Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT0FZ3QE)

• DOT Name: Progesterone receptor (PGR)
• Synonyms: PR; Nuclear receptor subfamily 3 group C member 3
• Gene Name: PGR
• UniProt ID: PRGR_HUMAN
• PDB ID: 1A28; 1E3K; 1SQN; 1SR7; 1ZUC; 2C7A; 2OVH; 2OVM; 2W8Y; 3D90; 3G8O; 3HQ5; 3KBA; 3ZR7; 3ZRA; 3ZRB; 4A2J; 4APU; 4OAR; 5CC0
• Pfam ID: PF00104 ; PF02161 ; PF00105
• Sequence:
  MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF
  PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA
  PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA
  AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK
  PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV
  MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD
  CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG
  PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC
  KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP
  YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN
  YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV
  GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ
  LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP
  DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ
  FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA
  LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
• Function: The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Depending on the isoform, progesterone receptor functions as a transcriptional activator or repressor; [Isoform A]: Ligand-dependent transdominant repressor of steroid hormone receptor transcriptional activity including repression of its isoform B, MR and ER. Transrepressional activity may involve recruitment of corepressor NCOR2; [Isoform B]: Transcriptional activator of several progesteron-dependent promoters in a variety of cell types. Involved in activation of SRC-dependent MAPK signaling on hormone stimulation; [Isoform 4]: Increases mitochondrial membrane potential and cellular respiration upon stimulation by progesterone.
• Tissue Specificity: In reproductive tissues the expression of isoform A and isoform B varies as a consequence of developmental and hormonal status. Isoform A and isoform B are expressed in comparable levels in uterine glandular epithelium during the proliferative phase of the menstrual cycle. Expression of isoform B but not of isoform A persists in the glands during mid-secretory phase. In the stroma, isoform A is the predominant form throughout the cycle. Heterogeneous isoform expression between the glands of the endometrium basalis and functionalis is implying region-specific responses to hormonal stimuli.
• KEGG Pathway:
  Oocyte meiosis (hsa04114)
  Progesterone-mediated oocyte maturation (hsa04914)
  Estrogen sig.ling pathway (hsa04915)
  Chemical carcinogenesis - receptor activation (hsa05207)
  Breast cancer (hsa05224)
• Reactome Pathway:
  HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand (R-HSA-3371497)
  Nuclear Receptor transcription pathway (R-HSA-383280)
  SUMOylation of intracellular receptors (R-HSA-4090294)
  Estrogen-dependent gene expression (R-HSA-9018519)
  Nuclear signaling by ERBB4 (R-HSA-1251985)

Molecular Interaction Atlas (MIA) of This DOT

This DOT Affected the Regulation of Drug Effects of 1 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Promegestone	DMK4S8I	Approved	Progesterone receptor (PGR) increases the uptake of Promegestone.	[61]

2 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the methylation of Progesterone receptor (PGR).	[1]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of Progesterone receptor (PGR).	[35]

69 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Tretinoin	DM49DUI	Approved	Tretinoin increases the expression of Progesterone receptor (PGR).	[2]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Progesterone receptor (PGR).	[3]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Progesterone receptor (PGR).	[4]
Arsenic	DMTL2Y1	Approved	Arsenic decreases the expression of Progesterone receptor (PGR).	[5]
Testosterone	DM7HUNW	Approved	Testosterone increases the expression of Progesterone receptor (PGR).	[6]
Decitabine	DMQL8XJ	Approved	Decitabine increases the expression of Progesterone receptor (PGR).	[7]
Fluorouracil	DMUM7HZ	Approved	Fluorouracil affects the expression of Progesterone receptor (PGR).	[8]
Fulvestrant	DM0YZC6	Approved	Fulvestrant decreases the expression of Progesterone receptor (PGR).	[9]
Niclosamide	DMJAGXQ	Approved	Niclosamide decreases the expression of Progesterone receptor (PGR).	[10]
Diethylstilbestrol	DMN3UXQ	Approved	Diethylstilbestrol increases the expression of Progesterone receptor (PGR).	[11]
Nicotine	DMWX5CO	Approved	Nicotine decreases the expression of Progesterone receptor (PGR).	[12]
Ethinyl estradiol	DMODJ40	Approved	Ethinyl estradiol increases the expression of Progesterone receptor (PGR).	[13]
Mifepristone	DMGZQEF	Approved	Mifepristone decreases the activity of Progesterone receptor (PGR).	[14]
Lindane	DMB8CNL	Approved	Lindane increases the expression of Progesterone receptor (PGR).	[15]
Estrone	DM5T6US	Approved	Estrone decreases the expression of Progesterone receptor (PGR).	[4]
Docetaxel	DMDI269	Approved	Docetaxel decreases the expression of Progesterone receptor (PGR).	[16]
Aminoglutethimide	DMWFHMZ	Approved	Aminoglutethimide decreases the expression of Progesterone receptor (PGR).	[17]
Mestranol	DMG3F94	Approved	Mestranol increases the expression of Progesterone receptor (PGR).	[18]
Estriol	DMOEM2I	Approved	Estriol increases the expression of Progesterone receptor (PGR).	[19]
Sodium chloride	DMM3950	Approved	Sodium chloride increases the activity of Progesterone receptor (PGR).	[21]
Exemestane	DM9HPW3	Approved	Exemestane increases the expression of Progesterone receptor (PGR).	[22]
Tibolone	DM78XFG	Approved	Tibolone increases the activity of Progesterone receptor (PGR).	[23]
Letrozole	DMH07Y3	Approved	Letrozole decreases the expression of Progesterone receptor (PGR).	[24]
Potassium chloride	DMMTAJC	Approved	Potassium chloride increases the activity of Progesterone receptor (PGR).	[21]
ARZOXIFENE	DMOKCVI	Approved	ARZOXIFENE decreases the expression of Progesterone receptor (PGR).	[25]
Goserelin	DMAT8CG	Approved	Goserelin decreases the expression of Progesterone receptor (PGR).	[26]
Anastrozole	DMNP60F	Approved	Anastrozole decreases the expression of Progesterone receptor (PGR).	[24]
Nandrolone	DMFWKG1	Approved	Nandrolone increases the expression of Progesterone receptor (PGR).	[27]
Resveratrol	DM3RWXL	Phase 3	Resveratrol increases the expression of Progesterone receptor (PGR).	[29]
Epigallocatechin gallate	DMCGWBJ	Phase 3	Epigallocatechin gallate decreases the expression of Progesterone receptor (PGR).	[30]
EXISULIND	DMBY56U	Phase 3	EXISULIND decreases the expression of Progesterone receptor (PGR).	[31]
Guaiacol	DMN4E7T	Phase 3	Guaiacol decreases the expression of Progesterone receptor (PGR).	[30]
ICARIIN	DMOJQGT	Phase 3	ICARIIN increases the expression of Progesterone receptor (PGR).	[32]
Genistein	DM0JETC	Phase 2/3	Genistein decreases the expression of Progesterone receptor (PGR).	[30]
Afimoxifene	DMFORDT	Phase 2	Afimoxifene decreases the expression of Progesterone receptor (PGR).	[33]
Puerarin	DMJIMXH	Phase 2	Puerarin decreases the expression of Progesterone receptor (PGR).	[30]
Icaritin	DMGHQ37	Phase 2	Icaritin increases the expression of Progesterone receptor (PGR).	[34]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Progesterone receptor (PGR).	[36]
HEXESTROL	DM9AGWQ	Withdrawn from market	HEXESTROL increases the expression of Progesterone receptor (PGR).	[18]
Geldanamycin	DMS7TC5	Discontinued in Phase 2	Geldanamycin decreases the expression of Progesterone receptor (PGR).	[37]
MX-4509	DMC4RK7	Discontinued in Phase 1	MX-4509 increases the expression of Progesterone receptor (PGR).	[27]
MG-132	DMKA2YS	Preclinical	MG-132 increases the expression of Progesterone receptor (PGR).	[38]
Daidzin	DMFCMPS	Terminated	Daidzin increases the expression of Progesterone receptor (PGR).	[39]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A increases the expression of Progesterone receptor (PGR).	[11]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A increases the expression of Progesterone receptor (PGR).	[40]
Coumestrol	DM40TBU	Investigative	Coumestrol increases the expression of Progesterone receptor (PGR).	[9]
methyl p-hydroxybenzoate	DMO58UW	Investigative	methyl p-hydroxybenzoate increases the expression of Progesterone receptor (PGR).	[41]
Glyphosate	DM0AFY7	Investigative	Glyphosate increases the expression of Progesterone receptor (PGR).	[42]
Nickel chloride	DMI12Y8	Investigative	Nickel chloride increases the expression of Progesterone receptor (PGR).	[43]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE	DMNQL17	Investigative	2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE increases the expression of Progesterone receptor (PGR).	[45]
Okadaic acid	DM47CO1	Investigative	Okadaic acid decreases the expression of Progesterone receptor (PGR).	[46]
Chlorpyrifos	DMKPUI6	Investigative	Chlorpyrifos decreases the expression of Progesterone receptor (PGR).	[47]
U0126	DM31OGF	Investigative	U0126 decreases the expression of Progesterone receptor (PGR).	[48]
Kaempferol	DMHEMUB	Investigative	Kaempferol increases the expression of Progesterone receptor (PGR).	[49]
OXYBENZONE	DMMZYX6	Investigative	OXYBENZONE increases the expression of Progesterone receptor (PGR).	[50]
Daidzein	DMRFTJX	Investigative	Daidzein increases the expression of Progesterone receptor (PGR).	[49]
Linalool	DMGZQ5P	Investigative	Linalool increases the expression of Progesterone receptor (PGR).	[51]
biochanin A	DM0HPWY	Investigative	biochanin A increases the expression of Progesterone receptor (PGR).	[52]
Chlorogenic acid	DM2Y3P4	Investigative	Chlorogenic acid decreases the expression of Progesterone receptor (PGR).	[30]
27-hydroxycholesterol	DM2L6OZ	Investigative	27-hydroxycholesterol increases the expression of Progesterone receptor (PGR).	[53]
N-nonylphenol	DMH3OUX	Investigative	N-nonylphenol increases the expression of Progesterone receptor (PGR).	[54]
Tetramethylbutylphenol	DMW9CH2	Investigative	Tetramethylbutylphenol increases the expression of Progesterone receptor (PGR).	[27]
Alpha-naphthoflavone	DMELOIQ	Investigative	Alpha-naphthoflavone increases the expression of Progesterone receptor (PGR).	[56]
Ginsenoside Re	DM46FVD	Investigative	Ginsenoside Re increases the expression of Progesterone receptor (PGR).	[57]
HPTE	DMRPZD4	Investigative	HPTE increases the expression of Progesterone receptor (PGR).	[49]
Ginsenoside Rb1	DMF70AB	Investigative	Ginsenoside Rb1 increases the expression of Progesterone receptor (PGR).	[57]
Phenolsulfonphthalein	DMCTUAD	Investigative	Phenolsulfonphthalein increases the expression of Progesterone receptor (PGR).	[58]
TFMPP	DMAC8TP	Investigative	TFMPP increases the expression of Progesterone receptor (PGR).	[59]
1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole	DMQEJVU	Investigative	1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole increases the expression of Progesterone receptor (PGR).	[60]

7 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Mitotane	DMU1GX0	Approved	Mitotane affects the binding of Progesterone receptor (PGR).	[20]
Drospirenone	DM1A9W3	Approved	Drospirenone affects the binding of Progesterone receptor (PGR).	[28]
[3H]methyltrienolone	DMTSGOW	Investigative	[3H]methyltrienolone affects the binding of Progesterone receptor (PGR).	[44]
Apigenin	DMI3491	Investigative	Apigenin affects the binding of Progesterone receptor (PGR).	[20]
Chlorphrifos oxon	DMGBT68	Investigative	Chlorphrifos oxon affects the binding of Progesterone receptor (PGR).	[55]
toxaphene	DM4R657	Investigative	toxaphene affects the binding of Progesterone receptor (PGR).	[20]
Phthalic Acid	DMF9T64	Investigative	Phthalic Acid affects the binding of Progesterone receptor (PGR).	[20]

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