Target Information

Target General Infomation
Target ID
T11211
Former ID
TTDS00367
Target Name
Androgen receptor
Gene Name
AR
Synonyms
Dihydrotestosterone receptor; Testosterone receptor; AR
Target Type
Successful
Disease Alcoholic hepatitis [ICD9: 571.1; ICD10: K70.1]
Acne vulgaris [ICD9: 706.1; ICD10: L70.0]
Advanced prostate cancer [ICD9: 185; ICD10: C61]
Alopecia [ICD9: 704.09; ICD10: L65.9]
Bladder cancer [ICD9: 188; ICD10: C67]
Cardiovascular disorder [ICD10: I00-I99]
Cachexia [ICD9: 799.4; ICD10: R64]
Cystic fibrosis [ICD9: 277; ICD10: E84]
Contraception [ICD10: Z30]
Castration-resistant prostate cancer [ICD9: 185; ICD10: C61]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6]
Dermatological disease [ICD10: L00-L99]
Endocrine disease [ICD10: E00-E35]
Female androgenresponsive recurrent mammary cancer [ICD9: 174, 175; ICD10: C50]
Hormone deficiency [ICD10: E00-E90]
Heart failure [ICD9: 428; ICD10: I50]
Hormone refractory prostate cancer [ICD9: 140-229, 185; ICD10: C61]
Hypogonadism [ICD9: 257.2; ICD10: E23.0, E28.3, E29.1]
Male hormonal deficiencies [ICD10: E20-E35]
Male hypogonadism; Breast cancer [ICD9:257.2, 174, 175; ICD10: E23.0, E28.3, E29.1, C50]
Metastatic castration-resistant prostate cancer [ICD9: 140-229, 185; ICD10: C61]
Muscle atrophy [ICD10: M62.5]
Metastatic prostate cancer [ICD9: 185; ICD10: C61]
Osteoporosis in post-menopausal women [ICD9: 733; ICD10: M80-M81]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Prostate cancer [ICD9: 185; ICD10: C61]
Prostate hyperplasia [ICD10: N40]
Testosterone deficiency [ICD10: E29.1]
Unspecified [ICD code not available]
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. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.
BioChemical Class
Zinc-finger
Target Validation
T11211
UniProt ID
P10275
Sequence
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
Structure
1E3G; 1GS4; 1T5Z; 1T63; 1T65; 1XJ7; 1XOW; 1XQ3; 1Z95; 2AM9; 2AMA; 2AMB; 2AO6; 2AX6; 2AX7; 2AX8; 2AX9; 2AXA; 2HVC; 2OZ7; 2PIO; 2PIP; 2PIQ; 2PIR; 2PIT; 2PIU; 2PIV; 2PIW; 2PIX; 2PKL; 2PNU; 2Q7I; 2Q7J; 2Q7K; 2Q7L; 2YHD; 2YLO; 2YLP; 2YLQ; 2Z4J; 3B5R; 3B65; 3B66; 3B67; 3B68; 3BTR; 3L3X; 3L3Z; 3RLJ; 3RLL; 3V49; 3V4A; 3ZQT; 4HLW; 4K7A; 4OEA; 4OED; 4OEY; 4OEZ; 4OFR; 4OFU; 4OGH; 4OH5; 4OH6; 4OHA; 4OIL; 4OIU; 4OJ9; 4OJB; 4OK1; 4OKB; 4OKT; 4OKW; 4OKX; 4OLM
Drugs and Mode of Action
Drug(s) Bicalutamide Drug Info Approved Advanced prostate cancer [1], [2]
Cyproterone Drug Info Approved Prostate cancer [3]
Dromostanolone Drug Info Approved Female androgenresponsive recurrent mammary cancer [1], [4]
Enzalutamide Drug Info Approved Metastatic castration-resistant prostate cancer [5], [6], [7]
Ethylestrenol Drug Info Approved Testosterone deficiency [7]
Flufenamic Acid Drug Info Approved Dysmenorrhea [8], [7]
Fluoxymesterone Drug Info Approved Male hypogonadism; Breast cancer [1], [9], [7]
Flutamide Drug Info Approved Prostate cancer [10], [11]
Hydroxyflutamide Drug Info Approved Prostate cancer [12], [13]
Nandrolone Drug Info Approved Osteoporosis in post-menopausal women [1], [14]
Nilutamide Drug Info Approved Prostate cancer [12], [15]
Oxandrolone Drug Info Approved Alcoholic hepatitis [16], [17]
Testosterone Drug Info Approved Osteoporosis [18], [19]
DHEA Drug Info Phase 4 Cardiovascular disorder [20], [21]
Dihydrotestosterone Drug Info Phase 4 Prostate hyperplasia [22], [23]
ZANOTERONE Drug Info Phase 3 Prostate hyperplasia [24]
Androgen restored contraceptive Drug Info Phase 2 Contraception [25]
Antiandrogens Drug Info Phase 2 Endocrine disease [26]
ASCJ-9 topical Drug Info Phase 2 Alopecia [27]
CB-03-01 Drug Info Phase 2 Acne vulgaris [28]
Liproca Depot Drug Info Phase 2 Prostate cancer [29]
MK-0773 Drug Info Phase 2 Osteoporosis [30]
Testogen TDS Drug Info Phase 2 Hypogonadism [31]
Testosterone Drug Info Phase 2 Hormone deficiency [32]
TOK-001 Drug Info Phase 2 Prostate cancer [33], [34]
APC-100 Drug Info Phase 1/2 Castration-resistant prostate cancer [35]
ONC1-13B Drug Info Phase 1/2 Metastatic prostate cancer [36]
AZD-3514 Drug Info Phase 1 Hormone refractory prostate cancer [37]
AZD5312 Drug Info Phase 1 Prostate cancer [38]
Drug 2881078 Drug Info Phase 1 Heart failure [39]
PS-178990 Drug Info Phase 1 Muscle atrophy [40]
TESTOSTERONE BUCICLATE Drug Info Phase 1 Contraception [41]
GLPG-0492 Drug Info Preclinical Cachexia [42]
GW-275919 Drug Info Discontinued in Phase 2 Pain [43]
HE-2000 Drug Info Discontinued in Phase 2 Cystic fibrosis [44]
NP-619 Drug Info Discontinued in Phase 2 Alopecia [45]
Testosterone glucoside Drug Info Discontinued in Phase 2 Hypogonadism [46]
GSK2849466 Drug Info Discontinued in Phase 1 Heart failure [47]
LGD2941 Drug Info Discontinued in Phase 1 Osteoporosis [48]
Opterone Drug Info Discontinued in Phase 1 Hormone deficiency [49]
PF-06260414 Drug Info Discontinued in Phase 1 Cachexia [50]
LG-2293 Drug Info Terminated Prostate cancer [51]
ZD-3980 Drug Info Terminated Prostate hyperplasia [52]
Testosterone Drug Info Investigative Male hormonal deficiencies [53], [54]
Inhibitor 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane Drug Info [55]
11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol Drug Info [56]
6,11-dihydrothiochromeno[4,3-b]indol-8-ol Drug Info [56]
9alpha-Fluorocortisol Drug Info [57]
APC-100 Drug Info [35]
Calusterone Drug Info [58]
Flufenamic Acid Drug Info [59]
HE-2000 Drug Info [60]
Methyltrienolone Drug Info [61]
Mibolerone Drug Info [62]
Opterone Drug Info [63]
OXENDLONE Drug Info [64]
Palodesangren C Drug Info [64]
Palodesangren D Drug Info [64]
Palodesangren E Drug Info [64]
RU-59063 Drug Info [62]
TOK-001 Drug Info [34]
ZANOTERONE Drug Info [65]
Modulator 2849466 Drug Info
Andromustine Drug Info [66]
ASC-JMZ1 Drug Info [66]
AZD5312 Drug Info
Dihydrotestosterone Drug Info
Drug 2881078 Drug Info [67]
Enzalutamide Drug Info [7]
EPI-001 Drug Info [68]
Ethylestrenol Drug Info
GLPG-0492 Drug Info [69]
GSK2849466 Drug Info [70]
GTx-027 Drug Info [71]
GW-275919 Drug Info [43]
LG-2293 Drug Info [72]
LGD2941 Drug Info [73]
MK-0773 Drug Info [74]
NP-619 Drug Info [75]
PF-06260414 Drug Info [76]
RAD-140 Drug Info [77]
SARMs Drug Info [66]
Selective androgen receptor degraders Drug Info [66]
Testogen TDS Drug Info [63]
ZD-3980 Drug Info [78]
Antagonist Alpha-estradiol Drug Info [79]
Antiandrogens Drug Info [80]
ARN34 Drug Info [81]
ASC-JMX2 Drug Info [66]
AZD-3514 Drug Info [82]
Bicalutamide Drug Info [83], [84]
CB-03-01 Drug Info [85]
CH-4933468 Drug Info [66]
Cyproterone Drug Info [86]
DHEA Drug Info [87]
DL-3 Drug Info [66]
Flutamide Drug Info [83]
Hydroxyflutamide Drug Info [79], [81], [12]
HYG-440 Drug Info [88]
Liproca Depot Drug Info [89]
Nilutamide Drug Info [90]
ONC1-13B Drug Info [91]
SX-ARPC Drug Info [92]
Agonist Androgen receptor modulators Drug Info [66]
Androgen restored contraceptive Drug Info [93]
Boldenone Drug Info [61]
Delta1-dihydrotestosterone Drug Info [94]
Fluoxymesterone Drug Info [95], [96]
Nandrolone Drug Info [97]
Oxandrolone Drug Info [98]
Testetrol Drug Info [99]
Testosterone Drug Info [53], [54]
TESTOSTERONE BUCICLATE Drug Info [63]
Testosterone glucoside Drug Info [63]
Enhancer ASCJ-9 topical Drug Info [100]
Binder Dromostanolone Drug Info [101], [102]
PS-178990 Drug Info [103]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
DRM DRM Info
Pathways
KEGG Pathway Oocyte meiosis
Pathways in cancer
Prostate cancer
NetPath Pathway EGFR1 Signaling Pathway
AndrogenReceptor Signaling Pathway
FSH Signaling Pathway
Pathway Interaction Database Regulation of nuclear SMAD2/3 signaling
Coregulation of Androgen receptor activity
Regulation of Androgen receptor activity
Nongenotropic Androgen signaling
Regulation of nuclear beta catenin signaling and target gene transcription
FOXA1 transcription factor network
Notch-mediated HES/HEY network
Reactome Nuclear Receptor transcription pathway
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3
WikiPathways SIDS Susceptibility Pathways
Integrated Pancreatic Cancer Pathway
Prostate Cancer
Integrated Breast Cancer Pathway
Nuclear Receptors
Androgen receptor signaling pathway
References
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