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- Ahmed, S; James, K; Owen, CP; Patel, CK; Patel, M Novel inhibitors of the enzyme estrone sulfatase (ES). Bioorg Med Chem Lett 11: 841-4 (2001)
- Laplante, Y; Cadot, C; Fournier, MA; Poirier, D Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone. Bioorg Med Chem 16: 1849-60 (2008)
- Ahmed, S; James, K; Owen, CP; Patel, CK; Patel, M Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). Bioorg Med Chem Lett 11: 2525-8 (2001)
- Phan, CM; Liu, Y; Kim, BM; Mostafa, Y; Taylor, SD Inhibition of steroid sulfatase with 4-substituted estrone and estradiol derivatives. Bioorg Med Chem 19: 5999-6005 (2011)
- Oster, A; Klein, T; Werth, R; Kruchten, P; Bey, E; Negri, M; Marchais-Oberwinkler, S; Frotscher, M; Hartmann, RW Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. Bioorg Med Chem 18: 3494-505 (2010)
- Möller, G; Deluca, D; Gege, C; Rosinus, A; Kowalik, D; Peters, O; Droescher, P; Elger, W; Adamski, J; Hillisch, A Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone. Bioorg Med Chem Lett 19: 6740-4 (2009)
- Woo, LW; Purohit, A; Reed, MJ; Potter, BV Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates. J Med Chem 39: 1349-51 (1996)
- Schreiner, EP; Billich, A Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase. Bioorg Med Chem Lett 14: 4999-5002 (2004)
- Jütten, P; Schumann, W; Härtl, A; Dahse, HM; Gräfe, U Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase. J Med Chem 50: 3661-6 (2007)
- Ahmed, S; James, K Derivation of a possible transition-state for the reaction catalysed by the enzyme estrone Sulfatase (ES). Bioorg Med Chem Lett 9: 1645-50 (1999)
- Vicker, N; Ho, Y; Robinson, J; Woo, LL; Purohit, A; Reed, MJ; Potter, BV Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II. Bioorg Med Chem Lett 13: 863-5 (2003)
- Ahmed, S; James, K; Owen, CP Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. Bioorg Med Chem Lett 12: 2391-4 (2002)
- Ahmed, S; Owen, CP; James, K; Patel, CK; Patel, M Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). Bioorg Med Chem Lett 11: 899-902 (2001)
- Lawrence Woo, LW; Leblond, B; Purohit, A; Potter, BV Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. Bioorg Med Chem 20: 2506-19 (2012)
- Ahmed, S; James, K; Owen, CP; Patel, CK; Patel, MB Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism. Bioorg Med Chem Lett 11: 3001-5 (2001)
- Ahmed, S; James, K; Owen, CP; Patel, CK Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES). Bioorg Med Chem Lett 12: 1343-6 (2002)
- Patel, CK; Owen, CP; Ahmed, S Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. Bioorg Med Chem Lett 14: 605-9 (2004)
- Allan, GM; Lawrence, HR; Cornet, J; Bubert, C; Fischer, DS; Vicker, N; Smith, A; Tutill, HJ; Purohit, A; Day, JM; Mahon, MF; Reed, MJ; Potter, BV Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. J Med Chem 49: 1325-45 (2006)
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- Poirier, D; Boivin, RP 17 alpha-alkyl- or 17 alpha-substituted benzyl-17 beta-estradiols: a new family of estrone-sulfatase inhibitors. Bioorg Med Chem Lett 8: 1891-6 (1999)
- Bellavance, E; Luu-The, V; Poirier, D Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone. J Med Chem 52: 7488-502 (2009)
- ChEMBL_1577309 Inhibition of estrone sulfatase in human MCF7 cells using estrone sulphate as substrate
- ChEBML_68018 Inhibition of Estrone sulfatase
- ChEBML_68177 Inhibition of estrone sulfatase
- ChEMBL_1577310 Inhibition of human estrone sulfatase expressed in CHO cells using estrone sulphate as substrate
- ChEMBL_1577238 Inhibition of placental microsomal estrone sulfatase (unknown origin) using [3H]-estrone sulphate as substrate
- ChEBML_68020 Inhibition of estrone sulfatase (ES)
- ChEBML_68022 In vitro inhibition of estrone sulfatase.
- ChEBML_68019 Inhibitory concentration against estrone sulfatase
- ChEMBL_68016 Inhibitory activity against Estrone Sulfatase
- ChEBML_67983 Tested for the inhibitory activity against Estrone Sulfatase
- ChEBML_68015 Inhibitory activity against estrone sulfatase enzyme
- ChEBML_68017 Inhibitory activity against Estrone sulfatase was determined
- ChEMBL_1577317 Inhibition of estrone sulfatase in human MCF7 cells
- ChEMBL_398763 Inhibition of estradiol to estrone conversion in MG63 cells
- ChEMBL_439850 Inhibition of Estrone sulfatase in human placental microsome
- ChEMBL_67986 In vitro inhibition of estrone sulfatase in placental microsomes
- ChEMBL_67989 Inhibition against estrone sulfatase in placental preparation
- ChEMBL_1577226 Inhibition of estrone sulfatase in human MCF7 cells using [3H]-estrone sulphate as substrate incubated for 30 mins by liquid scintillation counting method
- ChEMBL_1577305 Inhibition of placental microsomal estrone sulfatase (unknown origin) using [3H]-estrone sulphate as substrate incubated for 20 mins by scintillation counting method
- ChEMBL_67988 Inhibition against estrone sulfatase in breast tumor preparations
- ChEMBL_68003 Binding affinity against estrone sulfatase in placental preparation
- ChEMBL_68176 Inhibitory activity against Estrone sulfatase (E1-STS)
- ChEMBL_838179 TP_TRANSPORTER: inhibition of Estrone sulfate in Xenopus laevis oocytes
- ChEMBL_1577225 Inhibition of estrone sulfatase in human JEG-3 cells using [3H]-estrone sulphate as substrate incubated for 1 hr by liquid scintillation counting method
- ChEMBL_1577316 Inhibition of estrone sulfatase in human JEG-3 cells using [3H]-estrone sulphate as substrate incubated for 4 hrs by liquid scintillation counting method
- ChEBML_68021 Inhibitory concentration required to inhibit the enzyme estrone sulfatase was determined
- ChEMBL_1482579 Inhibition of human OAT3 using estrone-3-sulfate as substrate
- ChEMBL_1482580 Inhibition of rat OAT3 using estrone-3-sulfate as substrate
- ChEMBL_1577306 Inhibition of estrone sulfatase in human sebocytes using DHEAS as substrate
- ChEMBL_1577308 Inhibition of estrone sulfatase human keratinocytes using DHEAS as substrate
- ChEMBL_552851 Inhibition of human placental 17beta-HSD1 using estrone substrate
- ChEMBL_630246 Displacement of [3H]estrone from human placental 17beta-HSD1
- ChEMBL_68002 Binding affinity against estrone sulfatase in breast tumor preparations
- ChEMBL_838168 TP_TRANSPORTER: uptake&inhibition of estrone sulfate in OAT3-S2 cells
- ChEMBL_838813 TP_TRANSPORTER: uptake&inhibition of estrone sulfate in OAT4-S2 cells
- ChEBML_68012 In vitro binding affinity against estrone sulfatase in rat liver microsomes
- ChEMBL_1577307 Inhibition of estrone sulfatase in human skin fibroblasts using DHEAS as substrate
- ChEMBL_1896403 Inhibition of human placental microsome sulfatase using estrone sulfate as substrate
- ChEMBL_68014 Compound was evaluated for its inhibitory activity against estrone sulfatase enzyme
- ChEMBL_838483 TP_TRANSPORTER: inhibition of Estrone sulfate uptake in OAT3-expressing S2 cells
- ChEMBL_838512 TP_TRANSPORTER: inhibition of Estrone sulfate uptake in OAT3-expressing S2 cells
- ChEMBL_838708 TP_TRANSPORTER: inhibition of Estrone sulfate uptake in OAT4-expressing S2 cells
- ChEMBL_1521478 Inhibition of STS activity in human placental microsome in presence of [3H]-estrone sulfate
- ChEMBL_877515 Inhibition of 17beta-HSD1 assessed as conversion of estrone to estradiol by scintillation counting method
- ChEMBL_203039 Inhibition of steroid sulfatase activity of JEG-3 cells by the compound at 20 uM, activity was determined by considering total labeled estrone ([3H]E1) formed from labeled estrone sulfate ([3H]-E1S)
- ChEBML_67985 Inhibitory activity againist Estrone sulfatase from MCF-7 cells (placental microsomes)
- ChEMBL_1577234 Inhibition of estrone sulfatase (unknown origin) transfected in HEK293 cells using E1S as substrate
- ChEMBL_544137 Inhibition of 17beta-HSD1 assessed as conversion of [14C]estradiol to [14C]estrone using NADP+
- ChEMBL_1487742 Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
- ChEMBL_1577236 Reversible inhibition of human estrone sulfatase using 4-methylumbelliferyl sulfate as substrate by fluorimetric assay
- ChEMBL_1577312 Inhibition of recombinant human estrone sulfatase using 4-methylumbelliferyl sulfate as substrate by colorimetric assay
- ChEMBL_514253 Inhibition of human placental 17beta-HSD1 assessed as conversion of [3H]estrone to [3H]17beta-estradiol
- ChEMBL_514254 Inhibition of human placental 17beta-HSD2 assessed as conversion of [3H]17beta-estradiol to [3H]estrone
- ChEMBL_1577229 Inhibition of human placental microsomal estrone sulfatase using [3H]E1S as substrate incubated for 30 mins
- ChEMBL_2057745 Inhibition of OATP1B1 (unknown origin) mediated [3H]-estrone sulfate uptake expressed in human HepG2 cells
- ChEMBL_468301 Inhibition of 17beta-HSD1 in human T47D cells assessed as inhibition of transformation of [14C]-estrone into [14C]estrogen
- ChEMBL_544140 Inhibition of 17beta-HSD1 expressed in HEK 293 cells assessed as conversion of [14C]estrone to [14C]estradiol
- ChEMBL_560809 Inhibition of human aromatase-mediated conversion of [1beta3H]androstenedione to estrone by liquid scintillation counting in presence of NADPH
- ChEMBL_560810 Inhibition of human aromatase-mediated conversion of [1beta3H]androstenedione to estrone by Lineweaver-Burke plot in presence of NADPH
- ChEMBL_684635 Inhibition of human placenta 17beta-HSD1 using [2,4,6,7-3H]-estrone as substrate after 10 mins
- ChEMBL_852704 Inhibition of recombinant 17betaHSD1 using [3H]estrone as substrate after 20 mins by flow scintillation analysis
- ChEMBL_1467094 Inhibition of human OATP1B1-mediated [3H]estrone 3-sulfate at after 5 mins by Dixon plot method
- ChEMBL_1577322 Reversible inhibition of recombinant human estrone sulfatase using 4-methylumbelliferyl sulfate as substrate by Hanes plot analysis
- ChEMBL_555024 Inhibition of human recombinant 17beta-HSD1 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol
- ChEMBL_555026 Inhibition of human recombinant 17beta-HSD2 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol
- ChEMBL_555345 Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol
- ChEMBL_67990 Inhibitory activity against Estrone sulfatase (E1-STS) in MCF-7 breast cancer cells at 0.1 uM
- ChEMBL_684640 Inhibition of 17beta-HSD1 in human T47D cells using [2,4,6,7-3H]-estrone as substrate after 30 mins
- ChEMBL_1552528 Inhibition of human OAT3 expressed in HEK cells assessed as reduction of [3H]-estrone sulfate uptake by radioactivity counting analysis
- ChEMBL_1574256 Inhibition of steroid sulfatase in human JEG-3 cells assessed as [14C]-Estrone formation using [3H]E1S as substrate
- ChEMBL_1577235 Inhibition of recombinant human estrone sulfatase expressed in CHO cells using 4-methylumbelliferyl sulfate as substrate by fluorimetric assay
- ChEMBL_1577237 Reversible inhibition of estrone sulfatase (unknown origin) using 4-methylumbelliferyl sulfate as substrate by Lineweaver-Burk plot analysis
- ChEMBL_544139 Inhibition of 17beta-HSD1 expressed in HEK 293 cells assessed as conversion of [14C]estrone to [14C]estradiol using NADH
- ChEMBL_544141 Inhibition of 17beta-HSD1 expressed in HEK 293 cells assessed as conversion of [14C]estrone to [14C]estradiol using NADPH
- ChEMBL_67991 Tested for inhibition of estrone sulfatase in placental microsomal preparation (100000 g pellet) using substrate concentration of 20 uM
- ChEMBL_1363487 Inhibition of human placental 17beta-HSD2 microsomal fraction using tritiated estradiol as substrate assessed as formation of estrone by HPLC analysis
- ChEMBL_1363489 Inhibition of human placental 17beta-HSD1 cytosolic fraction using tritiated estrone as substrate assessed as formation of estradiol by HPLC analysis
- ChEMBL_1363494 Inhibition of mouse liver 17beta-HSD2 microsomal fraction using tritiated estradiol as substrate assessed as formation of estrone by HPLC analysis
- ChEMBL_1490912 Inhibition of OATP1B1-mediated [3H]estrone-3-sulfate uptake in human OATP1B1 expressing HEK293/PDZK1 cells by scintillation counting
- ChEMBL_1490913 Inhibition of OATP2B1-mediated [3H]estrone-3-sulfate uptake in human OATP2B1 expressing HEK293/PDZK1 cells by scintillation counting
- ChEMBL_1577233 Inhibition of estrone sulfatase in human MCF7 cells using [3H]E1S as substrate incubated for 24 hrs by scintillation counting method
- ChEMBL_1577318 Inhibition of human placental microsomal estrone sulfatase using [3H]E1S as substrate incubated for 20 mins by scintillation counting method
- ChEMBL_1577320 Inhibition of human placental microsomal estrone sulfatase using 4-methylumbelliferyl sulfate as substrate incubated for 1 hr by fluorescence assay
- ChEMBL_1577321 Inhibition of recombinant human estrone sulfatase expressed in CHO cells using 4-methylumbelliferyl sulfate as substrate by Hanes plot analysis
- ChEBML_68195 Estrone-sulfatase activity against homogenized human JEG-3 cells was determined by measuring the [3H]E1 obtained from [3H]E1S
- ChEMBL_619853 Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol after 7 hrs
- ChEMBL_68195 Estrone-sulfatase activity against homogenized human JEG-3 cells was determined by measuring the [3H]E1 obtained from [3H]E1S
- ChEMBL_1337227 Inhibition of human aromatase using androstenedione as substrate assessed as estrone formation at 10 uM after 30 mins by LC-MS/MS analysis
- ChEMBL_1577227 Inhibition of placental microsomal estrone sulfatase (unknown origin) using [6,7-3H]E1S as substrate incubated for 1 hr by scintillation spectrometric analysis
- ChEMBL_321589 Inhibition of 17-beta-hydroxysteroid dehydrogenase type 1 expressed in T47D human breast cancer cells using 2 nM [3H]estrone
- ChEMBL_701686 Displacement of [3H]estrone human recombinant 17beta-HSD1 expressed in Escherichia coli BL21 (DE3)-RIL by scintillation counting in presence of bacterial homogenate
- ChEMBL_1494639 Inhibition of OATP2B1 (unknown origin) expressed in MDCK2 cells assessed as reduction of [3H]estrone-3-sulfate uptake after 3 mins by beta-counting
- ChEMBL_1520470 Inhibition of human placental aromatase assessed as conversion of [1beta-3H]androst-4-ene-3,17-dione to estrone after 15 mins by scintillation counting
- ChEMBL_1577232 Inhibition of estrone sulfatase (unknown origin) transfected in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method
- ChEMBL_1577314 Inhibition of human placental estrone sulfatase expressed in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method
- ChEMBL_1577319 Non-competitive inhibition of human placental microsomal estrone sulfatase using [3H]E1S as substrate incubated for 20 mins by Lineweaver-Burk plot analysis
- ChEMBL_1744044 Inhibition of human 17beta-HSD1 expressed in HEK293 cell lysates incubated for 10 mins using [2,4,6,7-3H]-estrone and NADPH by scintillation counting method
- ChEMBL_202919 Compound was tested for its ability to inhibit human embryonal kidney cell derived steroid sulfatase activity in transforming [3H]E1S (estrone sulfate) to E1
- ChEMBL_587693 Inhibition of human placental aromatase assessed as conversion of [1-beta-3H]androstenedione to [1beta-3H]estrone after 20 mins by liquid scintillation counting
- ChEMBL_701687 Displacement of [3H]estrone human recombinant 17beta-HSD1 expressed in Escherichia coli BL21 (DE3)-RIL by competitive inhibition assay in presence of bacterial homogenate
- ChEMBL_879539 Inhibition of 17beta-HSD1 in human T47D cells assessed as decrease in transformation of [14C]estrone to [14C]-estradiol after 24 hrs by thin layer chromatography
- ChEMBL_1367282 Inhibition of human placental 17beta-HSD1 cytosolic fraction using [2, 4, 6, 7-3H]-estrone as substrate after 10 mins by HPLC analysis
- ChEMBL_861317 Inhibition of human placenta 17beta-HSD1 cytosolic fraction using unlabelled and [2,4,6,7-3H]estrone as substrate after 10 mins by HPLC analysis in presence of NADH
- ChEMBL_988473 Inhibition of human placenta 17beta-HSD1 cytosolic fraction using unlabeled, [2,4,6,7-3H]-estrone as substrate after 20 mins by HPLC analysis in presence of NADH
- ChEMBL_1343606 Apparent inhibition of human placental microsomal aromatase assessed as [C14]estrone/[C14]estradiol formation using 0.075 to 0.515 uM [C14]androstenedione substrate by liquid scintillation counting
- ChEMBL_786680 Inhibition of human placental 17beta-HSD1 using [2,4,6,7-3H]-estrone as substrate after 10 mins by radio flow detector-based HPLC analysis in presence of NADH as cofactor
- ChEMBL_861311 Inhibition of 17beta-HSD1 in human T47D cells using unlabelled and [2,4,6,7-3H]estrone as substrate preincubated for 30 mins prior to substrate addition measured 0.5 hrs post substrate addition
- ChEMBL_786678 Inhibition of human placental 17beta-HSD2 assessed as formation of [2,4,6,7-3H]-estrone using [2,4,6,7-3H]-estradiol as substrate after 20 mins by radio flow detector-based HPLC analysis in presence of NAD+ as cofactor
- Sulfatase Assay The extent of in vitro inhibition of sulfatase activities was assessed using intact monolayers of JEG-3 cells. Sulfatase activity was measured using [6,7-3H] EIS over 3 hrs, determined by measuring the total amount of 3H-labeled estrone and estradiol formed.
- Sulfatase Inhibition Assay The extent of in vitro inhibition of sulfatase activities was assessed using intact monolayers of JEG-3 cells. Sulfatase activity was measured using [6,7-3H] E1S over 3 hrs, determined by measuring the total amount of 3H-labeled estrone and estradiol formed.
- Competition-Based Ligand Binding Assay and Transactivation Assay. Ligand binding was determined using a scintillation proximity assay with streptavidin-coated SPA beads (Amersham) and biotinylated receptor. Receptor-bound [3H]estrone was determined by scintillation counting (Perkin-Elmer). The binding IC50 value (the concentration of compound required for 50% inhibition of [3H]estrone binding to ER was calculated using XL-fit one-site dose response. To determine the agonist activity of the compounds on receptors, the full length receptors were stably expressed under ERE promoter with luciferase as reporter in Hela cells. The transactivation EC50 (the concentration of compound required to achieve 50% of transactivation caused by 10 nM estradiol) was calculated using XL-fit one-site dose response.
- CYP19 Assay Inhibition of human placental aromatase was determined by monitoring the amount of 3H2O released as the enzyme converts [1beta-3H]androst-4-ene-3,17-dione to estrone. The aqueous layer was extracted with chloroform, and the amount of radioactivity was determined by scintillation counting. Each sample was run in triplicate, and background values were determined with microsomal protein inactivated by boiling. Sample containing aminoglutethimide was used as a positive control.
- Enzymatic Assay (Inhibition of Type 1 17beta-HSD) The enzymatic reaction was performed in the reaction buffer containing substrate, [14C]-estrone, and the test inhibitors. After the reaction, radiolabeled steroids were extracted from the reaction mixture, and solvent was evaporated to dryness. Steroids were dissolved and separated on TLC plates. Radioactivity signals were detected and quantified using a PhosphoImager (Sunny Vale, CA). The percentage of transformation of [14C]-E1 into [14C]-E2 was calculated. The IC50 values were calculated using an unweighted iterative least-squares method for four-parameter logistic curve fitting (DE50 program, CHUL Research Center, Quebec).