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 Alopecia [ICD9: 704.09; ICD10: L65.9]
Alcoholic hepatitis [ICD9: 571.1; ICD10: K70.1]
Acne vulgaris [ICD9: 706.1; ICD10: L70.0]
Advanced prostate cancer [ICD9: 185; ICD10: C61]
Bladder cancer [ICD9: 188; ICD10: C67]
Contraception [ICD10: Z30]
Castration-resistant prostate cancer [ICD9: 185; ICD10: C61]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Cardiovascular disorder [ICD10: I00-I99]
Cachexia [ICD9: 799.4; ICD10: R64]
Cystic fibrosis [ICD9: 277; ICD10: E84]
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]
Muscle atrophy [ICD10: M62.5]
Metastatic prostate cancer [ICD9: 185; ICD10: C61]
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]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Osteoporosis in post-menopausal women [ICD9: 733; ICD10: M80-M81]
Prostate hyperplasia [ICD10: N40]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Prostate cancer [ICD9: 185; ICD10: C61]
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 [536361], [539888]
Cyproterone Drug Info Approved Prostate cancer [550706]
Dromostanolone Drug Info Approved Female androgenresponsive recurrent mammary cancer [536361], [541986]
Enzalutamide Drug Info Approved Metastatic castration-resistant prostate cancer [524719], [541894], [551871]
Ethylestrenol Drug Info Approved Testosterone deficiency [551871]
Flufenamic Acid Drug Info Approved Dysmenorrhea [539575], [551871]
Fluoxymesterone Drug Info Approved Male hypogonadism; Breast cancer [536361], [539886], [551871]
Flutamide Drug Info Approved Prostate cancer [538297], [541984]
Hydroxyflutamide Drug Info Approved Prostate cancer [536387], [539887]
Nandrolone Drug Info Approved Osteoporosis in post-menopausal women [536361], [541987]
Nilutamide Drug Info Approved Prostate cancer [536387], [539889]
Oxandrolone Drug Info Approved Alcoholic hepatitis [538317], [542098]
Testosterone Drug Info Approved Osteoporosis [536296], [539883]
DHEA Drug Info Phase 4 Cardiovascular disorder [525084], [539508]
Dihydrotestosterone Drug Info Phase 4 Prostate hyperplasia [521560], [539881]
ZANOTERONE Drug Info Phase 3 Prostate hyperplasia [545244]
Androgen restored contraceptive Drug Info Phase 2 Contraception [527054]
Antiandrogens Drug Info Phase 2 Endocrine disease [529385]
ASCJ-9 topical Drug Info Phase 2 Alopecia [523346]
CB-03-01 Drug Info Phase 2 Acne vulgaris [548553]
Liproca Depot Drug Info Phase 2 Prostate cancer [525060]
MK-0773 Drug Info Phase 2 Osteoporosis [522114]
Testogen TDS Drug Info Phase 2 Hypogonadism [524351]
Testosterone Drug Info Phase 2 Hormone deficiency [550655]
TOK-001 Drug Info Phase 2 Prostate cancer [532794], [543224]
APC-100 Drug Info Phase 1/2 Castration-resistant prostate cancer [550204]
ONC1-13B Drug Info Phase 1/2 Metastatic prostate cancer [549513]
AZD-3514 Drug Info Phase 1 Hormone refractory prostate cancer [523468]
AZD5312 Drug Info Phase 1 Prostate cancer [524767]
Drug 2881078 Drug Info Phase 1 Heart failure [525334]
PS-178990 Drug Info Phase 1 Muscle atrophy [548632]
TESTOSTERONE BUCICLATE Drug Info Phase 1 Contraception [526819]
GLPG-0492 Drug Info Preclinical Cachexia [547691]
GW-275919 Drug Info Discontinued in Phase 2 Pain [546813]
HE-2000 Drug Info Discontinued in Phase 2 Cystic fibrosis [546877]
NP-619 Drug Info Discontinued in Phase 2 Alopecia [548745]
Testosterone glucoside Drug Info Discontinued in Phase 2 Hypogonadism [547667]
GSK2849466 Drug Info Discontinued in Phase 1 Heart failure [549417]
LGD2941 Drug Info Discontinued in Phase 1 Osteoporosis [547162]
Opterone Drug Info Discontinued in Phase 1 Hormone deficiency [547562]
PF-06260414 Drug Info Discontinued in Phase 1 Cachexia [549537]
LG-2293 Drug Info Terminated Prostate cancer [546195]
ZD-3980 Drug Info Terminated Prostate hyperplasia [546660]
Testosterone Drug Info Investigative Male hormonal deficiencies [535239], [536683]
Inhibitor 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane Drug Info [528558]
11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol Drug Info [528123]
6,11-dihydrothiochromeno[4,3-b]indol-8-ol Drug Info [528123]
9alpha-Fluorocortisol Drug Info [551374]
APC-100 Drug Info [550204]
Calusterone Drug Info [551389]
Flufenamic Acid Drug Info [551392]
HE-2000 Drug Info [526848]
Methyltrienolone Drug Info [551393]
Mibolerone Drug Info [525861]
Opterone Drug Info [533385]
OXENDLONE Drug Info [534505]
Palodesangren C Drug Info [534505]
Palodesangren D Drug Info [534505]
Palodesangren E Drug Info [534505]
RU-59063 Drug Info [525861]
TOK-001 Drug Info [543224]
ZANOTERONE Drug Info [527548]
Modulator 2849466 Drug Info
Andromustine Drug Info [1572605]
ASC-JMZ1 Drug Info [1572605]
AZD5312 Drug Info
Dihydrotestosterone Drug Info
Drug 2881078 Drug Info [549527]
Enzalutamide Drug Info [551871]
EPI-001 Drug Info [525416]
Ethylestrenol Drug Info
GLPG-0492 Drug Info [532281]
GSK2849466 Drug Info [549418]
GTx-027 Drug Info [552011]
GW-275919 Drug Info [546813]
LG-2293 Drug Info [546196]
LGD2941 Drug Info [530124]
MK-0773 Drug Info [530821]
NP-619 Drug Info [548746]
PF-06260414 Drug Info [550356]
RAD-140 Drug Info [552010]
SARMs Drug Info [1572605]
Selective androgen receptor degraders Drug Info [1572605]
Testogen TDS Drug Info [533385]
ZD-3980 Drug Info [546661]
Antagonist Alpha-estradiol Drug Info [534842]
Antiandrogens Drug Info [531856]
ARN34 Drug Info [535939]
ASC-JMX2 Drug Info [1572605]
AZD-3514 Drug Info [532431]
Bicalutamide Drug Info [535561], [537480]
CB-03-01 Drug Info [527374]
CH-4933468 Drug Info [1572605]
Cyproterone Drug Info [537365]
DHEA Drug Info [525358]
DL-3 Drug Info [1572605]
Flutamide Drug Info [535561]
Hydroxyflutamide Drug Info [534842], [535939], [536387]
HYG-440 Drug Info [552008]
Liproca Depot Drug Info [527745]
Nilutamide Drug Info [536659]
ONC1-13B Drug Info [532660]
SX-ARPC Drug Info [551681]
Agonist Androgen receptor modulators Drug Info [1572605]
Androgen restored contraceptive Drug Info [551483]
Boldenone Drug Info [551393]
Delta1-dihydrotestosterone Drug Info [551383]
Fluoxymesterone Drug Info [536288], [537750]
Nandrolone Drug Info [536093]
Oxandrolone Drug Info [536376]
Testetrol Drug Info [525360]
Testosterone Drug Info [535239], [536683]
TESTOSTERONE BUCICLATE Drug Info [533385]
Testosterone glucoside Drug Info [533385]
Enhancer ASCJ-9 topical Drug Info [532450]
Binder Dromostanolone Drug Info [536002], [537807]
PS-178990 Drug Info [544063]
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
Ref 521560ClinicalTrials.gov (NCT00062790) Effect Of Dutasteride On Intraprostatic Dihydrotestosterone (DHT) Levels. U.S. National Institutes of Health.
Ref 522114ClinicalTrials.gov (NCT00529659) A Study of the Safety and Efficacy of MK-0773 in Women With Sarcopenia (Loss of Muscle Mass)(MK-0773-005). U.S. National Institutes of Health.
Ref 523346ClinicalTrials.gov (NCT01289574) Topical ASC-J9 Cream for Acne. U.S. National Institutes of Health.
Ref 523468ClinicalTrials.gov (NCT01351688) An Open Label Prostate Cancer Study in Japanese Patients. U.S. National Institutes of Health.
Ref 524351ClinicalTrials.gov (NCT01894308) A Dose Ranging Study to Examine Testagen TDS-Testosterone 5%. U.S. National Institutes of Health.
Ref 524719ClinicalTrials.gov (NCT02116582) A Study to Evaluate Enzalutamide After Abiraterone in Metastatic Castration-Resistant Prostate Cancer. U.S. National Institutes of Health.
Ref 524767ClinicalTrials.gov (NCT02144051) Phase I Open Label Dose Escalation Study to Investigate the Safety & Pharmacokinetics of AZD5312 in Patients With Androgen Receptor Tumors. U.S. National Institutes of Health.
Ref 525060ClinicalTrials.gov (NCT02341404) A Study of 2-hydroxyflutamide (Liproca Depot), Injected Into the Prostate in Patients With Localized Prostate Cancer. U.S. National Institutes of Health.
Ref 525084ClinicalTrials.gov (NCT02357472) The Effect of a Higher Dose of Dehydroepiandrosterone (DHEA) Supplementation in Poor Responders. U.S. National Institutes of Health.
Ref 525334ClinicalTrials.gov (NCT02567773) Safety, Tolerability, Pharmacokinetic (PK), and Pharmacodynamic Study of GSK2881078 and Study to Evaluate the Effect of CYP3A4 Inhibition on PK of GSK2881078.
Ref 526819Testosterone buciclate (20 Aet-1) in hypogonadal men: pharmacokinetics and pharmacodynamics of the new long-acting androgen ester. J Clin Endocrinol Metab. 1992 Nov;75(5):1204-10.
Ref 527054Treatment outcome in endodontics-the Toronto Study. Phase II: initial treatment. J Endod. 2004 May;30(5):302-9.
Ref 529385Phase II study of the pure non-steroidal antiandrogen nilutamide in prostatic cancer. Italian Prostatic Cancer Project (PONCAP). Eur J Cancer. 1991;27(9):1100-4.
Ref 532794Galeterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptor. Clin Cancer Res. 2014 Aug 1;20(15):4075-85.
Ref 535239Complexities of androgen action. J Am Acad Dermatol. 2001 Sep;45(3 Suppl):S87-94.
Ref 536296Emerging drugs for hypogonadism. Expert Opin Emerg Drugs. 2006 Nov;11(4):685-707.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536387Drug insight: role of the androgen receptor in the development and progression of prostate cancer. Nat Clin Pract Oncol. 2007 Apr;4(4):236-44.
Ref 536683Molecular mechanism of androgen action. Trends Endocrinol Metab. 1998 Oct 1;9(8):317-24.
Ref 538297FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075298.
Ref 538317FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076761.
Ref 539508(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2370).
Ref 539575(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2447).
Ref 539881(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2856).
Ref 539883(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2858).
Ref 539886(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2861).
Ref 539887(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2862).
Ref 539888(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2863).
Ref 539889(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2864).
Ref 541894(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6812).
Ref 541984(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6943).
Ref 541986(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6947).
Ref 541987(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6949).
Ref 542098(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7092).
Ref 543224(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8638).
Ref 545244Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002570)
Ref 546195Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006840)
Ref 546660Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009538)
Ref 546813Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010426)
Ref 546877Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010830)
Ref 547162Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013541)
Ref 547562Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017332)
Ref 547667Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018266)
Ref 547691Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018432)
Ref 548553Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026561)
Ref 548632Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027228)
Ref 548745Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028305)
Ref 549417Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036899)
Ref 549513Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800039208)
Ref 549537Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040072)
Ref 5502042011 Pipeline of Adamis Pharmaceuticals.
Ref 550655ARDANA ANNOUNCES PHASE I RESULTS FOR TESTOSTERONE CREAM. FDAnews report.
Ref 550706Drug information of Cyproterone, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525358Dehydroepiandrosterone, glucose-6-phosphate dehydrogenase, and longevity. Ageing Res Rev. 2004 Apr;3(2):171-87.
Ref 525360Estetrol review: profile and potential clinical applications. Climacteric. 2008;11 Suppl 1:47-58.
Ref 525416EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer. Oncotarget. 2015 Feb 28;6(6):3811-24.
Ref 525861J Med Chem. 2000 Aug 24;43(17):3344-7.Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand.
Ref 526848Dehydroepiandrosterone upregulates neural androgen receptor level and transcriptional activity. J Neurobiol. 2003 Nov;57(2):163-71.
Ref 527374Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist. Arzneimittelforschung. 2004;54(12):881-6.
Ref 527548J Med Chem. 1992 May 15;35(10):1663-70.Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles.
Ref 527745Effects of dihydrotestosterone and hydroxyflutamide on androgen receptors in cultured human breast cancer cells (EVSA-T). J Steroid Biochem Mol Biol. 1992 Jun;42(5):547-54.
Ref 528123Bioorg Med Chem Lett. 2006 Jun 15;16(12):3233-7. Epub 2006 Apr 5.Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands.
Ref 528558J Med Chem. 2006 Dec 14;49(25):7366-72.Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist.
Ref 530124Influence of testosterone and a novel SARM on gene expression in whole blood of Macaca fascicularis. J Steroid Biochem Mol Biol. 2009 Apr;114(3-5):167-73.
Ref 530821Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology. J Biol Chem. 2010 May 28;285(22):17054-64.
Ref 531856Steroid derivatives as pure antagonists of the androgen receptor. J Steroid Biochem Mol Biol. 2012 Oct;132(1-2):93-104.
Ref 532281GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophy. Pharmacol Res. 2013 Jun;72:9-24.
Ref 532431AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo. Mol Cancer Ther. 2013 Sep;12(9):1715-27.
Ref 532450Anti-androgen receptor ASC-J9 versus anti-androgens MDV3100 (Enzalutamide) or Casodex (Bicalutamide) leads to opposite effects on prostate cancer metastasis via differential modulation of macrophage infiltration and STAT3-CCL2 signaling. Cell Death Dis. 2013 Aug 8;4:e764.
Ref 532660Preclinical Development of ONC1-13B, Novel Antiandrogen for Prostate Cancer Treatment. J Cancer. 2014 Jan 21;5(2):133-42.
Ref 533385Evidence for a role of testosterone-androgen receptor interactions in mediating masculine sexual behavior in male rats. Endocrinology. 1989 Feb;124(2):618-26.
Ref 534505J Nat Prod. 1997 Oct;60(10):997-1002.Antiandrogenic natural Diels--Alder-type adducts from Brosimum rubescens.
Ref 534842Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. Biochem Pharmacol. 1998 May 1;55(9):1427-33.
Ref 535239Complexities of androgen action. J Am Acad Dermatol. 2001 Sep;45(3 Suppl):S87-94.
Ref 535561Androgen receptor as a target in androgen-independent prostate cancer. Urology. 2002 Sep;60(3 Suppl 1):132-8; discussion 138-9.
Ref 535939Ectopic expression of the amino-terminal peptide of androgen receptor leads to androgen receptor dysfunction and inhibition of androgen receptor-mediated prostate cancer growth. Mol Cell Endocrinol. 2004 Feb 12;214(1-2):175-87.
Ref 536002Endocrinological and pathological effects of anabolic-androgenic steroid in male rats. Endocr J. 2004 Aug;51(4):425-34.
Ref 536093Expression of androgen receptor on fibroblast and hepatocyte of rats after deep second-degree burn caused by scalding. Sichuan Da Xue Xue Bao Yi Xue Ban. 2005 May;36(3):362-4.
Ref 536288An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate. Endocrinology. 2007 Jan;148(1):363-73. Epub 2006 Oct 5.
Ref 536376The effect of oxandrolone treatment on human osteoblastic cells. J Burns Wounds. 2007 Mar 7;6:e4.
Ref 536387Drug insight: role of the androgen receptor in the development and progression of prostate cancer. Nat Clin Pract Oncol. 2007 Apr;4(4):236-44.
Ref 536659CX3CR1 is expressed by prostate epithelial cells and androgens regulate the levels of CX3CL1/fractalkine in the bone marrow: potential role in prostate cancer bone tropism. Cancer Res. 2008 Mar 15;68(6):1715-22.
Ref 536683Molecular mechanism of androgen action. Trends Endocrinol Metab. 1998 Oct 1;9(8):317-24.
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