NR3C1
ENSG00000113580
Target class
Nuclear receptor
Chromosome
5
Approved drugs
64
Clinical candidates (approved and in development)
75
- Approved drugs
- 64
- Clinical candidates (approved and in development)
- 75
- Chemical probe available
- Yes
- Other names
- GR
- Target name
- NR3C1
- Gene name
- Nuclear receptor subfamily 3 group C member 1
- Gene symbol
- NR3C1
- Previous gene symbols
- GRL
- Protein name
- Glucocorticoid receptor (GR) (Nuclear receptor subfamily 3 group C member 1)
- Gene biotype
- Protein coding
- Gene family
- Nuclear receptor subfamily 3 group C
- Target class
- Nuclear receptor
- Target type
- Human gene
- Tissues expressed in
- 54
- Protein localisation evidence grade
- Supported
- Highest tissue expression
- 55.25
- Tissue specificity (Gini)
- 0.318
- Tissue specificity (tau)
- 0.711
- KEGG gene identifiers
- hsa:2908
- Protein interaction confidence
- 0.847921
- Protein interaction partners
- 89
- R-HSA-3371497
- R-HSA-4090294
- R-HSA-8849473
- R-HSA-8939902
- R-HSA-9615017
- R-HSA-9679191
- R-HSA-9768777
- End position
- 143435512
- Start position
- 143277931
- Chromosome
- 5
- Strand
- Reverse
- [Isoform Alpha]: Cytoplasm . Nucleus . Mitochondrion . Cytoplasm, cytoskeleton, spindle . Cytoplasm, cytoskeleton, microtubule organizing center, centrosome . Chromosome . Nucleus, nucleoplasm . Note=After ligand activation, translocates from the cytoplasm to the nucleus (PubMed:30698747). The hormone-occupied receptor undergoes rapid exchange between chromatin and the nucleoplasmic compartment (By similarity). In the presence of NR1D1 shows a time-dependent subcellular localization, localizing to the cytoplasm at ZT8 and to the nucleus at ZT20 (By similarity). Lacks this diurnal pattern of localization in the absence of NR1D1, localizing to both nucleus and the cytoplasm at ZT8 and ZT20 (By similarity). Upon dexamethasone binding associates with the glucocorticoid response elements of target genes (By similarity). .
- SUBCELLULAR LOCATION: [Isoform Beta]: Nucleus . Cytoplasm . Note=Expressed predominantly in the nucleus with some expression also detected in the cytoplasm. .
- SUBCELLULAR LOCATION: [Isoform Alpha-B]: Nucleus . Cytoplasm . Note=After ligand activation, translocates from the cytoplasm to the nucleus. .
- Cytosol
- Mitochondria
- Nucleoplasm
- PubMed 15769988
- PubMed 17635946
- PubMed 18838540
- PubMed 27120390
- PubMed 30698747
- PubMed 8621628
- PubMed 21664385
- PubMed 25847991
- PubMed 19248771
- PubMed 26711253
- PubMed 15866175
- Tissue specificity (tau)
- 0.710981
- Expression inequality (Gini)
- 0.317627
Expression in transcripts per million
- Cells - EBV-transformed lymphocytes
- 55.25
- Nerve - Tibial
- 34.46
- Adipose - Subcutaneous
- 34.13
- Cells - Cultured fibroblasts
- 33.59
- Artery - Tibial
- 32.69
Expression in transcripts per million
- Cells - EBV-transformed lymphocytes55.25
- Nerve - Tibial34.46
- Adipose - Subcutaneous34.13
- Cells - Cultured fibroblasts33.59
- Artery - Tibial32.69
- Brain - Cerebellar Hemisphere28.96
- Adipose - Visceral (Omentum)26.4
- Breast - Mammary Tissue26.18
- Lung24.74
- Brain - Cerebellum24.3
- Artery - Coronary23.97
- Esophagus - Muscularis22.92
- Artery - Aorta22.51
- Vagina21.85
- Esophagus - Gastroesophageal Junction21.7
- Thyroid21.37
- Cervix - Ectocervix21.14
- Skin - Sun Exposed (Lower leg)20.77
- Uterus20.66
- Muscle - Skeletal20.17
- Pituitary19.78
- Cervix - Endocervix19.51
- Fallopian Tube18.52
- Bladder18.52
- Skin - Not Sun Exposed (Suprapubic)18.27
And 29 more, listed on the interactive page.
- GO:0000122
- GO:0006355
- GO:0007165
- GO:0045892
- GO:0045944
- GO:0071383
- GO:0071385
- GO:0071549
- GO:0071560
- GO:1902895
- GO:0005634
- GO:0005654
- GO:0005737
- GO:0005739
- GO:0005759
- GO:0005829
- GO:0016607
- GO:0032991
- GO:0000977
- GO:0000978
- GO:0001046
- GO:0001227
- GO:0001228
- GO:0003700
- GO:0004879
- GO:0004883
- GO:0005496
- GO:0005515
- GO:0017025
- GO:0019901
- GO:0051879
- GO:1990239
- GO:1990837
decreased memory
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased memory
- nervous system
- immune
- endocrine
PubMed 28216264decreased blood potassium
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased blood potassium
- nervous system
- immune
- endocrine
PubMed 28216264Increase, hypertension
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourcedecreased wound repair
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased wound repair
- nervous system
- immune
- endocrine
PubMed 28216264increased blood glucose
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased blood glucose
- nervous system
- immune
- endocrine
PubMed 28216264Decreased sperm quantity / quality in the adult, Decreased fertility
Studies
- cell-based
Evidence sourceincreased urinary sodium excretion
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased urinary sodium excretion
- nervous system
- immune
- endocrine
PubMed 28216264increased/decreased pain
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased/decreased pain
- nervous system
- immune
- endocrine
PubMed 28216264impaired, Fertility
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourcelipid redistribution
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: lipid redistribution
- nervous system
- immune
- endocrine
PubMed 28216264decreased pain
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased pain
- nervous system
- immune
- endocrine
PubMed 28216264Decrease, Population growth rate
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceDecreased sperm quantity or quality in the adult, Decreased fertility
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Evidence sourceincreased inflammation
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased inflammation
- nervous system
- immune
- endocrine
PubMed 28216264increased memory
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased memory
- nervous system
- immune
- endocrine
PubMed 28216264Increased, Liver Steatosis
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceIncreased, agitation
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourcedecreased muscle mass
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased muscle mass
- nervous system
- immune
- endocrine
PubMed 28216264Increased, depression
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceinsulin resistance
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: insulin resistance
- nervous system
- immune
- endocrine
PubMed 28216264decreased inflammation
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased inflammation
- nervous system
- immune
- endocrine
PubMed 28216264increased blood pressure
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased blood pressure
- nervous system
- immune
- endocrine
PubMed 28216264endometrial thickening
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: endometrial thickening
- nervous system
- immune
- endocrine
PubMed 28216264Increased, seizure
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourcefatigue
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: fatigue
- nervous system
- immune
- endocrine
PubMed 28216264
And 2 more, listed on the interactive page.
regulation of transcription factor activity
- cell-based: TOX21_GR_BLA_Antagonist_ratio is an assay readout measuring reporter gene via receptor activity and designed using inducible reporter (beta lactamase induction) detected with GAL4 b-lactamase reporter gene. The signal is derived from the ratio of cleaved (ch2) to uncleaved (ch1) reporter gene substrate used as the measure of target activity.
- cell-based: ATG_GRE_CIS, is one of 52 assay component(s) measured or calculated from the ATG_CIS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- cell-based: TOX21_GR_BLA_Agonist_ratio is an assay readout measuring reporter gene via receptor activity and designed using inducible reporter (beta lactamase induction) detected with GAL4 b-lactamase reporter gene. The signal is derived from the ratio of cleaved (ch2) to uncleaved (ch1) substrate used as the measure of target activity.
- cell-based: ATG_GRE_CIS, is one of 52 assay component(s) measured or calculated from the ATG_CIS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- cell-based: ATG_GR_TRANS, is one of 30 assay component(s) measured or calculated from the ATG_TRANS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- cell-based: ATG_GR_TRANS, is one of 30 assay component(s) measured or calculated from the ATG_TRANS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- HeLa, cell line
- HepG2, cell line
Evidence sourceimmunosuppression
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: immunosuppression
- immune
- endocrine
PubMed 23197038insulin resistance
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: insulin resistance
- immune
- endocrine
PubMed 23197038muscle wasting
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: muscle wasting
- immune
- endocrine
PubMed 23197038receptor binding
Studies
- biochemical: NVS_NR_hGR, is one of one assay component(s) measured or calculated from the NVS_NR_hGR assay. It is designed to make measurements of radioligand binding, a form of binding reporter, as detected with scintillation counting signals by Filter-based radiodetection technology.
Biological samples
- cell-free
Evidence sourceincreased body weight
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: increased body weight
- immune
- endocrine
PubMed 23197038regulation of steroid biosynthetic process
- cell-based: CEETOX_H295R_DOC, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_CORTISOL, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_CORTIC, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_CORTIC, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_11DCORT, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_CORTISOL, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_DOC, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_11DCORT, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
Biological samples
- H295R, cell line
Evidence sourcecardiac arrhythmia
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: cardiac arrhythmia
- immune
- endocrine
PubMed 23197038increased blood pressure
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: increased blood pressure
- immune
- endocrine
PubMed 23197038regulation of steroid hormone biosynthetic process
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
Biological samples
- H295R, cell line
Evidence sourceglaucoma
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: glaucoma
- immune
- endocrine
PubMed 23197038osteoporosis
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: osteoporosis
- immune
- endocrine
PubMed 23197038decreased plasma potassium
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: decreased plasma potassium
- immune
- endocrine
PubMed 23197038hyperglycaemia
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: hyperglycaemia
- immune
- endocrine
PubMed 23197038hypoglycaemia
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: hypoglycaemia
- immune
- endocrine
PubMed 23197038
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Drugs (82)
- ABBV-3373 Glucocorticoid receptor modulator
- Alclometasone dipropionate Glucocorticoid receptor agonist
- Amcinonide Glucocorticoid receptor agonist
- AZD-5423 Glucocorticoid receptor modulator
- Beclomethasone dipropionate Glucocorticoid receptor agonist
- Betamethasone Glucocorticoid receptor agonist
- Betamethasone acetate Glucocorticoid receptor agonist
- Betamethasone benzoate Glucocorticoid receptor agonist
- Betamethasone dipropionate Glucocorticoid receptor agonist
- Betamethasone phosphoric acid Glucocorticoid receptor agonist
- Betamethasone sodium phosphate Glucocorticoid receptor agonist
- Betamethasone valerate Glucocorticoid receptor agonist
- Budesonide Glucocorticoid receptor agonist
- Ciclesonide Glucocorticoid receptor agonist
- Clobetasol propionate Glucocorticoid receptor agonist
- Clocortolone pivalate Glucocorticoid receptor agonist
- CORT 108297 Glucocorticoid receptor antagonist
- Cortisone acetate Glucocorticoid receptor agonist
- Cortivazol Glucocorticoid receptor agonist
- Cyproterone acetate Glucocorticoid receptor antagonist