Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T11211
(Former ID: TTDS00367)
|
|||||
| Target Name |
Androgen receptor (AR)
|
|||||
| Synonyms |
Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR
|
|||||
| Gene Name |
AR
|
|||||
| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 11 Target-related Diseases | + | ||||
| 1 | Acne vulgaris [ICD-11: ED80] | |||||
| 2 | Acute myeloid leukaemia [ICD-11: 2A60] | |||||
| 3 | Alcoholic liver disease [ICD-11: DB94] | |||||
| 4 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
| 5 | Chronic obstructive pulmonary disease [ICD-11: CA22] | |||||
| 6 | Female pelvic pain [ICD-11: GA34] | |||||
| 7 | Hypo-osmolality/hyponatraemia [ICD-11: 5C72] | |||||
| 8 | Low bone mass disorder [ICD-11: FB83] | |||||
| 9 | Mammary tumour [ICD-11: 2C60-2C6Z] | |||||
| 10 | Prostate cancer [ICD-11: 2C82] | |||||
| 11 | Testicular dysfunction [ICD-11: 5A81] | |||||
| 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.
Click to Show/Hide
|
|||||
| BioChemical Class |
Nuclear hormone receptor
|
|||||
| UniProt ID | ||||||
| Sequence |
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII SVQVPKILSGKVKPIYFHTQ Click to Show/Hide
|
|||||
| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A01831 | |||||
| HIT2.0 ID | T20JZ2 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 19 Approved Drugs | + | ||||
| 1 | ARN-509 | Drug Info | Approved | Acute myeloid leukaemia | [2] | |
| 2 | Bicalutamide | Drug Info | Approved | Prostate cancer | [3], [4] | |
| 3 | Clascoterone | Drug Info | Approved | Acne vulgaris | [5] | |
| 4 | Cyproterone | Drug Info | Approved | Prostate cancer | [6] | |
| 5 | Darolutamide | Drug Info | Approved | Prostate cancer | [7] | |
| 6 | Dromostanolone | Drug Info | Approved | Mammary tumour | [4], [8] | |
| 7 | Enzalutamide | Drug Info | Approved | Prostate cancer | [9] | |
| 8 | Ethylestrenol | Drug Info | Approved | Testosterone deficiency | [10] | |
| 9 | Fludrocortisone | Drug Info | Approved | Cerebral salt-wasting syndrome | [11], [12] | |
| 10 | Flufenamic Acid | Drug Info | Approved | Dysmenorrhea | [10], [13] | |
| 11 | Fluoxymesterone | Drug Info | Approved | Breast cancer | [4], [10], [14] | |
| 12 | Flutamide | Drug Info | Approved | Prostate cancer | [15], [16] | |
| 13 | Hydroxyflutamide | Drug Info | Approved | Prostate cancer | [17], [18] | |
| 14 | Nandrolone | Drug Info | Approved | Osteoporosis | [19], [4] | |
| 15 | Nilutamide | Drug Info | Approved | Prostate cancer | [20], [18] | |
| 16 | Oxandrolone | Drug Info | Approved | Alcoholic hepatitis | [21], [22] | |
| 17 | Prasterone | Drug Info | Approved | Chronic obstructive pulmonary disease | [23] | |
| 18 | Testosterone | Drug Info | Approved | Osteoporosis | [24], [25] | |
| 19 | Dihydrotestosterone | Drug Info | Phase 4 | Prostate hyperplasia | [26], [27] | |
| Clinical Trial Drug(s) | [+] 21 Clinical Trial Drugs | + | ||||
| 1 | HC-1119 | Drug Info | Phase 3 | Prostate cancer | [28] | |
| 2 | ZANOTERONE | Drug Info | Phase 3 | Prostate hyperplasia | [29] | |
| 3 | ASC-J9 | Drug Info | Phase 2 | Thrombosis | [30] | |
| 4 | ASCJ-9 | Drug Info | Phase 2 | Alopecia | [31] | |
| 5 | AZD5312 | Drug Info | Phase 2 | Prostate cancer | [32] | |
| 6 | MK-0773 | Drug Info | Phase 2 | Osteoporosis | [33] | |
| 7 | Testogen TDS | Drug Info | Phase 2 | Hypogonadism | [34] | |
| 8 | TOK-001 | Drug Info | Phase 2 | Prostate cancer | [35], [36] | |
| 9 | APC-100 | Drug Info | Phase 1/2 | Prostate cancer | [37] | |
| 10 | ARV-110 | Drug Info | Phase 1/2 | Prostate cancer | [38] | |
| 11 | ARV-471 | Drug Info | Phase 1/2 | Breast cancer | [39] | |
| 12 | ONC1-13B | Drug Info | Phase 1/2 | Prostate cancer | [40] | |
| 13 | AZD-3514 | Drug Info | Phase 1 | Prostate cancer | [41] | |
| 14 | CC-94676 | Drug Info | Phase 1 | Prostate cancer | [42] | |
| 15 | Drug 2881078 | Drug Info | Phase 1 | Heart failure | [43] | |
| 16 | DT-200 | Drug Info | Phase 1 | Duchenne dystrophy | [44] | |
| 17 | EPI-7386 | Drug Info | Phase 1 | Prostate cancer | [45] | |
| 18 | PS-178990 | Drug Info | Phase 1 | Muscle atrophy | [46] | |
| 19 | RAD-140 | Drug Info | Phase 1 | Breast cancer | [32] | |
| 20 | TAS3681 | Drug Info | Phase 1 | Prostate cancer | [32] | |
| 21 | TESTOSTERONE BUCICLATE | Drug Info | Phase 1 | Contraception | [47] | |
| Discontinued Drug(s) | [+] 11 Discontinued Drugs | + | ||||
| 1 | GW-275919 | Drug Info | Discontinued in Phase 2 | Pain | [48] | |
| 2 | HE-2000 | Drug Info | Discontinued in Phase 2 | Cystic fibrosis | [49] | |
| 3 | NP-619 | Drug Info | Discontinued in Phase 2 | Alopecia | [50] | |
| 4 | Testosterone glucoside | Drug Info | Discontinued in Phase 2 | Hypogonadism | [51] | |
| 5 | GSK2849466 | Drug Info | Discontinued in Phase 1 | Heart failure | [52] | |
| 6 | LGD2941 | Drug Info | Discontinued in Phase 1 | Osteoporosis | [53] | |
| 7 | MX-4509 | Drug Info | Discontinued in Phase 1 | Neurological disorder | [54] | |
| 8 | Opterone | Drug Info | Discontinued in Phase 1 | Hormone deficiency | [55] | |
| 9 | PF-06260414 | Drug Info | Discontinued in Phase 1 | Cachexia | [56] | |
| 10 | LG-2293 | Drug Info | Terminated | Prostate cancer | [58] | |
| 11 | ZD-3980 | Drug Info | Terminated | Prostate hyperplasia | [59] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | GLPG-0492 | Drug Info | Preclinical | Cachexia | [57] | |
| Mode of Action | [+] 7 Modes of Action | + | ||||
| Inhibitor | [+] 22 Inhibitor drugs | + | ||||
| 1 | ARN-509 | Drug Info | [2] | |||
| 2 | Fludrocortisone | Drug Info | [65] | |||
| 3 | Flufenamic Acid | Drug Info | [66] | |||
| 4 | HC-1119 | Drug Info | [78] | |||
| 5 | ZANOTERONE | Drug Info | [79] | |||
| 6 | ASC-J9 | Drug Info | [80] | |||
| 7 | TOK-001 | Drug Info | [35] | |||
| 8 | APC-100 | Drug Info | [37] | |||
| 9 | EPI-7386 | Drug Info | [90] | |||
| 10 | HE-2000 | Drug Info | [93] | |||
| 11 | Opterone | Drug Info | [84] | |||
| 12 | 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane | Drug Info | [101] | |||
| 13 | 11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol | Drug Info | [102] | |||
| 14 | 6,11-dihydrothiochromeno[4,3-b]indol-8-ol | Drug Info | [102] | |||
| 15 | Calusterone | Drug Info | [105] | |||
| 16 | OXENDLONE | Drug Info | [110] | |||
| 17 | Palodesangren C | Drug Info | [110] | |||
| 18 | Palodesangren D | Drug Info | [110] | |||
| 19 | Palodesangren E | Drug Info | [110] | |||
| 20 | RU-59063 | Drug Info | [111] | |||
| 21 | [3H]methyltrienolone | Drug Info | [104] | |||
| 22 | [3H]mibolerone | Drug Info | [111] | |||
| Antagonist | [+] 18 Antagonist drugs | + | ||||
| 1 | Bicalutamide | Drug Info | [1], [60] | |||
| 2 | Clascoterone | Drug Info | [5] | |||
| 3 | Cyproterone | Drug Info | [61] | |||
| 4 | Darolutamide | Drug Info | [7] | |||
| 5 | Flutamide | Drug Info | [1] | |||
| 6 | Hydroxyflutamide | Drug Info | [18], [69], [70] | |||
| 7 | Nilutamide | Drug Info | [72] | |||
| 8 | Prasterone | Drug Info | [74] | |||
| 9 | ONC1-13B | Drug Info | [87] | |||
| 10 | AZD-3514 | Drug Info | [88] | |||
| 11 | TAS3681 | Drug Info | [32] | |||
| 12 | MX-4509 | Drug Info | [70] | |||
| 13 | ARN34 | Drug Info | [69] | |||
| 14 | ASC-JMX2 | Drug Info | [103] | |||
| 15 | CH-4933468 | Drug Info | [103] | |||
| 16 | DL-3 | Drug Info | [103] | |||
| 17 | HYG-440 | Drug Info | [109] | |||
| 18 | SX-ARPC | Drug Info | [112] | |||
| Binder | [+] 2 Binder drugs | + | ||||
| 1 | Dromostanolone | Drug Info | [62], [63] | |||
| 2 | PS-178990 | Drug Info | [91] | |||
| Modulator | [+] 22 Modulator drugs | + | ||||
| 1 | Enzalutamide | Drug Info | [10] | |||
| 2 | Ethylestrenol | Drug Info | [64] | |||
| 3 | Dihydrotestosterone | Drug Info | [77] | |||
| 4 | AZD5312 | Drug Info | [82] | |||
| 5 | MK-0773 | Drug Info | [83] | |||
| 6 | Testogen TDS | Drug Info | [84] | |||
| 7 | Drug 2881078 | Drug Info | [89] | |||
| 8 | DT-200 | Drug Info | [44] | |||
| 9 | RAD-140 | Drug Info | [92] | |||
| 10 | GW-275919 | Drug Info | [48] | |||
| 11 | NP-619 | Drug Info | [94] | |||
| 12 | GSK2849466 | Drug Info | [95] | |||
| 13 | LGD2941 | Drug Info | [96] | |||
| 14 | PF-06260414 | Drug Info | [97] | |||
| 15 | GLPG-0492 | Drug Info | [98] | |||
| 16 | LG-2293 | Drug Info | [99] | |||
| 17 | ZD-3980 | Drug Info | [100] | |||
| 18 | Andromustine | Drug Info | [103] | |||
| 19 | ASC-JMZ1 | Drug Info | [103] | |||
| 20 | EPI-001 | Drug Info | [107] | |||
| 21 | GTx-027 | Drug Info | [108] | |||
| 22 | SARMs | Drug Info | [103] | |||
| Agonist | [+] 9 Agonist drugs | + | ||||
| 1 | Fluoxymesterone | Drug Info | [67], [68] | |||
| 2 | Nandrolone | Drug Info | [71] | |||
| 3 | Oxandrolone | Drug Info | [73] | |||
| 4 | Testosterone | Drug Info | [75], [76] | |||
| 5 | TESTOSTERONE BUCICLATE | Drug Info | [84] | |||
| 6 | Testosterone glucoside | Drug Info | [84] | |||
| 7 | Boldenone | Drug Info | [104] | |||
| 8 | Delta1-dihydrotestosterone | Drug Info | [106] | |||
| 9 | Testetrol | Drug Info | [113] | |||
| Enhancer | [+] 1 Enhancer drugs | + | ||||
| 1 | ASCJ-9 | Drug Info | [81] | |||
| Degrader | [+] 3 Degrader drugs | + | ||||
| 1 | ARV-110 | Drug Info | [85] | |||
| 2 | ARV-471 | Drug Info | [86] | |||
| 3 | CC-94676 | Drug Info | [42] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Drug Resistance Mutation (DRM) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Oocyte meiosis | |||||
| 2 | Pathways in cancer | |||||
| 3 | Prostate cancer | |||||
| NetPath Pathway | [+] 3 NetPath Pathways | + | ||||
| 1 | EGFR1 Signaling Pathway | |||||
| 2 | AndrogenReceptor Signaling Pathway | |||||
| 3 | FSH Signaling Pathway | |||||
| PID Pathway | [+] 7 PID Pathways | + | ||||
| 1 | Regulation of nuclear SMAD2/3 signaling | |||||
| 2 | Coregulation of Androgen receptor activity | |||||
| 3 | Regulation of Androgen receptor activity | |||||
| 4 | Nongenotropic Androgen signaling | |||||
| 5 | Regulation of nuclear beta catenin signaling and target gene transcription | |||||
| 6 | FOXA1 transcription factor network | |||||
| 7 | Notch-mediated HES/HEY network | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Nuclear Receptor transcription pathway | |||||
| 2 | Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 | |||||
| WikiPathways | [+] 6 WikiPathways | + | ||||
| 1 | SIDS Susceptibility Pathways | |||||
| 2 | Integrated Pancreatic Cancer Pathway | |||||
| 3 | Prostate Cancer | |||||
| 4 | Integrated Breast Cancer Pathway | |||||
| 5 | Nuclear Receptors | |||||
| 6 | Androgen receptor signaling pathway | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Androgen receptor as a target in androgen-independent prostate cancer. Urology. 2002 Sep;60(3 Suppl 1):132-8; discussion 138-9. | |||||
| REF 2 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 3 | URL: 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 4 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020 | |||||
| REF 6 | Drug information of Cyproterone, 2008. eduDrugs. | |||||
| REF 7 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019 | |||||
| REF 8 | URL: 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 9 | Nat Rev Drug Discov. 2013 Feb;12(2):87-90. | |||||
| REF 10 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 11 | URL: 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: 2873). | |||||
| REF 12 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010060. | |||||
| REF 13 | URL: 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 14 | URL: 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 15 | URL: 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 16 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075298. | |||||
| REF 17 | URL: 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 18 | Drug 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 19 | URL: 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 20 | URL: 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 21 | URL: 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 22 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076761. | |||||
| REF 23 | Direct agonist/antagonist functions of dehydroepiandrosterone. Endocrinology. 2005 Nov;146(11):4568-76. | |||||
| REF 24 | URL: 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 25 | Emerging drugs for hypogonadism. Expert Opin Emerg Drugs. 2006 Nov;11(4):685-707. | |||||
| REF 26 | URL: 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 27 | ClinicalTrials.gov (NCT00062790) Effect Of Dutasteride On Intraprostatic Dihydrotestosterone (DHT) Levels. U.S. National Institutes of Health. | |||||
| REF 28 | ClinicalTrials.gov (NCT03850795) HC-1119 Versus Enzalutamide in Metastatic Castration-Resistant Prostate Cancer (mCRPC). U.S. National Institutes of Health. | |||||
| REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002570) | |||||
| REF 30 | ClinicalTrials.gov (NCT03612856) Safety and Efficacy Study of AB023 (Xisomab 3G3) in End Stage Renal Disease Patients on Chronic Hemodialysis. U.S. National Institutes of Health. | |||||
| REF 31 | ClinicalTrials.gov (NCT01289574) Topical ASC-J9 Cream for Acne. U.S. National Institutes of Health. | |||||
| REF 32 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 33 | ClinicalTrials.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 34 | ClinicalTrials.gov (NCT01894308) A Dose Ranging Study to Examine Testagen TDS-Testosterone 5%. U.S. National Institutes of Health. | |||||
| REF 35 | URL: 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 36 | Galeterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptor. Clin Cancer Res. 2014 Aug 1;20(15):4075-85. | |||||
| REF 37 | 2011 Pipeline of Adamis Pharmaceuticals. | |||||
| REF 38 | ClinicalTrials.gov (NCT03888612) Trial of ARV-110 in Patients With Metastatic Castration Resistant Prostate Cancer (mCRPC). U.S. National Institutes of Health. | |||||
| REF 39 | ClinicalTrials.gov (NCT04072952) A Phase 1/2 Trial of ARV-471 Alone and in Combination With Palbociclib (IBRANCE) in Patients With ER+/HER2- Locally Advanced or Metastatic Breast Cancer (mBC). U.S. National Institutes of Health. | |||||
| REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800039208) | |||||
| REF 41 | ClinicalTrials.gov (NCT01351688) An Open Label Prostate Cancer Study in Japanese Patients. U.S. National Institutes of Health. | |||||
| REF 42 | ClinicalTrials.gov (NCT04428788) Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of CC-94676 in Subjects With Metastatic Castration-Resistant Prostate Cancer. U.S. National Institutes of Health. | |||||
| REF 43 | ClinicalTrials.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 44 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 45 | ClinicalTrials.gov (NCT04421222) Oral EPI-7386 in Patients With Metastatic Castration-Resistant Prostate Cancer (EPI-7386). U.S. National Institutes of Health. | |||||
| REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027228) | |||||
| REF 47 | Testosterone 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 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010426) | |||||
| REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010830) | |||||
| REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028305) | |||||
| REF 51 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018266) | |||||
| REF 52 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036899) | |||||
| REF 53 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013541) | |||||
| REF 54 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020680) | |||||
| REF 55 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017332) | |||||
| REF 56 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040072) | |||||
| REF 57 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018432) | |||||
| REF 58 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006840) | |||||
| REF 59 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009538) | |||||
| REF 60 | Androgen receptor overexpression induces tamoxifen resistance in human breast cancer cells. Breast Cancer Res Treat. 2010 May;121(1):1-11. | |||||
| REF 61 | Coactivator selective regulation of androgen receptor activity. Steroids. 2009 Aug;74(8):669-74. | |||||
| REF 62 | Endocrinological and pathological effects of anabolic-androgenic steroid in male rats. Endocr J. 2004 Aug;51(4):425-34. | |||||
| REF 63 | Effects of 5-fluorouracil and 2 alpha-methyldihydrotestosterone propionate on the growth of human breast carcinoma MCF-7 in vitro. Eur J Cancer Clin Oncol. 1983 Sep;19(9):1231-7. | |||||
| REF 64 | Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, ... Endocrinology. 1984 Jun;114(6):2100-6. | |||||
| REF 65 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 66 | Ouellet M, Percival MD: Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms. Biochem J. 1995 Feb 15;306 ( Pt 1):247-51. | |||||
| REF 67 | An 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. | |||||
| REF 68 | Endocrine-responsive pancreatic carcinoma: steroid binding and cytotoxicity studies in human tumor cell lines. Cancer Res. 1986 May;46(5):2276-81. | |||||
| REF 69 | Ectopic 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 70 | Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. Biochem Pharmacol. 1998 May 1;55(9):1427-33. | |||||
| REF 71 | Expression 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 72 | CX3CR1 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 73 | The effect of oxandrolone treatment on human osteoblastic cells. J Burns Wounds. 2007 Mar 7;6:e4. | |||||
| REF 74 | Dehydroepiandrosterone, glucose-6-phosphate dehydrogenase, and longevity. Ageing Res Rev. 2004 Apr;3(2):171-87. | |||||
| REF 75 | Molecular mechanism of androgen action. Trends Endocrinol Metab. 1998 Oct 1;9(8):317-24. | |||||
| REF 76 | Complexities of androgen action. J Am Acad Dermatol. 2001 Sep;45(3 Suppl):S87-94. | |||||
| REF 77 | Inhibition of the dihydrotestosterone-activated androgen receptor by nuclear receptor corepressor. Mol Endocrinol. 2002 Jul;16(7):1492-501. | |||||
| REF 78 | Clinical pipeline report, company report or official report of Hinova Pharmaceuticals. | |||||
| REF 79 | Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. J Med Chem. 1992 May 15;35(10):1663-70. | |||||
| REF 80 | New therapeutic approach to suppress castration-resistant prostate cancer using ASC-J9 via targeting androgen receptor in selective prostate cells. Am J Pathol. 2013 Feb;182(2):460-73. | |||||
| REF 81 | Anti-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 82 | Company report (Astrazeneca) | |||||
| REF 83 | Discovery 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 84 | Evidence for a role of testosterone-androgen receptor interactions in mediating masculine sexual behavior in male rats. Endocrinology. 1989 Feb;124(2):618-26. | |||||
| REF 85 | Clinical pipeline report, company report or official report of Arvinas. | |||||
| REF 86 | Targeting estrogen receptor alpha for degradation with PROTACs: A promising approach to overcome endocrine resistance. Eur J Med Chem. 2020 Nov 15;206:112689. | |||||
| REF 87 | Preclinical Development of ONC1-13B, Novel Antiandrogen for Prostate Cancer Treatment. J Cancer. 2014 Jan 21;5(2):133-42. | |||||
| REF 88 | AZD3514: 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 89 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800039743) | |||||
| REF 90 | Clinical pipeline report, company report or official report of ESSA Pharma. | |||||
| REF 91 | Selective androgen receptor modulators in preclinical and clinical development. Nucl Recept Signal. 2008; 6: e010. | |||||
| REF 92 | Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Med Chem Lett. 2010 Dec 2;2(2):124-9. | |||||
| REF 93 | Dehydroepiandrosterone upregulates neural androgen receptor level and transcriptional activity. J Neurobiol. 2003 Nov;57(2):163-71. | |||||
| REF 94 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028305) | |||||
| REF 95 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036899) | |||||
| REF 96 | Influence 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 97 | Phase I clinical trail of PF-06260414 for treating cachexia. Pfizer Inc. | |||||
| REF 98 | GLPG0492, 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 99 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006840) | |||||
| REF 100 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009538) | |||||
| REF 101 | Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist. J Med Chem. 2006 Dec 14;49(25):7366-72. | |||||
| REF 102 | Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3233-7. | |||||
| REF 103 | The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954. | |||||
| REF 104 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 105 | MR appearance of intra-abdominal metastatic melanoma. Magn Reson Imaging. 1992;10(4):705-8. | |||||
| REF 106 | 17beta-hydroxy-5alpha-androst-1-en-3-one (1-testosterone) is a potent androgen with anabolic properties. Toxicol Lett. 2006 Aug 20;165(2):149-55. | |||||
| REF 107 | EPI-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 108 | Selective androgen receptor modulators (SARMs) negatively regulate triple-negative breast cancer growth and epithelial:mesenchymal stem cell signaling. PLoS One. 2014 Jul 29;9(7):e103202. | |||||
| REF 109 | Clinical pipeline report, company report or official report of Hygeia Therapeutics. | |||||
| REF 110 | Antiandrogenic natural Diels--Alder-type adducts from Brosimum rubescens. J Nat Prod. 1997 Oct;60(10):997-1002. | |||||
| REF 111 | Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile... J Med Chem. 2000 Aug 24;43(17):3344-7. | |||||
| REF 112 | Clinical pipeline report, company report or official report of Progenics Pharmaceuticals Serometrix. | |||||
| REF 113 | Estetrol review: profile and potential clinical applications. Climacteric. 2008;11 Suppl 1:47-58. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.