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Androgen receptor
An androgen receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P10275]
Synonyms
Dihydrotestosterone receptor;
Nuclear receptor subfamily 3 group C member 4
Research
Bioassay Publications (165)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 12 (7.27) | 18.2507 |
2000's | 59 (35.76) | 29.6817 |
2010's | 74 (44.85) | 24.3611 |
2020's | 20 (12.12) | 2.80 |
Compounds (97)
Drugs with Potency Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
mifepristone | Homo sapiens (human) | Potency | 0.0050 | 1 | 1 |
onapristone | Homo sapiens (human) | Potency | 0.2690 | 1 | 1 |
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bicalutamide | Homo sapiens (human) | IC50 | 3.3371 | 56 | 56 |
bicalutamide | Homo sapiens (human) | Ki | 0.4925 | 21 | 23 |
flufenamic acid | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
flutamide | Homo sapiens (human) | IC50 | 16.8697 | 7 | 7 |
flutamide | Homo sapiens (human) | Ki | 2.5000 | 2 | 2 |
entinostat | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
nilutamide | Homo sapiens (human) | IC50 | 1.4045 | 4 | 4 |
masoprocol | Homo sapiens (human) | IC50 | 32.9333 | 3 | 3 |
salicylamide | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
prednisolone | Homo sapiens (human) | IC50 | 18.0000 | 2 | 2 |
prednisolone | Homo sapiens (human) | Ki | 2.6807 | 3 | 3 |
3,3',5-triiodothyroacetic acid | Homo sapiens (human) | IC50 | 34.8000 | 1 | 1 |
spironolactone | Homo sapiens (human) | IC50 | 0.3585 | 6 | 6 |
spironolactone | Homo sapiens (human) | Ki | 0.0394 | 1 | 1 |
oxandrolone | Homo sapiens (human) | IC50 | 0.0008 | 1 | 1 |
oxandrolone | Homo sapiens (human) | Ki | 0.0620 | 1 | 1 |
triiodothyronine | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
testosterone propionate | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
medroxyprogesterone acetate | Homo sapiens (human) | IC50 | 0.0061 | 2 | 2 |
medroxyprogesterone acetate | Homo sapiens (human) | Ki | 0.0029 | 5 | 5 |
fluoxymesterone | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
fluoxymesterone | Homo sapiens (human) | Ki | 0.0057 | 2 | 2 |
bisphenol a | Homo sapiens (human) | IC50 | 5.9000 | 1 | 1 |
cyproterone acetate | Homo sapiens (human) | IC50 | 0.1408 | 2 | 2 |
cyproterone acetate | Homo sapiens (human) | Ki | 0.0140 | 1 | 1 |
flavanone | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
androstenediol | Homo sapiens (human) | IC50 | 0.2210 | 2 | 2 |
dihydrotestosterone | Homo sapiens (human) | IC50 | 5.0026 | 26 | 26 |
dihydrotestosterone | Homo sapiens (human) | Ki | 0.0014 | 19 | 19 |
flavone | Homo sapiens (human) | IC50 | 5.9000 | 1 | 2 |
3-hydroxyflavone | Homo sapiens (human) | IC50 | 23.5000 | 1 | 1 |
1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane | Homo sapiens (human) | IC50 | 0.0427 | 1 | 1 |
raspberry ketone | Homo sapiens (human) | IC50 | 251.5945 | 1 | 2 |
zingerone | Homo sapiens (human) | IC50 | 152.1780 | 1 | 2 |
mifepristone | Homo sapiens (human) | IC50 | 0.2988 | 18 | 21 |
mifepristone | Homo sapiens (human) | Ki | 0.0087 | 6 | 6 |
nitrogenase stabilizing-protective protein, bacteria | Homo sapiens (human) | GI50 | 1.8000 | 1 | 1 |
nitrogenase stabilizing-protective protein, bacteria | Homo sapiens (human) | IC50 | 4.0328 | 10 | 10 |
nitrogenase stabilizing-protective protein, bacteria | Homo sapiens (human) | Ki | 0.7418 | 6 | 6 |
5-hydroxyflavone | Homo sapiens (human) | IC50 | 0.6573 | 2 | 3 |
hydroxyflutamide | Homo sapiens (human) | IC50 | 2.6192 | 19 | 19 |
hydroxyflutamide | Homo sapiens (human) | Ki | 0.0697 | 9 | 9 |
5-Methoxyflavone | Homo sapiens (human) | IC50 | 8.7000 | 1 | 1 |
6-methoxyflavanone | Homo sapiens (human) | IC50 | 39.5000 | 1 | 1 |
5,5-dimethyl-3-(alpha,alpha,alpha,4-tetrafluoro-3-tolyl)hydantoin | Homo sapiens (human) | IC50 | 4.4000 | 1 | 1 |
4-(3,4,4-trimethyl-5-oxo-2-thioxo-1-imidazolidinyl)-2-(trifluoromethyl)benzonitrile | Homo sapiens (human) | IC50 | 0.0150 | 1 | 1 |
ru 58841 | Homo sapiens (human) | IC50 | 0.0239 | 7 | 7 |
2'-hydroxyflavone | Homo sapiens (human) | IC50 | 5.5000 | 2 | 2 |
triptophenolide | Homo sapiens (human) | IC50 | 0.3760 | 3 | 3 |
2'-hydroxyflavanone | Homo sapiens (human) | IC50 | 3.7000 | 2 | 2 |
metribolone | Homo sapiens (human) | IC50 | 0.0040 | 3 | 3 |
metribolone | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
(S)-bicalutamide | Homo sapiens (human) | Ki | 0.3650 | 1 | 1 |
eplerenone | Homo sapiens (human) | IC50 | 13.4000 | 5 | 5 |
2-(2-phenoxyethylsulfonyl)-1H-benzimidazole | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
tolfenamic acid | Homo sapiens (human) | IC50 | 52.4500 | 2 | 2 |
N-(4-phenylmethoxyphenyl)methanesulfonamide | Homo sapiens (human) | IC50 | 6.1100 | 1 | 1 |
7-benzyloxy-4-trifluoromethylcoumarin | Homo sapiens (human) | IC50 | 1.1800 | 1 | 1 |
6-hydroxyflavanone | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
epi 001 | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
biochanin a | Homo sapiens (human) | IC50 | 1,600.0000 | 1 | 1 |
apigenin | Homo sapiens (human) | IC50 | 5.2000 | 1 | 1 |
calcitriol | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
kaempferol | Homo sapiens (human) | IC50 | 9.7000 | 1 | 1 |
genistein | Homo sapiens (human) | IC50 | 1,300.0000 | 1 | 1 |
pyrvinium | Homo sapiens (human) | IC50 | 0.1900 | 1 | 1 |
dorzolamide | Homo sapiens (human) | IC50 | 0.0650 | 1 | 1 |
onapristone | Homo sapiens (human) | IC50 | 0.2690 | 3 | 3 |
onapristone | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | IC50 | 0.2200 | 1 | 1 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | Ki | 0.2400 | 1 | 1 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | IC50 | 0.6600 | 1 | 1 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | Ki | 0.3150 | 1 | 1 |
lonaprisan | Homo sapiens (human) | IC50 | 0.0540 | 1 | 1 |
asoprisnil | Homo sapiens (human) | IC50 | 0.0076 | 2 | 2 |
zk 216348 | Homo sapiens (human) | IC50 | 0.6310 | 1 | 1 |
andarine | Homo sapiens (human) | Ki | 0.0040 | 2 | 2 |
lg 121071 | Homo sapiens (human) | IC50 | 7.3537 | 3 | 3 |
lg 121071 | Homo sapiens (human) | Ki | 0.0126 | 5 | 5 |
bms-564929 | Homo sapiens (human) | Ki | 0.0042 | 6 | 6 |
way-362450 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
3beta-hydroxy-17-(1h-benzimidazole-1-yl)androsta-5,16-diene | Homo sapiens (human) | IC50 | 1.1080 | 1 | 1 |
mk 2866 | Homo sapiens (human) | IC50 | 0.0038 | 1 | 1 |
mk 2866 | Homo sapiens (human) | Ki | 0.0022 | 2 | 2 |
lgd 2226 | Homo sapiens (human) | IC50 | 10.0000 | 3 | 3 |
lgd 2226 | Homo sapiens (human) | Ki | 0.0026 | 8 | 8 |
crizotinib | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
lg190155 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
lg190178 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
mdv 3100 | Homo sapiens (human) | GI50 | 0.2050 | 2 | 2 |
mdv 3100 | Homo sapiens (human) | IC50 | 4.4049 | 28 | 28 |
mdv 3100 | Homo sapiens (human) | Ki | 1.4606 | 6 | 6 |
way 252623 | Homo sapiens (human) | IC50 | 2.3000 | 1 | 1 |
apalutamide | Homo sapiens (human) | IC50 | 0.0981 | 4 | 4 |
apalutamide | Homo sapiens (human) | Ki | 0.5266 | 3 | 3 |
pf 998425 | Homo sapiens (human) | IC50 | 0.0466 | 5 | 5 |
lgd 3303 | Homo sapiens (human) | Ki | 0.0009 | 1 | 1 |
nitd 609 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
pf-03882845 | Homo sapiens (human) | IC50 | 8.9100 | 2 | 2 |
azd3514 | Homo sapiens (human) | IC50 | 1.7789 | 3 | 3 |
azd3514 | Homo sapiens (human) | Ki | 3.1333 | 3 | 3 |
bay 94-8862 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
azd9496 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Exploration and Biological Evaluation of Basic Heteromonocyclic Propanamide Derivatives as SARDs for the Treatment of Enzalutamide-Resistant Prostate Cancer.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 27, Issue:5, 2017
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.Journal of medicinal chemistry, , Mar-12, Volume: 58, Issue:5, 2015
Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.Journal of medicinal chemistry, , Feb-12, Volume: 58, Issue:3, 2015
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.ACS medicinal chemistry letters, , Aug-13, Volume: 6, Issue:8, 2015
Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.European journal of medicinal chemistry, , Jun-24, Volume: 99, 2015
Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists.ACS medicinal chemistry letters, , Oct-10, Volume: 4, Issue:10, 2013
Discovery of non-LBD inhibitor for androgen receptor by structure-guide design.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1, 2013
Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Selectively targeting prostate cancer with antiandrogen equipped histone deacetylase inhibitors.ACS chemical biology, , Nov-15, Volume: 8, Issue:11, 2013
Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 2010
Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.ACS chemical biology, , Oct-16, Volume: 4, Issue:10, 2009
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships.Bioorganic & medicinal chemistry, , Jan-01, Volume: 15, Issue:1, 2007
(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 9, Issue:7, 1999
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.ACS chemical biology, , Oct-16, Volume: 4, Issue:10, 2009
Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 20, Issue:7, 2010
20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring.Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.Journal of medicinal chemistry, , Nov-04, Volume: 47, Issue:23, 2004
Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 13, Issue:16, 2003
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Discovery of diarylhydantoins as new selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.Journal of medicinal chemistry, , Nov-04, Volume: 47, Issue:23, 2004
Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.Journal of medicinal chemistry, , Nov-04, Volume: 47, Issue:23, 2004
Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.ACS medicinal chemistry letters, , Apr-09, Volume: 6, Issue:4, 2015
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Discovery of diarylhydantoins as new selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 8, Issue:23, 1998
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Discovery of Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
Androstene-3,5-dienes as ER-beta selective SERMs.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
Androstenediol analogs as ER-beta-selective SERMs.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.Bioorganic & medicinal chemistry, , 07-01, Volume: 25, Issue:13, 2017
Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.Journal of medicinal chemistry, , Sep-11, Volume: 57, Issue:17, 2014
Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1, 2013
Discovery of diarylhydantoins as new selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140.ACS medicinal chemistry letters, , Feb-10, Volume: 2, Issue:2, 2011
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs).Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.Journal of natural products, , Volume: 72, Issue:11, 2009
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 17, Issue:19, 2007
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 9, Issue:7, 1999
Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 9, Issue:7, 1999
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).Journal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.ACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jul-01, Volume: 16, Issue:13, 2008
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 55, 2022
New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 27, Issue:5, 2017
Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
The systematic structure-activity relationship to predict how flavones bind to human androgen receptor for their antagonistic activity.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer.Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists.ACS medicinal chemistry letters, , Oct-10, Volume: 4, Issue:10, 2013
Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.ACS chemical biology, , Oct-16, Volume: 4, Issue:10, 2009
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.Journal of natural products, , Volume: 72, Issue:11, 2009
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring.Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships.Bioorganic & medicinal chemistry, , Jan-01, Volume: 15, Issue:1, 2007
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.Journal of medicinal chemistry, , Apr-22, Volume: 53, Issue:8, 2010
Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs).Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.ACS chemical biology, , Oct-16, Volume: 4, Issue:10, 2009
A surface on the androgen receptor that allosterically regulates coactivator binding.Proceedings of the National Academy of Sciences of the United States of America, , Oct-09, Volume: 104, Issue:41, 2007
Discovery of Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 17, Issue:7, 2007
Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.Journal of medicinal chemistry, , Mar-12, Volume: 58, Issue:5, 2015
Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Discovery of diarylhydantoins as new selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 55, 2022
Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Discovery of 2-(1-(3-Chloro-4-cyanophenyl)-1Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Discovery of Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer.Bioorganic & medicinal chemistry, , 02-01, Volume: 31, 2021
Exploration and Biological Evaluation of Basic Heteromonocyclic Propanamide Derivatives as SARDs for the Treatment of Enzalutamide-Resistant Prostate Cancer.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Development of 2-(5,6,7-Trifluoro-1Journal of medicinal chemistry, , 10-28, Volume: 64, Issue:20, 2021
Spirocyclic Thiohydantoin Antagonists of F877L and Wild-Type Androgen Receptor for Castration-Resistant Prostate Cancer.ACS medicinal chemistry letters, , Aug-12, Volume: 12, Issue:8, 2021
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).Journal of medicinal chemistry, , 01-28, Volume: 64, Issue:2, 2021
Discovery of a Novel Androgen Receptor Antagonist Manifesting Evidence to Disrupt the Dimerization of the Ligand-Binding Domain via Attenuating the Hydrogen-Bonding Network Between the Two Monomers.Journal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
A critical update on the strategies towards modulators targeting androgen receptors.Bioorganic & medicinal chemistry, , 07-01, Volume: 28, Issue:13, 2020
Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
New drug approvals for 2019: Synthesis and clinical applications.European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
Discovery of pyridine tetrahydroisoquinoline thiohydantoin derivatives with low blood-brain barrier penetration as the androgen receptor antagonists.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
In silico selection and cell-based characterization of selective and bioactive compounds for androgen-dependent prostate cancer cell.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 27, Issue:10, 2017
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 26, Issue:21, 2016
Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3β-Imidazole Carbamate.ACS medicinal chemistry letters, , Jul-14, Volume: 7, Issue:7, 2016
Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.ACS medicinal chemistry letters, , Aug-11, Volume: 7, Issue:8, 2016
Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.European journal of medicinal chemistry, , Jun-24, Volume: 99, 2015
Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Selectively targeting prostate cancer with antiandrogen equipped histone deacetylase inhibitors.ACS chemical biology, , Nov-15, Volume: 8, Issue:11, 2013
Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
New drug approvals for 2019: Synthesis and clinical applications.European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.European journal of medicinal chemistry, , Jun-24, Volume: 99, 2015
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Therapeutic Strategies to Target the Androgen Receptor.Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Monomeric Targeted Protein Degraders.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Enables
This protein enables 23 target(s):
Target | Category | Definition |
transcription cis-regulatory region binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH] |
RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
RNA polymerase II general transcription initiation factor binding | molecular function | Binding to a basal RNA polymerase II transcription factor, any of the factors involved in formation of the preinitiation complex (PIC) by RNA polymerase II and defined as a basal or general transcription factor. [GOC:txnOH, PMID:16858867] |
transcription coactivator binding | molecular function | Binding to a transcription coactivator, a protein involved in positive regulation of transcription via protein-protein interactions with transcription factors and other proteins that positively regulate transcription. Transcription coactivators do not bind DNA directly, but rather mediate protein-protein interactions between activating transcription factors and the basal transcription machinery. [GOC:krc] |
DNA-binding transcription activator activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets transcribed by RNA polymerase II. [GOC:aruk, GOC:txnOH-2018, PMID:20737563, PMID:27145859] |
chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
DNA-binding transcription factor activity | molecular function | A transcription regulator activity that modulates transcription of gene sets via selective and non-covalent binding to a specific double-stranded genomic DNA sequence (sometimes referred to as a motif) within a cis-regulatory region. Regulatory regions include promoters (proximal and distal) and enhancers. Genes are transcriptional units, and include bacterial operons. [GOC:txnOH-2018] |
nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
steroid binding | molecular function | Binding to a steroid, any of a large group of substances that have in common a ring system based on 1,2-cyclopentanoperhydrophenanthrene. [GOC:jl, ISBN:0198506732] |
androgen binding | molecular function | Binding to an androgen, a male sex hormone. [GOC:jl] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
beta-catenin binding | molecular function | Binding to a catenin beta subunit. [GOC:bf] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
ATPase binding | molecular function | Binding to an ATPase, any enzyme that catalyzes the hydrolysis of ATP. [GOC:ai] |
molecular adaptor activity | molecular function | The binding activity of a molecule that brings together two or more molecules through a selective, non-covalent, often stoichiometric interaction, permitting those molecules to function in a coordinated way. [GOC:mtg_MIT_16mar07, GOC:vw] |
RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
POU domain binding | molecular function | Binding to a POU domain of a protein. The POU domain is a bipartite DNA binding domain composed of two subunits separated by a non-conserved region of 15-55 amino acids; it is found in several eukaryotic transcription factors. [GOC:mah, GOC:yaf, InterPro:IPR000327] |
molecular condensate scaffold activity | molecular function | Binding and bringing together two or more macromolecules in contact, permitting those molecules to organize as a molecular condensate. [PMID:28225081] |
estrogen response element binding | molecular function | Binding to an estrogen response element (ERE), a conserved sequence found in the promoters of genes whose expression is regulated in response to estrogen. [GOC:ecd, PMID:15036253, PMID:17975005] |
Located In
This protein is located in 5 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
nuclear speck | cellular component | A discrete extra-nucleolar subnuclear domain, 20-50 in number, in which splicing factors are seen to be localized by immunofluorescence microscopy. [http://www.cellnucleus.com/] |
Active In
This protein is active in 2 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 2 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
Involved In
This protein is involved in 56 target(s):
Target | Category | Definition |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
MAPK cascade | biological process | An intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267] |
in utero embryonic development | biological process | The process whose specific outcome is the progression of the embryo in the uterus over time, from formation of the zygote in the oviduct, to birth. An example of this process is found in Mus musculus. [GOC:go_curators, GOC:mtg_sensu] |
regulation of systemic arterial blood pressure | biological process | The process that modulates the force with which blood travels through the systemic arterial circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:mtg_cardio] |
epithelial cell morphogenesis | biological process | The change in form that occurs when an epithelial cell progresses from its initial formation to its mature state. [GOC:ascb_2009, GOC:dph, GOC:tb] |
transcription by RNA polymerase II | biological process | The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
spermatogenesis | biological process | The developmental process by which male germ line stem cells self renew or give rise to successive cell types resulting in the development of a spermatozoa. [GOC:jid, ISBN:9780878933846, PMID:28073824, PMID:30990821] |
single fertilization | biological process | The union of male and female gametes to form a zygote. [GOC:ems, GOC:mtg_sensu] |
positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
male somatic sex determination | biological process | The determination of sex and sexual phenotypes in a male organism's soma. [GOC:mah] |
intracellular estrogen receptor signaling pathway | biological process | The series of molecular signals initiated by estrogen binding to its nuclear receptor inside the cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling] |
androgen receptor signaling pathway | biological process | The series of molecular signals initiated by androgen binding to its receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah] |
intracellular receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a receptor located within a cell. [GOC:bf, GOC:mah] |
positive regulation of intracellular estrogen receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of the activity of an intracellular estrogen receptor signaling pathway. [GOC:mah] |
Leydig cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized structural and/or functional features of a Leydig cell. A Leydig cell is a testosterone-secreting cell in the interstitial area, between the seminiferous tubules, in the testis. [GOC:ln, PMID:12050120] |
multicellular organism growth | biological process | The increase in size or mass of an entire multicellular organism, as opposed to cell growth. [GOC:bf, GOC:curators, GOC:dph, GOC:tb] |
positive regulation of phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to a molecule. [GOC:jl] |
positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
positive regulation of insulin-like growth factor receptor signaling pathway | biological process | Any process that increases the frequency, rate or extent of insulin-like growth factor receptor signaling. [GOC:bf] |
positive regulation of cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of cell differentiation. [GOC:go_curators] |
negative regulation of integrin biosynthetic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of integrins. [GOC:go_curators] |
positive regulation of integrin biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of integrins. [GOC:go_curators] |
positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
positive regulation of transcription by RNA polymerase III | biological process | Any process that activates or increases the frequency, rate or extent of transcription mediated by RNA polymerase III. [GOC:go_curators, GOC:txnOH] |
insulin-like growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to an insulin-like growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
regulation of developmental growth | biological process | Any process that modulates the frequency, rate or extent of developmental growth. [GOC:go_curators] |
animal organ formation | biological process | The process pertaining to the initial formation of an animal organ from unspecified parts. The process begins with the specific processes that contribute to the appearance of the discrete structure, such as inductive events, and ends when the structural rudiment of the organ is recognizable, such as a condensation of mesenchymal cells into the organ rudiment. Organs are a natural part or structure in an animal or a plant, capable of performing some special action (termed its function), which is essential to the life or well-being of the whole. The heart and lungs are organs of animals, and the petal and leaf are organs of plants. In animals the organs are generally made up of several tissues, one of which usually predominates, and determines the principal function of the organ. [GOC:dph, GOC:jid] |
male genitalia morphogenesis | biological process | The process in which the anatomical structures of male genitalia are generated and organized. [GOC:ems, ISBN:0140512888] |
epithelial cell proliferation | biological process | The multiplication or reproduction of epithelial cells, resulting in the expansion of a cell population. Epithelial cells make up the epithelium, the covering of internal and external surfaces of the body, including the lining of vessels and other small cavities. It consists of cells joined by small amounts of cementing substances. [ISBN:0721662544] |
negative regulation of epithelial cell proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of epithelial cell proliferation. [GOC:ai] |
positive regulation of NF-kappaB transcription factor activity | biological process | Any process that activates or increases the frequency, rate or extent of activity of the transcription factor NF-kappaB. [GOC:dph, GOC:tb, PMID:15087454, PMID:15170030] |
activation of prostate induction by androgen receptor signaling pathway | biological process | The series of molecular signals initiated by androgen binding to its receptor in the urogenital sinus mesenchyme that initiates prostate induction. Prostate induction is the close range interaction of the urogenital sinus mesenchyme and the urogenital sinus epithelium that causes the cells of the urogenital sinus epithelium to change their fates and specify the development of the prostate gland. [GOC:dph, GOC:tb, PMID:18977204] |
morphogenesis of an epithelial fold | biological process | The morphogenetic process in which an epithelial sheet bends along a linear axis. [GOC:dph] |
lateral sprouting involved in mammary gland duct morphogenesis | biological process | The process in which a branch forms along the side of a mammary duct. [GOC:dph, PMID:17120154] |
prostate gland growth | biological process | The increase in size or mass of the prostate gland where the increase in size or mass has the specific outcome of the progression of the gland, from its formation to its mature state. [GOC:dph] |
prostate gland epithelium morphogenesis | biological process | The process in which the anatomical structures of epithelia of the prostate gland are generated and organized. An epithelium consists of closely packed cells arranged in one or more layers, that covers the outer surfaces of the body or lines any internal cavity or tube. [GOC:dph] |
epithelial cell differentiation involved in prostate gland development | biological process | The process in which a relatively unspecialized cell acquires specialized features of an epithelial cell of the prostate gland. [GOC:dph] |
tertiary branching involved in mammary gland duct morphogenesis | biological process | The branching process in which the mammary gland ducts form tertiary branches off of the secondary branches as part of diestrus and pregnancy. [GOC:dph, PMID:18614704] |
mammary gland alveolus development | biological process | The progression of the mammary gland alveolus over time, from its formation to its mature state. The mammary gland alveolus is a sac-like structure that is found in the mature gland. [GOC:dph] |
positive regulation of epithelial cell proliferation involved in prostate gland development | biological process | Any process that increases the rate, frequency or extent of epithelial cell proliferation that contributes to the progression of the prostate gland over time. [GOC:dph] |
cellular response to steroid hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a steroid hormone stimulus. [GOC:mah] |
cellular response to estrogen stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by an estrogen, C18 steroid hormones that can stimulate the development of female sexual characteristics. [GOC:mah] |
cellular response to testosterone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a testosterone stimulus. [GOC:mah] |
seminiferous tubule development | biological process | The reproductive developmental process whose specific outcome is the progression of the seminiferous tubule over time, from its formation to the mature structure. Seminiferous tubules are ducts located in the testicles, and are the specific location of meiosis, and the subsequent creation of gametes, namely spermatozoa. [GOC:BHF, GOC:mah, UBERON:0001343] |
non-membrane-bounded organelle assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form a non-membrane-bounded organelle. [PMID:28225081] |
positive regulation of miRNA transcription | biological process | Any process that activates or increases the frequency, rate or extent of microRNA (miRNA) gene transcription. [GO_REF:0000058, GOC:dph, GOC:kmv, GOC:TermGenie, PMID:24699545] |
regulation of protein localization to plasma membrane | biological process | Any process that modulates the frequency, rate or extent of protein localization to plasma membrane. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:11602640] |
negative regulation of extrinsic apoptotic signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of extrinsic apoptotic signaling pathway. [GOC:mtg_apoptosis] |
male gonad development | biological process | The process whose specific outcome is the progression of the male gonad over time, from its formation to the mature structure. [GOC:jid] |
intracellular steroid hormone receptor signaling pathway | biological process | The series of molecular signals initiated by a steroid binding to an intracellular steroid hormone receptor. [GOC:mah, GOC:signaling] |