Details of the Target

General Information of Target

Target ID LDTP02147
Target Name Progesterone receptor (PGR)
Gene Name PGR
Gene ID 5241
Synonyms
NR3C3; Progesterone receptor; PR; Nuclear receptor subfamily 3 group C member 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF
PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA
PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA
AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK
PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV
MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD
CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG
PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC
KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP
YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN
YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV
GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ
LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP
DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ
FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA
LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Nuclear hormone receptor family, NR3 subfamily
Subcellular location
Nucleus; Mitochondrion outer membrane
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.
TTD ID
T22939
Uniprot ID
P06401
DrugMap ID
TTUV8G9
Ensemble ID
ENST00000263463.9
HGNC ID
HGNC:8910
ChEMBL ID
CHEMBL208

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
769P SNV: p.F275S .
8505C SNV: p.P483R .
AN3CA SNV: p.S378I; p.T440M .
CAL78 SNV: p.H888Y .
COLO678 SNV: p.D379Y .
EFO21 SNV: p.A133S .
HCT15 SNV: p.R766I .
HEC1 SNV: p.R94G .
HEC1B SNV: p.R94G; p.G455E .
HT SNV: p.A507V .
HT115 SNV: p.F143L .
HUH7 SNV: p.M924L .
JM1 SNV: p.D225N .
KASUMI2 SNV: p.A373T .
LUDLU1 SNV: p.N828Y .
MEC1 SNV: p.A514T; p.I681V .
MELJUSO Substitution: p.I308P .
NCIH1793 SNV: p.V863F .
NCIH2286 SNV: p.V268F .
NCIH2291 SNV: p.L523I .
NCIH446 SNV: p.R637Ter .
P31FUJ SNV: p.A442T .
RAMOS SNV: p.R740Q .
RKO SNV: p.R187L .
SW837 SNV: p.P364Q .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Probe 1
 Probe Info  		Y374(10.15)  LDD3495  [1]
DBIA
 Probe Info  		C488(1.31)  LDD3379  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0166  [3]
NAIA_5
 Probe Info  		N.A.  LDD2223  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0632  CL-Sc Hep-G2 C891(1.02); C820(0.58)  LDD2227  [4]
 LDCM0634  CY-0357 Hep-G2 C488(0.25)  LDD2228  [4]
 LDCM0022  KB02 AU565 C603(1.19); C488(1.40)  LDD2265  [2]
 LDCM0023  KB03 AU565 C603(1.29); C488(1.44)  LDD2682  [2]
 LDCM0024  KB05 OV56 C488(1.31)  LDD3379  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Progesterone receptor (PGR) Nuclear hormone receptor family P06401
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Estrogen receptor (ESR1) Nuclear hormone receptor family P03372
Signal transducer and activator of transcription 3 (STAT3) Transcription factor STAT family P40763
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CUE domain-containing protein 2 (CUEDC2) CUEDC2 family Q9H467

The Drug(s) Related To This Target

Approved
Click To Hide/Show 37 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Danazol Small molecular drug DB01406
Desogestrel Small molecular drug D06CGB
Dienogest Small molecular drug DB09123
Drospirenone Small molecular drug DB01395
Dydrogesterone Small molecular drug D0F1UL
Ethynodiol Diacetate Small molecular drug DB00823
Etonogestrel Small molecular drug D02KIU
Fluticasone Small molecular drug DB13867
Fluticasone Furoate Small molecular drug DB08906
Fluticasone Propionate Small molecular drug DB00588
Gestrinone Small molecular drug DB11619
Gtpl8662 Small molecular drug D0I2SD
Hydroxyprogesterone Caproate Small molecular drug DB06789
Levonorgestrel Small molecular drug D0BA9U
Lindane Small molecular drug DB00431
Medroxyprogesterone Small molecular drug D0R2KY
Medroxyprogesterone Acetate Small molecular drug DB00603
Megestrol Small molecular drug D04GJN
Megestrol Acetate Small molecular drug DB00351
Mifepristone Small molecular drug DB00834
Mitotane Small molecular drug DB00648
Nestorone Small molecular drug D06RFG
Norelgestromin Small molecular drug DB06713
Norethisterone Small molecular drug DB00717
Norgestimate Small molecular drug D09QZI
Oxybenzone Small molecular drug DB01428
Progesterone Small molecular drug D07BSQ
Spironolactone Small molecular drug DB00421
Ulipristal Small molecular drug D0V4WD
Zk-136798 Small molecular drug D0GL7U
Darolutamide . DB12941
Enzacamene . DB11219
Homosalate . DB11064
Medrogestone . DB09124
Mometasone Furoate . DB14512
Norgestrel . DB09389
Segesterone Acetate . DB14583
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ru-46556 Small molecular drug D02HUB
Gsk-1564023a . D0VF3C
Phase 2
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Onapristone Small molecular drug D07MON
Pf-2413873 Small molecular drug D0L3HU
Telapristone Small molecular drug D0U8AS
Tosagestin Small molecular drug D0H5BC
Vilaprisan Small molecular drug D07YGK
Mk-8342 . D01KMY
S-prant . D0S1YX
Virexxa . D0J0EM
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Zk-112993 Small molecular drug D0K2HA
Investigative
Click To Hide/Show 32 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-benzyl-3-phenylquinazoline-2,4(1h,3h)-dione Small molecular drug D07XCB
2,2,4-trimethyl-6-phenyl-1,2-dihydro-quinoline Small molecular drug D01ETZ
2-(4-amino-3'-chloro-biphenyl-3-yl)-propan-2-ol Small molecular drug D05CND
2-(4-amino-3'-chloro-biphenyl-3-yl)-propan-2-ol Small molecular drug D0N1RQ
3,3-dimethyl-5-m-tolyl-2,3-dihydro-1h-inden-1-one Small molecular drug D09VWK
3-(3,3-dimethyl-2-oxoindolin-5-yl)Benzonitrile Small molecular drug D0V4PL
3-phenyl-1-propylquinazoline-2,4(1h,3h)-dione Small molecular drug D0E9CG
4-(2,4-diethyl-1h-pyrrol-3-yloxy)Benzonitrile Small molecular drug D0D6HI
5,N-dihydroxythalidomide Small molecular drug D09GQF
5-(2-oxoindolin-5-yl)-1h-pyrrole-2-carbonitrile Small molecular drug D06DSF
6-(3-nitro-phenyl)-3h-benzothiazol-2-one Small molecular drug D0KX6D
Al-43 Small molecular drug D0GR5L
Allylestrenol Small molecular drug DB01431
Bay-39-9624 Small molecular drug D01NVD
Estradiol Valerate/Dienogest Small molecular drug D0VJ7A
Ethynodiol Diacetate Small molecular drug D0H2MF
Gsk-325971a Small molecular drug D09XAM
Lecanindole D Small molecular drug D0F1SS
Metribolone Small molecular drug DB02998
Mometasone Small molecular drug DB00764
Norethindrone Small molecular drug D00ZGW
Org2058 Small molecular drug D01UFF
Phthalic Acid Small molecular drug DB02746
Tanaproget Small molecular drug D0V9NE
Way-255348 Small molecular drug D0G5OV
Zk-114043 Small molecular drug D0ZM6R
[3h]Methyltrienolone Small molecular drug D08KQM
Bay 86-5044 . D01OYG
Demegestone . DB13857
Gestodene . DB06730
Gsk-008a . D02WQR
Telapristone Acetate . DB05253
Discontinued
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Asoprisnil Small molecular drug D0W5RL
Org-31710 Small molecular drug D03AZU
Lgd-5552 . D0O1PU
Pf-02367982 . D0N4PC

References

1 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
4 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264