Therapeutic Targets Database
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TTD Target ID: TTDS00245

Target Information
NameProgesterone receptor    
Type of targetSuccessful target    
SynonymsPR    
DiseaseBreast cancer    [1]
Drug(s)DesogestrelApprovedHormonal contraceptives[2]
DydrogesteroneApprovedMenstrual disorders[3]
Ethynodiol DiacetateApprovedHormonal contraceptives[4][5]
EtonogestrelApprovedFemale contraceptive[6][7]
LevonorgestrelApprovedHormonal contraceptives[8]
MedroxyprogesteroneApprovedHormonal contraceptives[3]
MegestrolApprovedAdvanced carcinoma of the breast and endometrium[9]
MifepristoneApprovedMedical abortion[10][11]
NorethindroneApprovedOral contraceptive[12]
NorgestimateApprovedHormonal contraceptives[6][13]
NorgestrelApprovedHormonal contraceptives[14]
UlipristalApprovedContraception[15]
AsoprisnilDiscontinued in Phase IIIEndometriosis[16]
BioChemical ClassZinc-finger    
UniProt IDP06401
PDB Structure1E3K; 1SQN; 1SR7; 1ZUC; 2C7A; 2OVH; 2OVM; 2W8Y.    
FunctionThe steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues.    
SequenceMTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
Related US Patent6,451,780
6,608,074
Target ValidationClick to Find Target Validation Information.    
Inhibitor1-Benzyl-3-phenylquinazoline-2,4 (1H,3H)-dione[17]
2,2,4-Trimethyl-6-phenyl-1,2-dihydro-quinoline[18]
2- (4-Amino-3'-chloro-biphenyl-3-yl)-propan-2-ol[19]
3,3-dimethyl-5-m-tolyl-2,3-dihydro-1H-inden-1-one[20]
3- (3,3-dimethyl-2-oxoindolin-5-yl)benzonitrile[21]
3-Phenyl-1-propylquinazoline-2,4 (1H,3H)-dione[17]
4- (2,4-diethyl-1H-pyrrol-3-yloxy)benzonitrile[22]
5,N-Dihydroxythalidomide[17]
5- (2-oxoindolin-5-yl)-1H-pyrrole-2-carbonitrile[21]
6- (3-Nitro-phenyl)-3H-benzothiazol-2-one[23]
AL-43[24]
GSK-1564023A[25]
GSK-325971A[25]
LGD-5552[26]
Lecanindole D[27]
Methyltrienolone[28]
ONAPRISTONE[18]
PF-02367982[22]
Tanaproget[29]
ULIPRISTAL ACETATE[30]
WAY-255348[21]
ZK-230211[31]
AgonistDydrogesterone[3]
Medroxyprogesterone[3]
Norethindrone[12]
Norgestimate[6][13]
Norgestrel[14]
AntagonistMifepristone[10][11]
Telaprevir[16]
ModulatorAsoprisnil[16]
Desogestrel[2]
Ulipristal[15]
BinderEthynodiol Diacetate[4][5]
Etonogestrel[6][7]
Levonorgestrel[8]
Megestrol[9]
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 9Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8. To Reference
Ref 10Formononetin, 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 11Selective 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 12Progesterone 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 13A review of transdermal hormonal contraception : focus on the ethinylestradiol/norelgestromin contraceptive patch. Treat Endocrinol. 2006;5(6):359-65. To Reference
Ref 14Toll-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 15Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. To Reference
Ref 16New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. To Reference
Ref 17Bioorg 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 18J 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 19Bioorg 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 20Bioorg 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 21J 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 22Bioorg 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 23J 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 24J 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 25Bioorg 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 26Proc 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 27J Nat Prod. 2009 Nov;72(11):1944-8.The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. To Reference
Ref 28Overington 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 29Berman 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 30Bioorg 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 31J Med Chem. 2000 Dec 28;43(26):5010-6.Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. To Reference



 

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