Page last updated: 2024-08-07 15:36:46
Glucocorticoid receptor
A glucocorticoid receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P04150]
Synonyms
GR;
Nuclear receptor subfamily 3 group C member 1
Research
Bioassay Publications (120)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 6 (5.00) | 18.2507 |
| 2000's | 57 (47.50) | 29.6817 |
| 2010's | 51 (42.50) | 24.3611 |
| 2020's | 6 (5.00) | 2.80 |
Compounds (95)
Drugs with Potency Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| mifepristone | Homo sapiens (human) | Potency | 0.0008 | 1 | 1 |
| onapristone | Homo sapiens (human) | Potency | 0.0270 | 1 | 1 |
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bicalutamide | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| clotrimazole | Homo sapiens (human) | IC50 | 3.2580 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 1.4810 | 1 | 0 |
| ellipticine | Homo sapiens (human) | IC50 | 90.0000 | 1 | 1 |
| cortisone acetate | Homo sapiens (human) | IC50 | 3.9110 | 1 | 0 |
| cortisone acetate | Homo sapiens (human) | Ki | 1.7780 | 1 | 0 |
| prednisolone | Homo sapiens (human) | IC50 | 0.0508 | 41 | 40 |
| prednisolone | Homo sapiens (human) | Ki | 0.0036 | 15 | 14 |
| estriol | Homo sapiens (human) | IC50 | 39.3450 | 1 | 0 |
| estriol | Homo sapiens (human) | Ki | 17.8840 | 1 | 0 |
| norethindrone acetate | Homo sapiens (human) | IC50 | 0.6460 | 1 | 0 |
| norethindrone acetate | Homo sapiens (human) | Ki | 0.2930 | 1 | 0 |
| spironolactone | Homo sapiens (human) | IC50 | 4.0745 | 5 | 4 |
| spironolactone | Homo sapiens (human) | Ki | 0.4487 | 2 | 1 |
| prednisone | Homo sapiens (human) | IC50 | 1.1460 | 1 | 0 |
| prednisone | Homo sapiens (human) | Ki | 0.5210 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | IC50 | 1.7100 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | Ki | 0.7770 | 1 | 0 |
| methyltestosterone | Homo sapiens (human) | IC50 | 1.8430 | 1 | 0 |
| methyltestosterone | Homo sapiens (human) | Ki | 0.8380 | 1 | 0 |
| fluocinolone acetonide | Homo sapiens (human) | IC50 | 0.0031 | 1 | 0 |
| fluocinolone acetonide | Homo sapiens (human) | Ki | 0.0014 | 1 | 0 |
| norethindrone | Homo sapiens (human) | IC50 | 0.4330 | 1 | 0 |
| norethindrone | Homo sapiens (human) | Ki | 0.1970 | 1 | 0 |
| 17-alpha-hydroxyprogesterone | Homo sapiens (human) | IC50 | 0.0510 | 1 | 0 |
| 17-alpha-hydroxyprogesterone | Homo sapiens (human) | Ki | 0.0230 | 1 | 0 |
| medroxyprogesterone acetate | Homo sapiens (human) | IC50 | 0.0130 | 3 | 2 |
| medroxyprogesterone acetate | Homo sapiens (human) | Ki | 0.0124 | 6 | 5 |
| triamcinolone acetonide | Homo sapiens (human) | IC50 | 0.0044 | 1 | 0 |
| triamcinolone acetonide | Homo sapiens (human) | Ki | 0.0020 | 1 | 0 |
| methylprednisolone | Homo sapiens (human) | IC50 | 0.0110 | 1 | 0 |
| methylprednisolone | Homo sapiens (human) | Ki | 0.0050 | 1 | 0 |
| chlormadinone acetate | Homo sapiens (human) | IC50 | 0.0377 | 1 | 0 |
| chlormadinone acetate | Homo sapiens (human) | Ki | 0.0172 | 1 | 0 |
| fluocinonide | Homo sapiens (human) | IC50 | 0.0053 | 1 | 0 |
| fluocinonide | Homo sapiens (human) | Ki | 0.0024 | 1 | 0 |
| betamethasone | Homo sapiens (human) | IC50 | 0.0077 | 1 | 0 |
| betamethasone | Homo sapiens (human) | Ki | 0.0035 | 1 | 0 |
| fluorometholone | Homo sapiens (human) | IC50 | 0.0035 | 1 | 0 |
| fluorometholone | Homo sapiens (human) | Ki | 0.0016 | 1 | 0 |
| cyproterone acetate | Homo sapiens (human) | IC50 | 0.2250 | 1 | 0 |
| cyproterone acetate | Homo sapiens (human) | Ki | 0.1020 | 1 | 0 |
| podophyllotoxin | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
| medroxyprogesterone | Homo sapiens (human) | IC50 | 0.0190 | 1 | 0 |
| medroxyprogesterone | Homo sapiens (human) | Ki | 0.0086 | 1 | 0 |
| dihydrotestosterone | Homo sapiens (human) | IC50 | 0.5400 | 1 | 1 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | IC50 | 15.4030 | 1 | 0 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | Ki | 7.0010 | 1 | 0 |
| megestrol acetate | Homo sapiens (human) | IC50 | 0.0190 | 1 | 0 |
| megestrol acetate | Homo sapiens (human) | Ki | 0.0088 | 1 | 0 |
| pregnenolone carbonitrile | Homo sapiens (human) | IC50 | 13.9570 | 1 | 0 |
| pregnenolone carbonitrile | Homo sapiens (human) | Ki | 6.3440 | 1 | 0 |
| flurandrenolone | Homo sapiens (human) | IC50 | 0.0044 | 1 | 0 |
| flurandrenolone | Homo sapiens (human) | Ki | 0.0020 | 1 | 0 |
| beclomethasone | Homo sapiens (human) | IC50 | 0.0082 | 1 | 0 |
| beclomethasone | Homo sapiens (human) | Ki | 0.0037 | 1 | 0 |
| danazol | Homo sapiens (human) | IC50 | 4.3140 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 1.9610 | 1 | 0 |
| triamcinolone | Homo sapiens (human) | IC50 | 0.0580 | 1 | 0 |
| triamcinolone | Homo sapiens (human) | Ki | 0.0260 | 1 | 0 |
| clobetasol propionate | Homo sapiens (human) | IC50 | 0.0015 | 1 | 0 |
| clobetasol propionate | Homo sapiens (human) | Ki | 0.0007 | 1 | 0 |
| mifepristone | Homo sapiens (human) | IC50 | 0.2587 | 51 | 50 |
| mifepristone | Homo sapiens (human) | Ki | 0.0149 | 21 | 20 |
| diflorasone diacetate | Homo sapiens (human) | IC50 | 0.0064 | 1 | 0 |
| diflorasone diacetate | Homo sapiens (human) | Ki | 0.0029 | 1 | 0 |
| 9-methoxyellipticine | Homo sapiens (human) | IC50 | 90.0000 | 1 | 1 |
| flunisolide | Homo sapiens (human) | IC50 | 0.0053 | 1 | 0 |
| flunisolide | Homo sapiens (human) | Ki | 0.0024 | 1 | 0 |
| nectandrin-b | Homo sapiens (human) | IC50 | 27.0000 | 1 | 1 |
| estradiol 3-benzoate | Homo sapiens (human) | IC50 | 5.0740 | 1 | 0 |
| estradiol 3-benzoate | Homo sapiens (human) | Ki | 2.3060 | 1 | 0 |
| cortisone | Homo sapiens (human) | IC50 | 2.3780 | 1 | 0 |
| cortisone | Homo sapiens (human) | Ki | 1.0810 | 1 | 0 |
| fludrocortisone acetate | Homo sapiens (human) | IC50 | 0.0200 | 1 | 0 |
| fludrocortisone acetate | Homo sapiens (human) | Ki | 0.0093 | 1 | 0 |
| metribolone | Homo sapiens (human) | Ki | 0.0096 | 1 | 1 |
| mometasone furoate | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| eplerenone | Homo sapiens (human) | IC50 | 22.6850 | 4 | 4 |
| eplerenone | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| halcinonide | Homo sapiens (human) | IC50 | 0.0016 | 1 | 0 |
| halcinonide | Homo sapiens (human) | Ki | 0.0007 | 1 | 0 |
| fluticasone propionate | Homo sapiens (human) | IC50 | 0.0003 | 5 | 5 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 10.6000 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 4.8180 | 1 | 0 |
| pulmicort | Homo sapiens (human) | IC50 | 0.0026 | 4 | 3 |
| pulmicort | Homo sapiens (human) | Ki | 0.0017 | 2 | 1 |
| baicalein | Homo sapiens (human) | IC50 | 19.0000 | 1 | 1 |
| ethisterone | Homo sapiens (human) | IC50 | 0.2090 | 1 | 0 |
| ethisterone | Homo sapiens (human) | Ki | 0.0950 | 1 | 0 |
| desoximetasone | Homo sapiens (human) | IC50 | 0.0026 | 1 | 0 |
| desoximetasone | Homo sapiens (human) | Ki | 0.0012 | 1 | 0 |
| onapristone | Homo sapiens (human) | IC50 | 0.0270 | 3 | 3 |
| onapristone | Homo sapiens (human) | Ki | 0.0418 | 1 | 1 |
| pregna-4,17-diene-3,16-dione | Homo sapiens (human) | IC50 | 50.8700 | 2 | 2 |
| pregna-4,17-diene-3,16-dione | Homo sapiens (human) | Ki | 0.2240 | 1 | 1 |
| pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | IC50 | 6.0600 | 1 | 1 |
| pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | Ki | 0.2520 | 1 | 1 |
| asoprisnil | Homo sapiens (human) | IC50 | 0.1025 | 2 | 2 |
| zk 216348 | Homo sapiens (human) | IC50 | 0.0152 | 4 | 4 |
| fluticasone furoate | Homo sapiens (human) | IC50 | 0.0004 | 2 | 2 |
| fluticasone furoate | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| way-362450 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| lgd 2226 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| mdv 3100 | Homo sapiens (human) | IC50 | 19.5000 | 2 | 2 |
| mdv 3100 | Homo sapiens (human) | Ki | 14.0000 | 1 | 1 |
| way 252623 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| endiandrin a | Homo sapiens (human) | IC50 | 0.9000 | 1 | 1 |
| cort 108297 | Homo sapiens (human) | Ki | 0.0048 | 3 | 3 |
| nitd 609 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| bi 653048 bs h3po4 | Homo sapiens (human) | IC50 | 0.2893 | 8 | 5 |
| pf-03882845 | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| bay 94-8862 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| azd9496 | Homo sapiens (human) | IC50 | 9.2000 | 1 | 1 |
| amg 221 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Discovery of a subnanomolar and selective spirocyclic agonist of the glucocorticoid receptor.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
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
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
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
Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 21, Issue:22, 2011
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-Journal of medicinal chemistry, , Oct-27, Volume: 54, Issue:20, 2011
Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
5-Functionalized indazoles as glucocorticoid receptor agonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators.Journal of medicinal chemistry, , Apr-22, Volume: 53, Issue:8, 2010
Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 18, Issue:12, 2008
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.Proceedings of the National Academy of Sciences of the United States of America, , Dec-04, Volume: 104, Issue:49, 2007
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 17, Issue:12, 2007
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 15, Issue:8, 2005
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
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
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.Journal of medicinal chemistry, , Dec-06, Volume: 44, Issue:25, 2001
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
[no title available],
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 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
[no title available],
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
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-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-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-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
[no title available],
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
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
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
Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
Profiling withanolide A for therapeutic targets in neurodegenerative diseases.Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
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
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.ACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
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
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid ReceptorJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
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
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
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators.Journal of medicinal chemistry, , Apr-22, Volume: 53, Issue:8, 2010
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.Journal of natural products, , Volume: 72, Issue:11, 2009
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 19, Issue:14, 2009
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
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
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.Journal of medicinal chemistry, , Sep-20, Volume: 50, Issue:19, 2007
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 17, Issue:1, 2007
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 17, Issue:21, 2007
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 16, Issue:23, 2006
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 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
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 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
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
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
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
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
[no title available],
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
[no title available]Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
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
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 21, Issue:19, 2011
Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 21, Issue:19, 2011
[no title available],
[no title available]Journal of natural products, , 01-28, Volume: 85, Issue:1, 2022
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 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
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
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
Discovery of quinolines as selective glucocorticoid receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 21, Issue:19, 2011
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
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
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
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 25, Issue:24, 2015
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
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
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.ACS medicinal chemistry letters, , Dec-11, Volume: 5, Issue:12, 2014
[no title available],
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
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 20 target(s):
| Target | Category | Definition |
|---|
| RNA polymerase II transcription regulatory region sequence-specific DNA binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls the transcription of a gene or cistron by RNA polymerase II. [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] |
| core promoter sequence-specific DNA binding | molecular function | Binding to a sequence of DNA that is part of a core promoter region. The core promoter is composed of the transcription start site and binding sites for the RNA polymerase and the basal transcription machinery. The transcribed region might be described as a gene, cistron, or operon. [GOC:pg, GOC:txnOH] |
| DNA-binding transcription repressor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that represses or decreases the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
| 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] |
| 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] |
| RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
| 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] |
| nuclear glucocorticoid receptor activity | molecular function | Combining with a glucocorticoid and transmitting the signal within the cell trigger a change in cell activity or function. [GOC:signaling, PMID:17689856, PMID:20920967] |
| 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] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
| TBP-class protein binding | molecular function | Binding to a member of the class of TATA-binding proteins (TBP), including any of the TBP-related factors (TRFs). [GOC:jl, GOC:txnOH, http://www.mblab.gla.ac.uk/, PMID:16858867] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| Hsp90 protein binding | molecular function | Binding to Hsp90 proteins, any of a group of heat shock proteins around 90kDa in size. [GOC:ai] |
| steroid hormone binding | molecular function | Binding to a steroid hormone. [GOC:ln] |
| sequence-specific double-stranded DNA binding | molecular function | Binding to double-stranded DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA, e.g. promotor binding or rDNA binding. [GOC:dos, GOC:sl] |
| 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 10 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] |
| mitochondrial matrix | cellular component | The gel-like material, with considerable fine structure, that lies in the matrix space, or lumen, of a mitochondrion. It contains the enzymes of the tricarboxylic acid cycle and, in some organisms, the enzymes concerned with fatty acid oxidation. [GOC:as, ISBN:0198506732] |
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
| spindle | cellular component | The array of microtubules and associated molecules that forms between opposite poles of a eukaryotic cell during mitosis or meiosis and serves to move the duplicated chromosomes apart. [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] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| 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/] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
Active In
This protein is active in 1 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] |
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 31 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] |
| regulation of gluconeogenesis | biological process | Any process that modulates the frequency, rate or extent of gluconeogenesis, the formation of glucose from noncarbohydrate precursors, such as pyruvate, amino acids and glycerol. [GOC:go_curators] |
| chromatin organization | biological process | The assembly or remodeling of chromatin composed of DNA complexed with histones, other associated proteins, and sometimes RNA. [PMID:20404130] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
| chromosome segregation | biological process | The process in which genetic material, in the form of chromosomes, is organized into specific structures and then physically separated and apportioned to two or more sets. In eukaryotes, chromosome segregation begins with the condensation of chromosomes, includes chromosome separation, and ends when chromosomes have completed movement to the spindle poles. [GOC:jl, GOC:mah, GOC:mtg_cell_cycle, GOC:vw] |
| 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] |
| glucocorticoid metabolic process | biological process | The chemical reactions and pathways involving glucocorticoids, hormonal C21 corticosteroids synthesized from cholesterol. Glucocorticoids act primarily on carbohydrate and protein metabolism, and have anti-inflammatory effects. [ISBN:0198506732] |
| gene expression | biological process | The process in which a gene's sequence is converted into a mature gene product (protein or RNA). This includes the production of an RNA transcript and its processing, as well as translation and maturation for protein-coding genes. [GOC:txnOH-2018, PMID:25934543, PMID:31580950] |
| microglia differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a microglial cell. Microglia are glial cells that act as the immune cells of the central nervous system. They form part of the supporting structure of this system. [GOC:ef] |
| adrenal gland development | biological process | The process whose specific outcome is the progression of the adrenal gland over time, from its formation to the mature structure. This gland can either be a discrete structure located bilaterally above each kidney, or a cluster of cells in the head kidney that perform the functions of the adrenal gland. In either case, this organ consists of two cells types, aminergic chromaffin cells and steroidogenic cortical cells. [GOC:dgh] |
| regulation of glucocorticoid biosynthetic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of glucocorticoids. [GOC:mah] |
| synaptic transmission, glutamatergic | biological process | The vesicular release of glutamate from a presynapse, across a chemical synapse, the subsequent activation of glutamate receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos] |
| maternal behavior | biological process | Female behaviors associated with the care and rearing of offspring. [GOC:curators] |
| intracellular glucocorticoid receptor signaling pathway | biological process | The series of molecular signals initiated by glucocorticoid binding to its nuclear receptor inside the cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah] |
| glucocorticoid mediated signaling pathway | biological process | The series of molecular signals mediated by the detection of a glucocorticoid hormone. [PMID:15240347] |
| positive regulation of neuron apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death of neurons by apoptotic process. [GOC:go_curators, GOC:mtg_apoptosis] |
| negative regulation of DNA-templated transcription | biological process | Any process that stops, prevents, or reduces 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] |
| astrocyte differentiation | biological process | The process in which a relatively unspecialized cell acquires the specialized features of an astrocyte. An astrocyte is the most abundant type of glial cell. Astrocytes provide support for neurons and regulate the environment in which they function. [GOC:vp, PMID:15139015] |
| cell division | biological process | The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr] |
| mammary gland duct morphogenesis | biological process | The process in which anatomical structures of the mammary ducts are generated and organized. Mammary ducts are epithelial tubes that transport milk. [GOC:dph, PMID:17120154] |
| motor behavior | biological process | The specific neuromuscular movement of a single organism in response to external or internal stimuli. [GOC:bf, GOC:PARL, PMID:25318560] |
| 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 glucocorticoid 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 glucocorticoid stimulus. Glucocorticoids are hormonal C21 corticosteroids synthesized from cholesterol with the ability to bind with the cortisol receptor and trigger similar effects. Glucocorticoids act primarily on carbohydrate and protein metabolism, and have anti-inflammatory effects. [GOC:mah] |
| cellular response to dexamethasone 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 dexamethasone stimulus. [GOC:mah, GOC:yaf] |
| cellular response to transforming growth factor beta 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 transforming growth factor beta stimulus. [GOC:ecd, PMID:15451575] |
| neuroinflammatory response | biological process | The immediate defensive reaction by neural vertebrate tissue to infection or injury caused by chemical or physical agents. [GOC:aruk, GOC:bc, PMID:10981966, PMID:11099416, PMID:18164423] |
| 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] |
| 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] |
| regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |