Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTS64P2)

DTT Name Androgen receptor (AR)
Synonyms Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR
Gene Name AR
DTT Type
Successful target
 [1]
BioChemical Class
Nuclear hormone receptor
UniProt ID
ANDR_HUMAN
TTD ID
T11211
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
Function
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. Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues.
KEGG Pathway
Oocyte meiosis (hsa04114 )
Pathways in cancer (hsa05200 )
Prostate cancer (hsa05215 )
Reactome Pathway
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 (R-HSA-5625886 )
Nuclear Receptor transcription pathway (R-HSA-383280 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
19 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ARN-509 DMT81LZ Acute myeloid leukaemia 2A60 Approved [2]
Bicalutamide DMZMSPF Prostate cancer 2C82.0 Approved [3]
Clascoterone DMPGR1E Acne vulgaris ED80 Approved [4]
Cyproterone DMQXLD2 Prostate cancer 2C82.0 Approved [5]
Darolutamide DMV7YFT Prostate cancer 2C82.0 Approved [6]
Dromostanolone DMF2JDG Aplastic anemia 3A70 Approved [7]
Enzalutamide DMGL19D Prostate cancer 2C82.0 Approved [8]
Ethylestrenol DM20VMW Testosterone deficiency 5A81.1 Approved [9]
Fludrocortisone DMUDIR8 Addison disease 5A74.0 Approved [10]
Flufenamic Acid DMC8VNH Dysmenorrhea GA34.3 Approved [11]
Fluoxymesterone DMUHCF1 Breast cancer 2C60-2C65 Approved [12]
Flutamide DMK0O7U Prostate cancer 2C82.0 Approved [1]
Hydroxyflutamide DMGIZF5 Prostate cancer 2C82.0 Approved [13]
Nandrolone DMFWKG1 Osteoporosis FB83.0 Approved [14]
Nilutamide DMFN07X Prostate cancer 2C82.0 Approved [15]
Oxandrolone DMU9MYJ Alcoholic hepatitis DB94.1 Approved [16]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [17]
Testosterone DM7HUNW Hot flushes GA30 Approved [18]
Dihydrotestosterone DM3S8XC Prostate hyperplasia GA90 Phase 4 [19]
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⏷ Show the Full List of 19 Approved Drug(s)
23 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
HC-1119 DMB06MU Prostate cancer 2C82.0 Phase 3 [20]
ZANOTERONE DM9HUYP Prostate hyperplasia GA90 Phase 3 [21]
ASC-J9 DMDQS4W End-stage renal disease GB61.5 Phase 2 [22]
ASCJ-9 DMMBVCJ Acne vulgaris ED80 Phase 2 [23]
AZD5312 DMJ8V3K Prostate cancer 2C82.0 Phase 2 [24]
MK-0773 DM2CJB4 Osteoporosis FB83.0 Phase 2 [25]
Testogen TDS DMMK6IT Hypogonadism 5A61.0 Phase 2 [26]
TOK-001 DMVJWPR Prostate cancer 2C82.0 Phase 2 [27]
APC-100 DM71I53 Prostate cancer 2C82.0 Phase 1/2 [28]
ARV-110 DMYCID5 Prostate cancer 2C82.0 Phase 1/2 [29]
ARV-471 DM276Y8 Breast cancer 2C60-2C65 Phase 1/2 [30]
ARV-766 DM8IUV1 Prostate cancer 2C82.0 Phase 1/2 [31]
ONC1-13B DM2DHJS Prostate cancer 2C82.0 Phase 1/2 [32]
AC0176 DM9WJFX Prostate cancer 2C82.0 Phase 1 [33]
AZD-3514 DMC1BXV Prostate cancer 2C82.0 Phase 1 [34]
CC-94676 DM4581B Invasive prostate cancer 2C82 Phase 1 [35]
Drug 2881078 DMWXQC9 Heart failure BD10-BD13 Phase 1 [36]
DT-200 DMYFOJQ Duchenne dystrophy 8C70 Phase 1 [37]
EPI-7386 DMUFN29 Prostate cancer 2C82.0 Phase 1 [38]
PS-178990 DM2594H Muscle atrophy FB32.Y Phase 1 [39]
RAD-140 DMNVDI2 Breast cancer 2C60-2C65 Phase 1 [40]
TAS3681 DMFG6ML Prostate cancer 2C82.0 Phase 1 [41]
TESTOSTERONE BUCICLATE DM3DUHL Contraception QA21 Phase 1 [26]
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⏷ Show the Full List of 23 Clinical Trial Drug(s)
11 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
GW-275919 DMOIL29 Pain MG30-MG3Z Discontinued in Phase 2 [42]
HE-2000 DMWH4CY Cystic fibrosis CA25 Discontinued in Phase 2 [43]
NP-619 DM50PZH Alopecia ED70 Discontinued in Phase 2 [44]
Testosterone glucoside DM5O6HM Hypogonadism 5A61.0 Discontinued in Phase 2 [26]
GSK2849466 DMM7Q3L Heart failure BD10-BD13 Discontinued in Phase 1 [45]
LGD2941 DM9LEGU Osteoporosis FB83.0 Discontinued in Phase 1 [46]
MX-4509 DMC4RK7 Neurological disorder 6B60 Discontinued in Phase 1 [47]
Opterone DMPDJC8 Hormone deficiency 5A61.1 Discontinued in Phase 1 [26]
PF-06260414 DMSE3WP Cachexia MG20 Discontinued in Phase 1 [48]
LG-2293 DMNXKR2 Prostate cancer 2C82.0 Terminated [50]
ZD-3980 DM91IPH Prostate hyperplasia GA90 Terminated [51]
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⏷ Show the Full List of 11 Discontinued Drug(s)
1 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
GLPG-0492 DMSW07R Cachexia MG20 Preclinical [49]
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25 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane DMDJYHK Discovery agent N.A. Investigative [52]
11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol DM9IHFY Discovery agent N.A. Investigative [53]
6,11-dihydrothiochromeno[4,3-b]indol-8-ol DM0RB53 Discovery agent N.A. Investigative [53]
Andromustine DMHL0ID Prostate cancer 2C82.0 Investigative [54]
ARN34 DMMCFEX Discovery agent N.A. Investigative [55]
ASC-JMX2 DMYJ87C Prostate hyperplasia GA90 Investigative [54]
ASC-JMZ1 DMT5LJN Bladder cancer 2C94 Investigative [54]
Boldenone DM0EKO5 Discovery agent N.A. Investigative [56]
Calusterone DMBK2S8 Discovery agent N.A. Investigative [57]
CH-4933468 DM1ZF3Y Prostate cancer 2C82.0 Investigative [54]
Delta1-dihydrotestosterone DML6MVH Discovery agent N.A. Investigative [58]
DL-3 DME9ODX Prostate cancer 2C82.0 Investigative [54]
EPI-001 DMYWV81 Prostate cancer 2C82.0 Investigative [59]
GTx-027 DM315VL Solid tumour/cancer 2A00-2F9Z Investigative [60]
HYG-440 DM7XISZ Dermatological disease DA24.Y Investigative [61]
OXENDLONE DM6RJOI Discovery agent N.A. Investigative [62]
Palodesangren C DMKLVSO Discovery agent N.A. Investigative [62]
Palodesangren D DMY6NRC Discovery agent N.A. Investigative [62]
Palodesangren E DMUEK1N Discovery agent N.A. Investigative [62]
RU-59063 DM5D9UT Discovery agent N.A. Investigative [63]
SARMs DMILBO9 Solid tumour/cancer 2A00-2F9Z Investigative [54]
SX-ARPC DMEA36L Prostate cancer 2C82.0 Investigative [64]
Testetrol DMQDVNZ Hypogonadism 5A61.0 Investigative [65]
[3H]methyltrienolone DMTSGOW Discovery agent N.A. Investigative [56]
[3H]mibolerone DM6HDKQ Discovery agent N.A. Investigative [63]
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⏷ Show the Full List of 25 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Alopecia EA90 Skin from scalp 5.97E-06 0.25 0.78
Prostate cancer 2C82 Prostate 4.81E-01 -0.23 -0.29
Osteoporosis FA20 Bone marrow 6.77E-02 0.76 2.2
Myopathy 8A00.0 Muscle tissue 2.13E-01 -0.07 -0.11
Atopic dermatitis EA90 Skin 7.61E-08 -0.59 -2.99
Bladder cancer 2C82 Bladder tissue 4.00E-13 -1.62 -8.45
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⏷ Show the Full List of DTT Expression Under 6 Diseases

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