Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00245

Target Information
NameProgesterone receptor    
Type of targetSuccessful target    
DiseaseBreast cancer
[ICD9: 174, 175   ICD10: C50]
Drug(s)DesogestrelApprovedHormonal contraceptives[2]
DydrogesteroneApprovedMenstrual disorders[3]
Ethynodiol DiacetateApprovedHormonal contraceptives[4][5]
EtonogestrelApprovedFemale contraceptive[6][7]
LevonorgestrelApprovedHormonal contraceptives[8]
MedroxyprogesteroneApprovedHormonal contraceptives[3]
Medroxyprogesterone acetateApprovedOncological disease (breast and endometrial neoplasms)[9][10][11]
MegestrolApprovedAdvanced carcinoma of the breast and endometrium[12]
MifepristoneApprovedMedical abortion[13][14]
NorethindroneApprovedOral contraceptive[15]
NorgestimateApprovedHormonal contraceptives[6][16]
NorgestrelApprovedHormonal contraceptives[17]
AsoprisnilDiscontinued in Phase IIIEndometriosis[19]
BioChemical ClassZinc-finger    
UniProt IDP06401
PDB Structure1A28; 1E3K; 1SQN; 1SR7; 1ZUC; 2C7A; 2OVH; 2OVM; 2W8Y; 3D90; 3G8O; 3HQ5; 3KBA; 3ZR7; 3ZRA; 3ZRB; 4A2J; 4APU.    
FunctionThe steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues.    
Related US Patent6,451,780
Target ValidationClick to Find Target Validation Information.    
Inhibitor1-Benzyl-3-phenylquinazoline-2,4 (1H,3H)-dione[20]
2- (4-Amino-3'-chloro-biphenyl-3-yl)-propan-2-ol[22]
3- (3,3-dimethyl-2-oxoindolin-5-yl)benzonitrile[24]
3-Phenyl-1-propylquinazoline-2,4 (1H,3H)-dione[20]
4- (2,4-diethyl-1H-pyrrol-3-yloxy)benzonitrile[25]
5- (2-oxoindolin-5-yl)-1H-pyrrole-2-carbonitrile[24]
6- (3-Nitro-phenyl)-3H-benzothiazol-2-one[26]
Lecanindole D[30]
BinderEthynodiol Diacetate[4][5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The biology of breast carcinoma. Cancer. 2003 Feb 1;97(3 Suppl):825-33. To Reference
Ref 2Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40. To Reference
Ref 3Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids. 2008 Feb;73(2):222-31. Epub 2007 Oct 22. To Reference
Ref 4Contribution 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. To Reference
Ref 5The place of progestational hormones in gynecological therapy. Ginekol Pol. 1970 May;41(5):497-502. To Reference
Ref 6Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7. To Reference
Ref 7Endometrial effects of etonogestrel (Implanon) contraceptive implant. Curr Opin Obstet Gynecol. 2001 Jun;13(3):335-41. To Reference
Ref 8Met909 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. Epub 2009 Mar 16. To Reference
Ref 9FDA To Reference
Ref 10Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. To Reference
Ref 118098222 To Reference
Ref 12Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8. To Reference
Ref 13Formononetin, an isoflavone, relaxes rat isolated aorta through endothelium-dependent and endothelium-independent pathways. J Nutr Biochem. 2009 Jun 29. [Epub ahead of print] To Reference
Ref 14Selective progesterone receptor modulators and progesterone antagonists: mechanisms of action and clinical applications. Hum Reprod Update. 2005 May-Jun;11(3):293-307. Epub 2005 Mar 24. To Reference
Ref 15Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes. J Med Chem. 2004 Jun 17;47(13):3381-7. To Reference
Ref 16A review of transdermal hormonal contraception : focus on the ethinylestradiol/norelgestromin contraceptive patch. Treat Endocrinol. 2006;5(6):359-65. To Reference
Ref 17Toll-like receptor-4-mediated macrophage activation is differentially regulated by progesterone via the glucocorticoid and progesterone receptors. Immunology. 2008 Sep;125(1):59-69. Epub 2008 Mar 28. To Reference
Ref 18Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. To Reference
Ref 19New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. To Reference
Ref 20Bioorg Med Chem. 2008 Jul 15;16(14):7046-54. Epub 2008 May 10.Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton. To Reference
Ref 21J Med Chem. 1998 Aug 27;41(18):3461-6.Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore. To Reference
Ref 22Bioorg Med Chem Lett. 2002 Mar 11;12(5):787-90.Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines. To Reference
Ref 23Bioorg Med Chem Lett. 2009 Dec 1;19(23):6666-9. Epub 2009 Oct 7.5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators. To Reference
Ref 24J Med Chem. 2008 Mar 27;51(6):1861-73. Epub 2008 Mar 5.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-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348). To Reference
Ref 25Bioorg Med Chem Lett. 2010 Jun 1;20(11):3384-6. Epub 2010 Apr 13.Optimisation of a pyrazole series of progesterone antagonists; Part 1. To Reference
Ref 26J Med Chem. 2005 Aug 11;48(16):5092-5.Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget. To Reference
Ref 27J Med Chem. 2003 Mar 13;46(6):1016-30.Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. To Reference
Ref 28Bioorg Med Chem Lett. 2010 Apr 1;20(7):2340-3. Epub 2010 Feb 4.The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. To Reference
Ref 29Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. Epub 2007 Nov 21.Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. To Reference
Ref 30J Nat Prod. 2009 Nov;72(11):1944-8.The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. To Reference
Ref 31Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 32Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 33Bioorg Med Chem. 2008 Mar 15;16(6):2753-63. Epub 2008 Jan 11.11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists. To Reference
Ref 34J Med Chem. 2000 Dec 28;43(26):5010-6.Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. To Reference


Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.

Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore

All rights reserved.

Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links


Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543