Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM5T6US)

Drug Name
Estrone Drug Info
Synonyms
Aquacrine; Crinovaryl; Cristallovar; Crystogen; Destrone; Disynformon; Endofolliculina; Esterone; Estrin; Estrol; Estron; Estrona; Estronum; Estrovarin; Estrugenone; Estrusol; Femidyn; Fermidyn; Folikrin; Folipex; Folisan; Follestrine; Follestrol; Folliculin; Folliculine; Follicunodis; Glandubolin; Hiestrone; Hormestrin; Hormofollin; Hormovarine; Kestrone; Ketodestrin; Ketohydroxyestrin; Ketohydroxyoestrin; Ketophydroxyestrin; Kolpon; Menagen; Menformon; Mestronaq; OESTRONE; Oestrin; Oestroform; Oestronum; Oestroperos; Ovifollin; Perlatan; Solliculin; Theelin; Thelestrin; Thelykinin; Thynestron; Tokokin; Unden; Unigen; Wehgen; Wynestron; Estrogenic Substance; Estrona [Spanish]; Femestrone injection; Follicular hormone; Folliculine benzoate; Hauck Brand of Estrone; Hyrex Brand of Estrone; Menformon A; Oestrone [Steroidal oestrogens]; Penncap M; Vortech Brand of Estrone; WynestronPencap M; CMC_13458; E 9750; E0026; E(sub 1); Estrona [INN-Spanish]; Estrone (E1); Estrone (TN); Estrone [USAN:INN]; Estrone-A; Estronum [INN-Latin]; Femestrone inj.; Ketohydroxy-Estratriene; NATURAL ESTROGENIC SUBSTANCE-ESTRONE; Oestrone, Estrone; Ovex (tablets); Unden (pharmaceutical); Unden (pharmaceutical) (VAN); Estrone (JAN/USP/INN); Estrone, (8 alpha)-Isomer; Estrone, (9 beta)-Isomer; Estrone, (+-)-Isomer; [2,4,6,7-3H]-E1; Delta-1,3,5-Estratrien-3beta-ol-17-one; Delta-1,3,5-Oestratrien-3beta-ol-17-one; Delta-1,3,5-estratrien-3-beta-ol-17-one; Delta-1,3,5-oestratrien-3-beta-ol-17-one; (13S)-3-hydroxy-13-methyl-7,8,9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthren-17(14H)-one; (8R,9S,13S,14S)-3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one; 1,3,5(10)-Estratrien-3-ol-17-one; 1,3,5(10)-Oestratrien-3-ol-17-one; 3-Hydroxy-1,3,5(10)-estratrien-17-one; 3-Hydroxy-17-keto-estra-1,3,5-triene; 3-Hydroxy-17-keto-oestra-1,3,5-triene; 3-Hydroxy-oestra-1,3,5(10)-trien-17-one; 3-Hydroxyestra-1,3,5(10)-trien-17-one; 3-Hydroxyestra-1,3,5(10)-triene-17-one; 3-hydroxy-estra-1,3,5(10)-trien-17-one
Indication
Disease Entry ICD 11 Status REF
Acne vulgaris ED80 Approved [1]
Menopausal and postmenopausal disorder GA30 Approved [2]
Therapeutic Class
Antimenopausal Agents
Cross-matching ID
PubChem CID
5870
ChEBI ID
CHEBI:17263
CAS Number
CAS 53-16-7
TTD Drug ID
DM5T6US
VARIDT Drug ID
DR00494
INTEDE Drug ID
DR0648

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Estrogen receptor (ESR) TTZAYWL ESR1_HUMAN Agonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [5]
Cytochrome P450 2E1 (CYP2E1) DEVDYN7 CP2E1_HUMAN Approved [6]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [7]
Cytochrome P450 1A1 (CYP1A1) DE6OQ3W CP1A1_HUMAN Approved [8]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Approved [9]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [10]
Cytochrome P450 1B1 (CYP1B1) DE9QHP6 CP1B1_HUMAN Approved [8]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [11]
Estradiol 17-beta-dehydrogenase 2 (HSD17B2) DEBMFZ8 DHB2_HUMAN Approved [12]
Keto-steroid reductase (HSD17B7) DEDMWFX DHB7_HUMAN Approved [12]
Farnesol dehydrogenase (AKR1B15) DER0XCH AK1BF_HUMAN Approved [13]
Lauric acid omega-hydroxylase (CYP4A11) DE2XQGW CP4AB_HUMAN Approved [11]
Peroxisomal multifunctional enzyme 2 (HSD17B4) DEJHG19 DHB4_HUMAN Approved [12]
Ketoacyl-CoA reductase (HSD17B12) DE915QP DHB12_HUMAN Approved [14]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Estrogen receptor (ESR) DTT ESR1 3.728 3.17 4.897 4.505
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 12.054 3.968 2.945 4.1
Peroxisomal multifunctional enzyme 2 (HSD17B4) DME HSD17B4 9.491 7.489 7.983 8.154
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Keto-steroid reductase (HSD17B7) DME HSD17B7 7.559 6.401 6.14 7.096
Estradiol 17-beta-dehydrogenase 2 (HSD17B2) DME HSD17B2 9.546 8.31 4.358 10.177
Cytochrome P450 1B1 (CYP1B1) DME CYP1B1 5.098 5.256 8.133 6.2
Ketoacyl-CoA reductase (HSD17B12) DME HSD17B12 9.224 8.977 9.128 8.66
Cytochrome P450 1A1 (CYP1A1) DME CYP1A1 5.952 6.384 4.897 6.293
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Lauric acid omega-hydroxylase (CYP4A11) DME CYP4A11 9.415 5.236 7.84 6.152
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Acne vulgaris
ICD Disease Classification ED80
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
P-glycoprotein 1 (ABCB1) DTP P-GP 7.23E-01 -8.20E-02 -3.22E-01
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 7.75E-01 -1.76E-01 -6.23E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 3.97E-02 -1.72E-01 -9.29E-01
Peroxisomal multifunctional enzyme 2 (HSD17B4) DME HSD17B4 7.65E-01 -2.57E-02 -1.57E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 9.96E-01 -7.53E-02 -5.68E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 5.82E-01 -6.00E-02 -2.69E-01
Keto-steroid reductase (HSD17B7) DME HSD17B7 1.13E-01 -1.66E-01 -4.75E-01
Estradiol 17-beta-dehydrogenase 2 (HSD17B2) DME HSD17B2 9.57E-01 -3.67E-03 -2.48E-02
Cytochrome P450 1B1 (CYP1B1) DME CYP1B1 6.91E-03 2.71E-01 1.34E+00
Ketoacyl-CoA reductase (HSD17B12) DME HSD17B12 7.76E-01 -1.30E-01 -2.17E-01
Cytochrome P450 1A1 (CYP1A1) DME CYP1A1 5.01E-01 -1.01E-02 -6.05E-02
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 9.09E-01 -9.26E-02 -3.68E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 9.85E-01 2.24E-02 7.33E-02
Lauric acid omega-hydroxylase (CYP4A11) DME CYP4A11 7.58E-02 -1.17E-01 -8.85E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Estrone FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2818).
3 Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
4 P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm Res. 2004 Jul;21(7):1284-93.
5 Regioselective hydroxylation of steroid hormones by human cytochromes P450. Drug Metab Rev. 2015 May;47(2):89-110.
6 Novel metabolic pathway of estrone and 17beta-estradiol catalyzed by cytochrome P-450. Drug Metab Dispos. 2000 Feb;28(2):110-2.
7 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
8 A common CYP1B1 polymorphism is associated with 2-OHE1/16-OHE1 urinary estrone ratio. Clin Chem Lab Med. 2005;43(7):702-6.
9 A transgenic mouse expressing human CYP1A2 in the pancreas. Biochem Pharmacol. 2000 Sep 15;60(6):857-63.
10 16Alpha-hydroxylation of estrone by human cytochrome P4503A4/5. Carcinogenesis. 1998 May;19(5):867-72.
11 Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
12 Steroid signalling in the ovarian surface epithelium. Trends Endocrinol Metab. 2005 Sep;16(7):327-33.
13 Aldo-keto Reductase 1B15 (AKR1B15): a mitochondrial human aldo-keto reductase with activity toward steroids and 3-keto-acyl-CoA conjugates. J Biol Chem. 2015 Mar 6;290(10):6531-45.
14 Characterization of type 12 17beta-hydroxysteroid dehydrogenase, an isoform of type 3 17beta-hydroxysteroid dehydrogenase responsible for estradiol formation in women. Mol Endocrinol. 2006 Feb;20(2):437-43.