Target Information
| Target General Information | Top | |||||
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| Target ID |
T22939
(Former ID: TTDS00245)
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| Target Name |
Progesterone receptor (PGR)
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| Synonyms |
PR; Nuclear receptor subfamily 3 group C member 3; NR3C3
Click to Show/Hide
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| Gene Name |
PGR
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 5 Target-related Diseases | + | ||||
| 1 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
| 2 | Contraceptive management [ICD-11: QA21] | |||||
| 3 | Menstrual cycle bleeding disorder [ICD-11: GA20] | |||||
| 4 | Preterm labour/delivery [ICD-11: JB00] | |||||
| 5 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Depending on the isoform, progesterone receptor functions as transcriptional activator or repressor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues.
Click to Show/Hide
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| BioChemical Class |
Nuclear hormone receptor
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| UniProt ID | ||||||
| Sequence |
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF
PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T11OU8 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 12 Approved Drugs | + | ||||
| 1 | Desogestrel | Drug Info | Approved | Contraception | [3], [4] | |
| 2 | Dydrogesterone | Drug Info | Approved | Menstrual disorder | [5], [6] | |
| 3 | Estradiol valerate/dienogest | Drug Info | Approved | Discovery agent | [7] | |
| 4 | Ethynodiol Diacetate | Drug Info | Approved | Contraception | [8], [9] | |
| 5 | Etonogestrel | Drug Info | Approved | Contraception | [4], [10] | |
| 6 | Levonorgestrel | Drug Info | Approved | Contraception | [4], [11] | |
| 7 | Medroxyprogesterone | Drug Info | Approved | Solid tumour/cancer | [7] | |
| 8 | Megestrol | Drug Info | Approved | Breast cancer | [12] | |
| 9 | Norethindrone | Drug Info | Approved | Solid tumour/cancer | [7] | |
| 10 | Norgestimate | Drug Info | Approved | Contraception | [4], [13] | |
| 11 | Progesterone | Drug Info | Approved | Premature labour | [14], [15] | |
| 12 | Segesterone acetate; ethinyl estradiol | Drug Info | Approved | Contraception | [16] | |
| Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
| 1 | Nestorone | Drug Info | Phase 3 | Endometriosis | [18] | |
| 2 | BAY 86-5044 | Drug Info | Phase 2 | Breast cancer | [20] | |
| 3 | MK-8342 | Drug Info | Phase 2 | Contraception | [21] | |
| 4 | ONAPRISTONE | Drug Info | Phase 2 | Breast cancer | [22] | |
| 5 | S-PRAnt | Drug Info | Phase 2 | Uterine fibroids | [23] | |
| 6 | Tosagestin | Drug Info | Phase 2 | Contraception | [24] | |
| 7 | Vilaprisan | Drug Info | Phase 2 | Endometriosis | [25] | |
| 8 | Virexxa | Drug Info | Phase 2 | Endometrial cancer | [26] | |
| 9 | PF-2413873 | Drug Info | Phase 1 | Endometriosis | [27] | |
| Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
| 1 | Org-31710 | Drug Info | Discontinued in Phase 1 | Contraception | [30] | |
| 2 | BAY-39-9624 | Drug Info | Terminated | Osteoporosis | [31] | |
| 3 | RU-46556 | Drug Info | Terminated | Endometrial cancer | [32] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Modulator | [+] 8 Modulator drugs | + | ||||
| 1 | Desogestrel | Drug Info | [33] | |||
| 2 | Estradiol valerate/dienogest | Drug Info | [2] | |||
| 3 | Segesterone acetate; ethinyl estradiol | Drug Info | [16] | |||
| 4 | ONAPRISTONE | Drug Info | [47] | |||
| 5 | Org-31710 | Drug Info | [52] | |||
| 6 | RU-46556 | Drug Info | [54] | |||
| 7 | ZK-112993 | Drug Info | [66] | |||
| 8 | ZK-136798 | Drug Info | [67] | |||
| Agonist | [+] 11 Agonist drugs | + | ||||
| 1 | Dydrogesterone | Drug Info | [34] | |||
| 2 | Medroxyprogesterone | Drug Info | [34] | |||
| 3 | Norethindrone | Drug Info | [42] | |||
| 4 | Norgestimate | Drug Info | [37], [43] | |||
| 5 | Progesterone | Drug Info | [1] | |||
| 6 | Nestorone | Drug Info | [44] | |||
| 7 | MK-8342 | Drug Info | [46] | |||
| 8 | Tosagestin | Drug Info | [49] | |||
| 9 | BAY-39-9624 | Drug Info | [53] | |||
| 10 | GSK-008A | Drug Info | [46] | |||
| 11 | ORG2058 | Drug Info | [46] | |||
| Binder | [+] 4 Binder drugs | + | ||||
| 1 | Ethynodiol Diacetate | Drug Info | [35], [36] | |||
| 2 | Etonogestrel | Drug Info | [37], [38] | |||
| 3 | Levonorgestrel | Drug Info | [39], [40] | |||
| 4 | Megestrol | Drug Info | [41] | |||
| Inhibitor | [+] 17 Inhibitor drugs | + | ||||
| 1 | BAY 86-5044 | Drug Info | [45] | |||
| 2 | 1-Benzyl-3-phenylquinazoline-2,4(1H,3H)-dione | Drug Info | [55] | |||
| 3 | 2-(4-Amino-3'-chloro-biphenyl-3-yl)-propan-2-ol | Drug Info | [56] | |||
| 4 | 3,3-dimethyl-5-m-tolyl-2,3-dihydro-1H-inden-1-one | Drug Info | [57] | |||
| 5 | 3-Phenyl-1-propylquinazoline-2,4(1H,3H)-dione | Drug Info | [55] | |||
| 6 | 4-(2,4-diethyl-1H-pyrrol-3-yloxy)benzonitrile | Drug Info | [58] | |||
| 7 | 5,N-Dihydroxythalidomide | Drug Info | [55] | |||
| 8 | 5-(2-oxoindolin-5-yl)-1H-pyrrole-2-carbonitrile | Drug Info | [59] | |||
| 9 | 6-(3-Nitro-phenyl)-3H-benzothiazol-2-one | Drug Info | [60] | |||
| 10 | AL-43 | Drug Info | [61] | |||
| 11 | GSK-1564023A | Drug Info | [62] | |||
| 12 | GSK-325971A | Drug Info | [62] | |||
| 13 | Lecanindole D | Drug Info | [64] | |||
| 14 | LGD-5552 | Drug Info | [65] | |||
| 15 | PF-02367982 | Drug Info | [58] | |||
| 16 | WAY-255348 | Drug Info | [59] | |||
| 17 | [3H]methyltrienolone | Drug Info | [68] | |||
| Antagonist | [+] 4 Antagonist drugs | + | ||||
| 1 | S-PRAnt | Drug Info | [48] | |||
| 2 | Vilaprisan | Drug Info | [7], [50] | |||
| 3 | PF-2413873 | Drug Info | [51] | |||
| 4 | GTPL8662 | Drug Info | [63] | |||
| Inducer | [+] 1 Inducer drugs | + | ||||
| 1 | Virexxa | Drug Info | [46] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Norethindrone | Ligand Info | |||||
| Structure Description | Progesterone Receptor Ligand Binding Domain with bound Norethindrone | PDB:1SQN | ||||
| Method | X-ray diffraction | Resolution | 1.45 Å | Mutation | No | [42] |
| PDB Sequence |
QLIPPLINLL
691 MSIEPDVIYA701 GHDNPDTSSS713 LLTSLNQLGE723 RQLLSVVKWS733 KSLPGFRNLH 743 IDDQITLIQY753 SWMSLMVFGL763 GWRSYKHVSG773 QMLYFAPDLI783 LNEQRMKESS 793 FYSLCLTMWQ803 IPQEFVKLQV813 SQEEFLCMKV823 LLLLNTIPLE833 GLRSQTQFEE 843 MRSSYIRELI853 KAIGLRQGVV864 SSSQRFYQLT874 KLLDNLHDLV884 KQLHLYCLNT 894 FIQSRALSVE904 FPEMMSEVIA914 AQLPKILAGM924 VKPLLFHK
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LEU715
3.352
LEU718
3.657
ASN719
3.650
LEU721
3.786
GLY722
4.286
GLN725
2.950
TRP755
4.468
MET756
3.795
MET759
3.591
VAL760
4.002
LEU763
4.112
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| Ligand Name: Mifepristone | Ligand Info | |||||
| Structure Description | RU486 bound to the progesterone receptor in a destabilized agonistic conformation | PDB:2W8Y | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [69] |
| PDB Sequence |
LIPPLINLLM
692 SIEPDVIYAG702 HDNTKPDTSS712 SLLTSLNQLG722 ERQLLSVVKW732 SKSLPGFRNL 742 HIDDQITLIQ752 YSWMSLMVFG762 LGWRSYKHVS772 GQMLYFAPDL782 ILNEQRMKES 792 SFYSLCLTMW802 QIPQEFVKLQ812 VSQEEFLCMK822 VLLLLNTIPL832 EGLRSQTQFE 842 EMRSSYIREL852 IKAIGLRQKG862 VVSSSQRFYQ872 LTKLLDNLHD882 LVKQLHLYCL 892 NTFIQSRALS902 VEFPEMMSEV912 IAAQLPKILA922 GMVKPLLFHK932 K |
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LEU715
3.133
LEU718
3.569
ASN719
3.221
LEU721
3.639
GLY722
3.605
GLU723
3.503
GLN725
2.735
LEU726
3.982
TRP755
3.162
MET756
3.668
MET759
3.511
VAL760
4.080
LEU763
4.287
ARG766
2.884
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Oocyte meiosis | hsa04114 | Affiliated Target |
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| Class: Cellular Processes => Cell growth and death | Pathway Hierarchy | ||
| Progesterone-mediated oocyte maturation | hsa04914 | Affiliated Target |
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| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Estrogen signaling pathway | hsa04915 | Affiliated Target |
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| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Degree | 11 | Degree centrality | 1.18E-03 | Betweenness centrality | 6.54E-05 |
|---|---|---|---|---|---|
| Closeness centrality | 2.49E-01 | Radiality | 1.43E+01 | Clustering coefficient | 3.64E-01 |
| Neighborhood connectivity | 7.55E+01 | Topological coefficient | 1.40E-01 | Eccentricity | 11 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Oocyte meiosis | |||||
| 2 | Progesterone-mediated oocyte maturation | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | Cellular roles of Anthrax toxin | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Nuclear signaling by ERBB4 | |||||
| 2 | Nuclear Receptor transcription pathway | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Ovarian Infertility Genes | |||||
| 2 | Signaling by ERBB4 | |||||
| 3 | Nuclear Receptors | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Clinical pipeline report, company report or official report of lipocine. | |||||
| REF 2 | Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. | |||||
| REF 3 | 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: 7065). | |||||
| REF 4 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 5 | 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: 2878). | |||||
| REF 6 | Drug information of Dydrogesterone, 2008. eduDrugs. | |||||
| REF 7 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 8 | 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: 7072). | |||||
| REF 9 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018168. | |||||
| REF 10 | 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: 7590). | |||||
| REF 11 | 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: 2881). | |||||
| REF 12 | Hormonal therapy in epithelial ovarian cancer. Expert Rev Anticancer Ther. 2006 Jan;6(1):43-7. | |||||
| REF 13 | 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: 7091). | |||||
| REF 14 | 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: 2377). | |||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038483) | |||||
| REF 16 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 17 | ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health. | |||||
| REF 18 | ClinicalTrials.gov (NCT00455156) Study of the Safety, Efficacy and Cycle Control of a Contraceptive Vaginal Ring. U.S. National Institutes of Health. | |||||
| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014404) | |||||
| REF 20 | ClinicalTrials.gov (NCT00555919) ZK 230211 in Postmenopausal Woman With Metastatic Breast Cancer. U.S. National Institutes of Health. | |||||
| REF 21 | Clinical pipeline report, company report or official report of Merck (May 7, 2015). | |||||
| REF 22 | Clinical pipeline report, company report or official report of Context Therapeutics. | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033040) | |||||
| REF 24 | Excretion balance and metabolism of the progestagen Org 30659 in healthy postmenopausal women. J Steroid Biochem Mol Biol. 2000 May;73(1-2):39-48. | |||||
| REF 25 | ClinicalTrials.gov (NCT02465814) Assess Safety and Efficacy of Vilaprisan in Patients With Uterine Fibroids. | |||||
| REF 26 | ClinicalTrials.gov (NCT02064725) Virexxa (Sodium Cridanimod) w/Progestin Therapy in Pts w/Progesterone Receptor Neg Recurrent/Persistent Endometrial CA. U.S. National Institutes of Health. | |||||
| REF 27 | ClinicalTrials.gov (NCT00800618) A Study To Investigate How The Body Handles Multiple Doses Of PF-0243873 And To Investigate The Effect Of PF-02413873 On Sex Hormone Levels In Healthy Young Women. U.S. National Institutes of Health. | |||||
| REF 28 | 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: 2883). | |||||
| REF 29 | New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. | |||||
| REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002550) | |||||
| REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014491) | |||||
| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003252) | |||||
| REF 33 | Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40. | |||||
| REF 34 | Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharm... Steroids. 2008 Feb;73(2):222-31. | |||||
| REF 35 | Contribution of functional groups of 19-nor-progestogens to binding to progesterone and estradiol-17beta receptors in rabbit uterus. Endocrinology. 1977 Jun;100(6):1579-84. | |||||
| REF 36 | The place of progestational hormones in gynecological therapy. Ginekol Pol. 1970 May;41(5):497-502. | |||||
| REF 37 | Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7. | |||||
| REF 38 | Endometrial effects of etonogestrel (Implanon) contraceptive implant. Curr Opin Obstet Gynecol. 2001 Jun;13(3):335-41. | |||||
| REF 39 | Met909 plays a key role in the activation of the progesterone receptor and also in the high potency of 13-ethyl progestins. Mol Pharmacol. 2009 Jun;75(6):1317-24. | |||||
| REF 40 | Toll-like receptor-4-mediated macrophage activation is differentially regulated by progesterone via the glucocorticoid and progesterone receptors. Immunology. 2008 Sep;125(1):59-69. | |||||
| REF 41 | Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8. | |||||
| REF 42 | Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes. J Med Chem. 2004 Jun 17;47(13):3381-7. | |||||
| REF 43 | A review of transdermal hormonal contraception : focus on the ethinylestradiol/norelgestromin contraceptive patch. Treat Endocrinol. 2006;5(6):359-65. | |||||
| REF 44 | Efficacy of the selective progesterone receptor agonist Nestorone for chronic experimental autoimmune encephalomyelitis. J Neuroimmunol. 2014 Nov 15;276(1-2):89-97. | |||||
| REF 45 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6. | |||||
| REF 46 | 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. (Target id: 627). | |||||
| REF 47 | Onapristone, a progesterone receptor antagonist, as first-line therapy in primary breast cancer. Eur J Cancer. 1999 Feb;35(2):214-8. | |||||
| REF 48 | BAY 1002670: a novel, highly potent and selective progesterone receptor modulator for gynaecological therapies. Hum Reprod. 2013 Aug;28(8):2253-64. | |||||
| REF 49 | Effects of progestins on the proliferation of estrogen-dependent human breast cancer cells under growth factor-defined conditions. J Steroid Biochem Mol Biol. 1992 Jun;42(5):457-65. | |||||
| REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033939) | |||||
| REF 51 | Unusual base-catalyzed exchange in the synthesis of deuterated PF-2413873. Journal of Labelled Compounds. 08/2009; 52(10):435 - 442. | |||||
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