Details of the Target

General Information of Target

Target ID LDTP02488
Target Name Androgen receptor (AR)
Gene Name AR
Gene ID 367
Synonyms
DHTR; NR3C4; Androgen receptor; Dihydrotestosterone receptor; Nuclear receptor subfamily 3 group C member 4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR3 subfamily
Subcellular location
Nucleus
Function
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins like ZBTB7A that recruits NCOR1 and NCOR2 to the androgen response elements/ARE on target genes, negatively regulating androgen receptor signaling and androgen-induced cell proliferation. Transcription activation is also down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.; [Isoform 3]: Lacks the C-terminal ligand-binding domain and may therefore constitutively activate the transcription of a specific set of genes independently of steroid hormones.; [Isoform 4]: Lacks the C-terminal ligand-binding domain and may therefore constitutively activate the transcription of a specific set of genes independently of steroid hormones.
TTD ID
T11211
Uniprot ID
P10275
DrugMap ID
TTS64P2
Ensemble ID
ENST00000374690.9
HGNC ID
HGNC:644
ChEMBL ID
CHEMBL1871

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.H875Y DBIA    Probe Info 
AGS SNV: p.E773V .
COLO792 SNV: p.P555L .
DU4475 SNV: p.R386C DBIA    Probe Info 
FTC133 SNV: p.A270T .
IGROV1 SNV: p.A400V .
JURKAT Insertion: p.Q803PfsTer27 .
JURLMK1 SNV: p.G421V .
KATOIII SNV: p.E666K .
LNCaP clone FGC SNV: p.T878A DBIA    Probe Info 
MCC13 SNV: p.P379S; p.R539H .
MDAMB453 SNV: p.Q868H DBIA    Probe Info 
MEWO SNV: p.E523D .
MIAPACA2 SNV: p.G536R .
NCIH2172 SNV: p.P486R .
OCUG1 SNV: p.K633T .
RKO SNV: p.Q74K; p.T306I .
RL952 SNV: p.G482D .
SKNSH SNV: p.H382N .

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
Curcusone 37
 Probe Info  		3.31  LDD0188  [1]
NAIA_5
 Probe Info  		C519(20.00)  LDD2227  [2]
DBIA
 Probe Info  		C619(1.63)  LDD0080  [3]
IPM
 Probe Info  		N.A.  LDD2156  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0632  CL-Sc Hep-G2 C519(20.00)  LDD2227  [2]
 LDCM0033  Curcusone1d MCF-7 3.31  LDD0188  [1]
 LDCM0022  KB02 HCT 116 C619(1.63)  LDD0080  [3]
 LDCM0023  KB03 HCT 116 C619(3.59)  LDD0081  [3]
 LDCM0024  KB05 HCT 116 C619(2.39)  LDD0082  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 34 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone-lysine N-methyltransferase NSD2 (NSD2) Histone-lysine methyltransferase family O96028
Histone-lysine N-methyltransferase 2A (KMT2A) Histone-lysine methyltransferase family Q03164
Histone-lysine N-methyltransferase 2D (KMT2D) Histone-lysine methyltransferase family O14686
Aromatic-L-amino-acid decarboxylase (DDC) Group II decarboxylase family P20711
Histone deacetylase 4 (HDAC4) Histone deacetylase family P56524
Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2 (INPPL1) Inositol 1,4,5-trisphosphate 5-phosphatase family O15357
Lysine-specific demethylase 5D (KDM5D) JARID1 histone demethylase family Q9BY66
Probable JmjC domain-containing histone demethylation protein 2C (JMJD1C) JHDM2 histone demethylase family Q15652
E3 ubiquitin-protein ligase Mdm2 (MDM2) MDM2/MDM4 family Q00987
Histone acetyltransferase KAT7 (KAT7) MYST (SAS/MOZ) family O95251
Caspase-8 (CASP8) Peptidase C14A family Q14790
Parkinson disease protein 7 (PARK7) Peptidase C56 family Q99497
Peroxiredoxin-1 (PRDX1) Peroxiredoxin family Q06830
DNA-dependent protein kinase catalytic subunit (PRKDC) PI3/PI4-kinase family P78527
Serine/threonine-protein kinase MAK (MAK) CMGC Ser/Thr protein kinase family P20794
Tyrosine-protein kinase ABL1 (ABL1) Tyr protein kinase family P00519
Megakaryocyte-associated tyrosine-protein kinase (MATK) Tyr protein kinase family P42679
Tyrosine-protein kinase Fes/Fps (FES) Tyr protein kinase family P07332
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
Tyrosine-protein kinase Blk (BLK) Tyr protein kinase family P51451
Tyrosine-protein kinase Fgr (FGR) Tyr protein kinase family P09769
Tyrosine-protein kinase Lck (LCK) Tyr protein kinase family P06239
Tyrosine-protein kinase Lyn (LYN) Tyr protein kinase family P07948
Tyrosine-protein kinase Yes (YES1) Tyr protein kinase family P07947
Tyrosine-protein phosphatase non-receptor type 11 (PTPN11) Protein-tyrosine phosphatase family Q06124
Tensin-1 (TNS1) PTEN phosphatase protein family Q9HBL0
E3 ubiquitin-protein ligase RNF14 (RNF14) RBR family Q9UBS8
E3 ubiquitin-protein ligase RNF6 (RNF6) RNF12 family Q9Y252
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 (PLCG1) . P19174
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-2 (PLCG2) . P16885
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 2 (CTDSP2) . O14595
CREB-binding protein (CREBBP) . Q92793
Peptidyl-prolyl cis-trans isomerase FKBP4 (FKBP4) . Q02790
Set1/Ash2 histone methyltransferase complex subunit ASH2 (ASH2L) . Q9UBL3
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
G1/S-specific cyclin-D1 (CCND1) Cyclin family P24385
Transcription factor
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Mothers against decapentaplegic homolog 1 (SMAD1) Dwarfin/SMAD family Q15797
Transcriptional regulator ERG (ERG) ETS family P11308
Gamma-interferon-inducible protein 16 (IFI16) HIN-200 family Q16666
Nuclear receptor coactivator 2 (NCOA2) SRC/p160 nuclear receptor coactivator family Q15596
Forkhead box protein H1 (FOXH1) . O75593
Hepatocyte nuclear factor 3-alpha (FOXA1) . P55317
Hypoxia-inducible factor 1-alpha (HIF1A) . Q16665
Other
Click To Hide/Show 19 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Catenin beta-1 (CTNNB1) Beta-catenin family P35222
Protein BTG2 (BTG2) BTG family P78543
Death domain-associated protein 6 (DAXX) DAXX family Q9UER7
Growth factor receptor-bound protein 7 (GRB7) GRB7/10/14 family Q14451
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) PI3K p85 subunit family P27986
Phosphatidylinositol 3-kinase regulatory subunit beta (PIK3R2) PI3K p85 subunit family O00459
Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) PI3K p85 subunit family Q92569
Small ubiquitin-related modifier 1 (SUMO1) Ubiquitin family P63165
Gelsolin (GSN) Villin/gelsolin family P06396
B-cell linker protein (BLNK) . Q8WV28
Nuclear receptor coactivator 6 (NCOA6) . Q14686
Ras GTPase-activating protein 1 (RASA1) . P20936
SH2 domain-containing adapter protein E (SHE) . Q5VZ18
SH2 domain-containing protein 1B (SH2D1B) . O14796
SH2 domain-containing protein 2A (SH2D2A) . Q9NP31
SHC-transforming protein 1 (SHC1) . P29353
SHC-transforming protein 4 (SHC4) . Q6S5L8
Signal-transducing adaptor protein 1 (STAP1) . Q9ULZ2
Suppressor of cytokine signaling 6 (SOCS6) . O14544

The Drug(s) Related To This Target

Approved
Click To Hide/Show 58 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetophenazine Small molecular drug DB01063
Apalutamide Small molecular drug DB11901
Arn-509 Small molecular drug D0S7LG
Bicalutamide Small molecular drug D0V9BD
Clascoterone Small molecular drug D08TEJ
Cyproterone Small molecular drug D06AEO
Cyproterone Acetate Small molecular drug DB04839
Danazol Small molecular drug DB01406
Dienogest Small molecular drug DB09123
Diethylstilbestrol Small molecular drug DB00255
Dromostanolone Small molecular drug D09NNA
Drospirenone Small molecular drug DB01395
Enzalutamide Small molecular drug D0QK5X
Estrone Small molecular drug DB00655
Ethylestrenol Small molecular drug D0SC8F
Eugenol Small molecular drug DB09086
Fludrocortisone Small molecular drug D0R7JT
Flufenamic Acid Small molecular drug D0B2WJ
Flufenamic Acid Small molecular drug DB02266
Fluoxymesterone Small molecular drug D0L2LS
Fluphenazine Small molecular drug DB00623
Flutamide Small molecular drug D0Y0SW
Gestrinone Small molecular drug DB11619
Hydroxyflutamide Small molecular drug D0BC2E
Ketoconazole Small molecular drug DB01026
Levonorgestrel Small molecular drug DB00367
Methyltestosterone Small molecular drug DB06710
Mitotane Small molecular drug DB00648
Nandrolone Small molecular drug D00YWP
Nandrolone Decanoate Small molecular drug DB08804
Nandrolone Phenpropionate Small molecular drug DB00984
Nilutamide Small molecular drug D0SN9T
Norelgestromin Small molecular drug DB06713
Norethisterone Small molecular drug DB00717
Norgestimate Small molecular drug DB00957
Oxandrolone Small molecular drug D0U3GL
Oxybenzone Small molecular drug DB01428
Oxymetholone Small molecular drug DB06412
Periciazine Small molecular drug DB01608
Prasterone Small molecular drug D0K0EK
Progesterone Small molecular drug DB00396
Spironolactone Small molecular drug DB00421
Tamoxifen Small molecular drug DB00675
Testosterone Small molecular drug D06XMU
Testosterone Propionate Small molecular drug DB01420
Testosterone Undecanoate Small molecular drug DB13946
Triclosan Small molecular drug DB08604
Ulipristal Small molecular drug DB08867
Darolutamide . D0DV6D
Enzacamene . DB11219
Esculin . DB13155
Homosalate . DB11064
Norethynodrel . DB09371
Norgestrel . DB09389
Segesterone Acetate . DB14583
Stanozolol . DB06718
Testosterone Cypionate . DB13943
Testosterone Enanthate . DB13944
Phase 4
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dihydrotestosterone Small molecular drug D04DJN
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Hc-1119 Small molecular drug DE4AO8
Zanoterone Small molecular drug D04NNJ
Phase 2
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Arv-110 Small molecular drug D3ZY1K
Arv-471 Small molecular drug DS41PJ
Asc-j9 Small molecular drug DZTX12
Mk-0773 Small molecular drug D0RV6F
Tok-001 Small molecular drug D0U0BU
Apc-100 . D0N7DQ
Ascj-9 . D04KYB
Azd5312 . D0C9EN
Onc1-13b . D03CVT
Testogen Tds . D0G1IV
Phase 1
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Epi-7386 Small molecular drug DY7Q1O
Rad-140 Small molecular drug D09ZLZ
Testosterone Buciclate Small molecular drug D05VNP
Azd-3514 . D08AAV
Cc-94676 . DNY63Z
Drug 2881078 . D0D3FP
Dt-200 . D0C4FS
Ps-178990 . D04XWX
Tas3681 . D0N5NC
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Glpg-0492 . D0BJ7W
Investigative
Click To Hide/Show 51 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,2-dibromo-4-(1,2-dibromoethyl)Cyclohexane Small molecular drug D06BLF
11-methyl-6,11-dihydro-5h-benzo[A]Carbazol-9-ol Small molecular drug D07TLT
6,11-dihydrothiochromeno[4,3-b]Indol-8-ol Small molecular drug D00QVP
Andarine Small molecular drug DB07423
Bms-564929 Small molecular drug DB07286
Boldenone Small molecular drug D09HQH
Calusterone Small molecular drug D03KYW
Ch-4933468 Small molecular drug D0W5IF
Delta1-dihydrotestosterone Small molecular drug D0Z3WA
Epi-001 Small molecular drug D0T1DZ
Lgd-2226 Small molecular drug DB08089
Metribolone Small molecular drug DB02998
Oxendlone Small molecular drug D0MM9P
Palodesangren C Small molecular drug D0A7YH
Palodesangren D Small molecular drug D0I3LL
Palodesangren E Small molecular drug D0JI4G
Ru-59063 Small molecular drug D07KOY
[3h]Methyltrienolone Small molecular drug D01ETZ
[3h]Mibolerone Small molecular drug D06VZE
(2s)-2-hydroxy-2-methyl-n-[4-nitro-3-(Trifluoromethyl)Phenyl]-3-(Pentafluorophenoxy)Propanamide . DB07422
(2s)-n-(4-cyano-3-iodophenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide . DB07039
(3aalpha4alpha7alpha7aalpha)- 3a477a-tetrahydro-2-(4-nitro-1-naphthalenyl)-47-ethano-1h-isoindole-13(2h)-dione . DB04709
(5s8r9s10s13r14s17s)-13-{2-[(35-difluorobenzyl)Oxy]Ethyl}-17-hydroxy-10-methylhexadecahydro-3h-cyclopenta[A]Phenanthren-3-one . DB07717
(R)-3-bromo-2-hydroxy-2-methyl-n-[4-nitro-3-(Trifluoromethyl)Phenyl]Propanamide . DB07454
(R)-bicalutamide . DB02932
1-tert-butyl-3-(25-dimethylbenzyl)-1h-pyrazolo[34-d]Pyrimidin-4-amine . DB08035
2-chloro-4-{[(1r3z7s7as)-7-hydroxy-1-(Trifluoromethyl)Tetrahydro-1h-pyrrolo[12-c][13]Oxazol-3-ylidene]Amino}-3-methylbenzonitrile . DB08088
3-[(4-amino-1-tert-butyl-1h-pyrazolo[34-d]Pyrimidin-3-yl)Methyl]Phenol . DB08461
4-[(7r7as)-7-hydroxy-13-dioxotetrahydro-1h-pyrrolo[12-c]Imidazol-2(3h)-yl]-1-naphthonitrile . DB08087
4-{[(1r2s)-12-dihydroxy-2-methyl-3-(4-nitrophenoxy)Propyl]Amino}-2-(Trifluoromethyl)Benzonitrile . DB07421
Andromustine . D0W8AI
Arn34 . D0D8QN
Asc-jmx2 . D02RZC
Asc-jmz1 . D0O0II
Dimethylcurcumin . DB06133
Dl-3 . D04MFW
Echinacoside . DB15488
Gtx-027 . D04QFY
Hyg-440 . D0NH0U
Ketodarolutamide . DB15647
Ligandrol . DB13934
Luprostiol . DB11425
Mibolerone . DB11429
Phenothiazine . DB11447
S-23 . DB07419
S-3-(4-fluorophenoxy)-2-hydroxy-2-methyl-n-[4-nitro-3-(Trifluoromethyl)Phenyl]Propanamide . DB07769
Sarms . D0JC4J
Stanolone Acetate . DB13951
Sx-arpc . D0C1UP
Testetrol . D09XGK
Tetrahydrogestrinone . DB06870
Discontinued
Click To Hide/Show 15 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-testosterone Small molecular drug DB01481
Drostanolone Small molecular drug DB00858
He-2000 Small molecular drug D0F7WQ
Lgd2941 Small molecular drug D03KTE
Mx-4509 Small molecular drug D05BCA
Stanolone Small molecular drug DB02901
Boldenone Undecylenate . DB14639
Gsk2849466 . D03SHP
Gw-275919 . D09IZX
Lg-2293 . D0G6PL
Np-619 . D0E3EK
Opterone . D00ABW
Pf-06260414 . D0S7UU
Testosterone Glucoside . D08NNR
Zd-3980 . D07VUD

References

1 Total Synthesis and Target Identification of the Curcusone Diterpenes. J Am Chem Soc. 2021 Mar 24;143(11):4379-4386. doi: 10.1021/jacs.1c00557. Epub 2021 Mar 11.
2 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
3 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
4 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019