Target Information
Target General Infomation | |||||
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Target ID |
T22939
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Former ID |
TTDS00245
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Target Name |
Progesterone receptor
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Gene Name |
PGR
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Synonyms |
PR; PGR
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Target Type |
Successful
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Disease | Advanced breast carcinoma; Advanced endometrium carcinoma [ICD9: 174, 175, 182.0; ICD10: C50, C54.1] | ||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Contraception [ICD10: Z30] | |||||
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6] | |||||
Estrogen deficiency [ICD10: E28.39] | |||||
Endometrial cancer [ICD9: 182; ICD10: C54.1] | |||||
Endometriosis [ICD9: 617; ICD10: N80] | |||||
Female contraception [ICD10: Z30] | |||||
Gynecological disorder [ICD10: N70-N98] | |||||
Hormonal contraceptives [ICD10: Z30] | |||||
Menstrual disorders [ICD9: 626; ICD10: N91-N95] | |||||
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890] | |||||
Premature labour [ICD9: 644, 765; ICD10: O60.1, P07.3] | |||||
Uterine leiomyoma [ICD9: 218.9; ICD10: D25] | |||||
Uterine fibroids [ICD10: D25] | |||||
Unspecified [ICD code not available] | |||||
Function |
Isoform 4: Increases mitochondrial membrane potential and cellular respiration upon stimulation by progesterone.
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BioChemical Class |
Zinc-finger
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Target Validation |
T22939
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UniProt ID | |||||
Sequence |
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF
PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK |
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Drugs and Mode of Action | |||||
Drug(s) | Desogestrel | Drug Info | Approved | Hormonal contraceptives | [1], [2] |
Dydrogesterone | Drug Info | Approved | Menstrual disorders | [3], [4] | |
Estradiol valerate/dienogest | Drug Info | Approved | Unspecified | [5] | |
Ethynodiol Diacetate | Drug Info | Approved | Hormonal contraceptives | [6], [7] | |
Etonogestrel | Drug Info | Approved | Female contraception | [1], [8] | |
Levonorgestrel | Drug Info | Approved | Hormonal contraceptives | [1], [9] | |
Medroxyprogesterone | Drug Info | Approved | Cancer | [5] | |
Megestrol | Drug Info | Approved | Advanced breast carcinoma; Advanced endometrium carcinoma | [10] | |
Norethindrone | Drug Info | Approved | Cancer | [5] | |
Norgestimate | Drug Info | Approved | Hormonal contraceptives | [1], [11] | |
Norgestrel | Drug Info | Approved | Contraception | [12], [5] | |
Progesterone | Drug Info | Approved | Premature labour | [13], [14] | |
Ulipristal | Drug Info | Approved | Contraception | [15] | |
Nestorone transdermal spray | Drug Info | Phase 3 | Endometriosis | [16] | |
NPC-01 | Drug Info | Phase 3 | Dysmenorrhea | [17] | |
Androgen restored contraceptive | Drug Info | Phase 2 | Contraception | [18] | |
MK-8342 | Drug Info | Phase 2 | Contraception | [19] | |
S-PRAnt | Drug Info | Phase 2 | Uterine leiomyoma | [20] | |
Telapristone | Drug Info | Phase 2 | Endometriosis | [21] | |
Tosagestin | Drug Info | Phase 2 | Contraception | [22] | |
Vilaprisan | Drug Info | Phase 2 | Endometriosis | [23] | |
Virexxa | Drug Info | Phase 2 | Endometrial cancer | [24] | |
ONAPRISTONE | Drug Info | Phase 1/2 | Contraception | [25], [26] | |
PF-2413873 | Drug Info | Phase 1 | Endometriosis | [27] | |
Asoprisnil | Drug Info | Discontinued in Phase 3 | Endometriosis | [28], [29] | |
Org-31710 | Drug Info | Discontinued in Phase 1 | Contraception | [30] | |
BAY-39-9624 | Drug Info | Terminated | Osteoporosis | [31] | |
RU-46556 | Drug Info | Terminated | Endometrial cancer | [32] | |
Inhibitor | 1-Benzyl-3-phenylquinazoline-2,4(1H,3H)-dione | Drug Info | [33] | ||
2,2,4-Trimethyl-6-phenyl-1,2-dihydro-quinoline | Drug Info | [34] | |||
2-(4-Amino-3'-chloro-biphenyl-3-yl)-propan-2-ol | Drug Info | [35] | |||
3,3-dimethyl-5-m-tolyl-2,3-dihydro-1H-inden-1-one | Drug Info | [36] | |||
3-(3,3-dimethyl-2-oxoindolin-5-yl)benzonitrile | Drug Info | [37] | |||
3-Phenyl-1-propylquinazoline-2,4(1H,3H)-dione | Drug Info | [33] | |||
4-(2,4-diethyl-1H-pyrrol-3-yloxy)benzonitrile | Drug Info | [38] | |||
5,N-Dihydroxythalidomide | Drug Info | [33] | |||
5-(2-oxoindolin-5-yl)-1H-pyrrole-2-carbonitrile | Drug Info | [37] | |||
6-(3-Nitro-phenyl)-3H-benzothiazol-2-one | Drug Info | [39] | |||
AL-43 | Drug Info | [40] | |||
GSK-1564023A | Drug Info | [41] | |||
GSK-325971A | Drug Info | [41] | |||
Lecanindole D | Drug Info | [42] | |||
LGD-5552 | Drug Info | [43] | |||
Methyltrienolone | Drug Info | [44] | |||
PF-02367982 | Drug Info | [38] | |||
Tanaproget | Drug Info | [45] | |||
WAY-255348 | Drug Info | [37] | |||
ZK-230211 | Drug Info | [46] | |||
Agonist | Androgen restored contraceptive | Drug Info | [47] | ||
BAY-39-9624 | Drug Info | [48] | |||
Dydrogesterone | Drug Info | [49] | |||
GSK-008A | Drug Info | [50] | |||
Medroxyprogesterone | Drug Info | [49] | |||
MK-8342 | Drug Info | [50] | |||
Nestorone transdermal spray | Drug Info | [51] | |||
Norethindrone | Drug Info | [52] | |||
Norgestimate | Drug Info | [53], [54] | |||
Norgestrel | Drug Info | [55] | |||
NPC-01 | Drug Info | [17] | |||
ORG2058 | Drug Info | [50] | |||
Progesterone | Drug Info | [56] | |||
Tosagestin | Drug Info | [57] | |||
[3H]ORG2058 | Drug Info | [50] | |||
Antagonist | APR19 | Drug Info | [58] | ||
PF-2413873 | Drug Info | [59] | |||
S-PRAnt | Drug Info | [60] | |||
Telapristone | Drug Info | [61] | |||
Vilaprisan | Drug Info | [62], [5] | |||
Modulator | Asoprisnil | Drug Info | [28] | ||
Desogestrel | Drug Info | [63] | |||
Estradiol valerate/dienogest | Drug Info | [15] | |||
ONAPRISTONE | Drug Info | ||||
Org-31710 | Drug Info | [64] | |||
RU-46556 | Drug Info | [65] | |||
SPRMs, oral, uterine fibroids, Tokai Pharmaceuticals | Drug Info | [50] | |||
Ulipristal | Drug Info | [15] | |||
ZK-112993 | Drug Info | ||||
ZK-114043 | Drug Info | ||||
ZK-136798 | Drug Info | ||||
Binder | Ethynodiol Diacetate | Drug Info | [66], [67] | ||
Etonogestrel | Drug Info | [68], [54] | |||
Levonorgestrel | Drug Info | [69] | |||
Megestrol | Drug Info | [70] | |||
Inducer | Virexxa | Drug Info | [50] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Oocyte meiosis | ||||
Progesterone-mediated oocyte maturation | |||||
Pathway Interaction Database | Cellular roles of Anthrax toxin | ||||
Reactome | Nuclear signaling by ERBB4 | ||||
Nuclear Receptor transcription pathway | |||||
WikiPathways | Ovarian Infertility Genes | ||||
Signaling by ERBB4 | |||||
Nuclear Receptors | |||||
References | |||||
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REF 3 | (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: 2878). | ||||
REF 4 | Drug information of Dydrogesterone, 2008. eduDrugs. | ||||
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REF 9 | (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: 2881). | ||||
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REF 12 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017031. | ||||
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REF 23 | ClinicalTrials.gov (NCT02465814) Assess Safety and Efficacy of Vilaprisan in Patients With Uterine Fibroids. | ||||
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REF 25 | ClinicalTrials.gov (NCT02049190) Phase 1-2 Study of Onapristone in Patients With Advanced Castration-resistant Prostate Cancer. U.S. National Institutes of Health. | ||||
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