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
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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.
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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 | |||||
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| Approved Drug(s) | [+] 13 Approved Drugs | + | ||||
| 1 | Desogestrel | Drug Info | Approved | Contraception | [2], [3] | |
| 2 | Dydrogesterone | Drug Info | Approved | Menstrual disorder | [4], [5] | |
| 3 | Estradiol valerate/dienogest | Drug Info | Approved | Discovery agent | [6] | |
| 4 | Ethynodiol Diacetate | Drug Info | Approved | Contraception | [7], [8] | |
| 5 | Etonogestrel | Drug Info | Approved | Contraception | [3], [9] | |
| 6 | Levonorgestrel | Drug Info | Approved | Contraception | [3], [10] | |
| 7 | Medroxyprogesterone | Drug Info | Approved | Solid tumour/cancer | [6] | |
| 8 | Megestrol | Drug Info | Approved | Breast cancer | [11] | |
| 9 | Norethindrone | Drug Info | Approved | Solid tumour/cancer | [6] | |
| 10 | Norgestimate | Drug Info | Approved | Contraception | [3], [12] | |
| 11 | Progesterone | Drug Info | Approved | Premature labour | [13], [14] | |
| 12 | Segesterone acetate; ethinyl estradiol | Drug Info | Approved | Contraception | [15] | |
| 13 | Ulipristal | Drug Info | Approved | Contraception | [16] | |
| Clinical Trial Drug(s) | [+] 11 Clinical Trial Drugs | + | ||||
| 1 | Nestorone | Drug Info | Phase 3 | Endometriosis | [17] | |
| 2 | NPC-01 | Drug Info | Phase 3 | Dysmenorrhea | [18] | |
| 3 | BAY 86-5044 | Drug Info | Phase 2 | Breast cancer | [19] | |
| 4 | MK-8342 | Drug Info | Phase 2 | Contraception | [20] | |
| 5 | ONAPRISTONE | Drug Info | Phase 2 | Breast cancer | [21] | |
| 6 | S-PRAnt | Drug Info | Phase 2 | Uterine fibroids | [22] | |
| 7 | Telapristone | Drug Info | Phase 2 | Endometriosis | [23] | |
| 8 | Tosagestin | Drug Info | Phase 2 | Contraception | [24] | |
| 9 | Vilaprisan | Drug Info | Phase 2 | Endometriosis | [25] | |
| 10 | Virexxa | Drug Info | Phase 2 | Endometrial cancer | [26] | |
| 11 | PF-2413873 | Drug Info | Phase 1 | Endometriosis | [27] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | Asoprisnil | Drug Info | Discontinued in Phase 3 | Endometriosis | [28], [29] | |
| 2 | Org-31710 | Drug Info | Discontinued in Phase 1 | Contraception | [30] | |
| 3 | BAY-39-9624 | Drug Info | Terminated | Osteoporosis | [31] | |
| 4 | RU-46556 | Drug Info | Terminated | Endometrial cancer | [32] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Modulator | [+] 11 Modulator drugs | + | ||||
| 1 | Desogestrel | Drug Info | [33] | |||
| 2 | Estradiol valerate/dienogest | Drug Info | [16] | |||
| 3 | Segesterone acetate; ethinyl estradiol | Drug Info | [15] | |||
| 4 | Ulipristal | Drug Info | [16] | |||
| 5 | ONAPRISTONE | Drug Info | [47] | |||
| 6 | Asoprisnil | Drug Info | [29] | |||
| 7 | Org-31710 | Drug Info | [53] | |||
| 8 | RU-46556 | Drug Info | [55] | |||
| 9 | ZK-112993 | Drug Info | [69] | |||
| 10 | ZK-114043 | Drug Info | [70] | |||
| 11 | ZK-136798 | Drug Info | [71] | |||
| Agonist | [+] 12 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 | NPC-01 | Drug Info | [18] | |||
| 8 | MK-8342 | Drug Info | [46] | |||
| 9 | Tosagestin | Drug Info | [50] | |||
| 10 | BAY-39-9624 | Drug Info | [54] | |||
| 11 | GSK-008A | Drug Info | [46] | |||
| 12 | 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 | [+] 20 Inhibitor drugs | + | ||||
| 1 | BAY 86-5044 | Drug Info | [45] | |||
| 2 | 1-Benzyl-3-phenylquinazoline-2,4(1H,3H)-dione | Drug Info | [56] | |||
| 3 | 2,2,4-Trimethyl-6-phenyl-1,2-dihydro-quinoline | Drug Info | [57] | |||
| 4 | 2-(4-Amino-3'-chloro-biphenyl-3-yl)-propan-2-ol | Drug Info | [58] | |||
| 5 | 3,3-dimethyl-5-m-tolyl-2,3-dihydro-1H-inden-1-one | Drug Info | [59] | |||
| 6 | 3-(3,3-dimethyl-2-oxoindolin-5-yl)benzonitrile | Drug Info | [60] | |||
| 7 | 3-Phenyl-1-propylquinazoline-2,4(1H,3H)-dione | Drug Info | [56] | |||
| 8 | 4-(2,4-diethyl-1H-pyrrol-3-yloxy)benzonitrile | Drug Info | [61] | |||
| 9 | 5,N-Dihydroxythalidomide | Drug Info | [56] | |||
| 10 | 5-(2-oxoindolin-5-yl)-1H-pyrrole-2-carbonitrile | Drug Info | [60] | |||
| 11 | 6-(3-Nitro-phenyl)-3H-benzothiazol-2-one | Drug Info | [62] | |||
| 12 | AL-43 | Drug Info | [63] | |||
| 13 | GSK-1564023A | Drug Info | [64] | |||
| 14 | GSK-325971A | Drug Info | [64] | |||
| 15 | Lecanindole D | Drug Info | [66] | |||
| 16 | LGD-5552 | Drug Info | [67] | |||
| 17 | PF-02367982 | Drug Info | [61] | |||
| 18 | Tanaproget | Drug Info | [68] | |||
| 19 | WAY-255348 | Drug Info | [60] | |||
| 20 | [3H]methyltrienolone | Drug Info | [72] | |||
| Antagonist | [+] 5 Antagonist drugs | + | ||||
| 1 | S-PRAnt | Drug Info | [48] | |||
| 2 | Telapristone | Drug Info | [49] | |||
| 3 | Vilaprisan | Drug Info | [6], [51] | |||
| 4 | PF-2413873 | Drug Info | [52] | |||
| 5 | GTPL8662 | Drug Info | [65] | |||
| Inducer | [+] 1 Inducer drugs | + | ||||
| 1 | Virexxa | Drug Info | [46] | |||
| 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 | |||||
|---|---|---|---|---|---|---|
| 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 | 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 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 4 | 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 5 | Drug information of Dydrogesterone, 2008. eduDrugs. | |||||
| REF 6 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 7 | 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 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018168. | |||||
| REF 9 | 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 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: 2881). | |||||
| REF 11 | Hormonal therapy in epithelial ovarian cancer. Expert Rev Anticancer Ther. 2006 Jan;6(1):43-7. | |||||
| REF 12 | 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 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: 2377). | |||||
| REF 14 | 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 15 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 16 | Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. | |||||
| REF 17 | ClinicalTrials.gov (NCT00455156) Study of the Safety, Efficacy and Cycle Control of a Contraceptive Vaginal Ring. U.S. National Institutes of Health. | |||||
| REF 18 | ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health. | |||||
| REF 19 | ClinicalTrials.gov (NCT00555919) ZK 230211 in Postmenopausal Woman With Metastatic Breast Cancer. U.S. National Institutes of Health. | |||||
| REF 20 | Clinical pipeline report, company report or official report of Merck (May 7, 2015). | |||||
| REF 21 | Clinical pipeline report, company report or official report of Context Therapeutics. | |||||
| REF 22 | 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 23 | 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 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 | In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88. | |||||
| REF 50 | 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 51 | 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 52 | Unusual base-catalyzed exchange in the synthesis of deuterated PF-2413873. Journal of Labelled Compounds. 08/2009; 52(10):435 - 442. | |||||
| REF 53 | Progesterone receptor antagonists Org 31710 and RU 486 increase apoptosis in human periovulatory granulosa cells. Fertil Steril. 2001 Dec;76(6):1225-31. | |||||
| REF 54 | Bayer is seeking an exclusive licensee for its end-of-Phase I progestinagonist Bay 39-9624. Thepharmaletter. 29-04-2002. | |||||
| REF 55 | New analogues of mifepristone with more dissociated antiprogesterone activities. J Steroid Biochem. 1989;34(1-6):413-7. | |||||
| REF 56 | Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton. Bioorg Med Chem. 2008 Jul 15;16(14):7046-54. | |||||
| REF 57 | Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore. J Med Chem. 1998 Aug 27;41(18):3461-6. | |||||
| REF 58 | Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines. Bioorg Med Chem Lett. 2002 Mar 11;12(5):787-90. | |||||
| REF 59 | 5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6666-9. | |||||
| REF 60 | Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-... J Med Chem. 2008 Mar 27;51(6):1861-73. | |||||
| REF 61 | Optimisation of a pyrazole series of progesterone antagonists; Part 1. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3384-6. | |||||
| REF 62 | Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading... J Med Chem. 2005 Aug 11;48(16):5092-5. | |||||
| REF 63 | Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dih... J Med Chem. 2003 Mar 13;46(6):1016-30. | |||||
| REF 64 | The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2340-3. | |||||
| REF 65 | A new strategy for selective targeting of progesterone receptor with passive antagonists. Mol Endocrinol. 2013 Jun;27(6):909-24. | |||||
| REF 66 | The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. J Nat Prod. 2009 Nov;72(11):1944-8. | |||||
| REF 67 | Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. | |||||
| REF 68 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 69 | Tumor-inhibiting potential of ZK 112.993, a new progesterone antagonist, in hormone-sensitive, experimental rodent and human mammary tumors.Anticancer Res.1990 May-Jun;10(3):683-7. | |||||
| REF 70 | Progesterone inhibits glucocorticoid-dependent aromatase induction in human adipose fibroblasts. J Endocrinol. 1998 Sep;158(3):401-7. | |||||
| REF 71 | The antiovulatory activity of progesterone antagonists is not correlated to their antiprogestational potency in the rat. J Steroid Biochem Mol Biol. 1996 Sep;59(1):75-82. | |||||
| REF 72 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
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