Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T40016
(Former ID: TTDS00283)
|
|||||
Target Name |
Glucocorticoid receptor (NR3C1)
|
|||||
Synonyms |
Nuclear receptor subfamily 3 group C member 1; GRL; GR
Click to Show/Hide
|
|||||
Gene Name |
NR3C1
|
|||||
Target Type |
Successful target
|
[1] | ||||
Disease | [+] 11 Target-related Diseases | + | ||||
1 | Adaptive immunity immunodeficiency [ICD-11: 4A01] | |||||
2 | Allergic/hypersensitivity disorder [ICD-11: 4A80-4A8Z] | |||||
3 | Asthma [ICD-11: CA23] | |||||
4 | Chronic obstructive pulmonary disease [ICD-11: CA22] | |||||
5 | Cushing syndrome [ICD-11: 5A70] | |||||
6 | Muscular dystrophy [ICD-11: 8C70] | |||||
7 | Oesophagitis [ICD-11: DA24] | |||||
8 | Postoperative inflammation [ICD-11: 1A00-CA43] | |||||
9 | Rheumatoid arthritis [ICD-11: FA20] | |||||
10 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
11 | Vasomotor/allergic rhinitis [ICD-11: CA08] | |||||
Function |
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling. Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay. Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity).
Click to Show/Hide
|
|||||
BioChemical Class |
Nuclear hormone receptor
|
|||||
UniProt ID | ||||||
Sequence |
MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A00948 ; BADD_A02053 | |||||
HIT2.0 ID | T47G3X |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Approved Drug(s) | [+] 21 Approved Drugs | + | ||||
1 | Betamethasone | Drug Info | Approved | Inflammation | [2], [3] | |
2 | Betamethasone Benzoate | Drug Info | Approved | Inflammation | [4] | |
3 | Betamethasone Valerate | Drug Info | Approved | Dermatological disease | [4] | |
4 | Budesonide | Drug Info | Approved | Asthma | [5], [6] | |
5 | Deflazacort | Drug Info | Approved | Duchenne dystrophy | [4], [7], [8], [9] | |
6 | Dexamethasone | Drug Info | Approved | Rheumatoid arthritis | [10], [11] | |
7 | Dexamethasone sodium phosphate | Drug Info | Approved | Ataxia-telangiectasia | [12] | |
8 | Flunisolide | Drug Info | Approved | Allergic rhinitis | [13], [14] | |
9 | Fluocinolone Acetonide | Drug Info | Approved | Inflammation | [15], [16] | |
10 | Fluorometholone | Drug Info | Approved | Chronic obstructive pulmonary disease | [4] | |
11 | Fluticasone | Drug Info | Approved | Allergic rhinitis | [4] | |
12 | GW685698X | Drug Info | Approved | Asthma | [17], [18] | |
13 | Hydrocortamate | Drug Info | Approved | Inflammation | [19] | |
14 | Hydrocortisone | Drug Info | Approved | Inflammation | [20], [6] | |
15 | Meprednisone | Drug Info | Approved | Chronic obstructive pulmonary disease | [4] | |
16 | Methylprednisolone | Drug Info | Approved | Solid tumour/cancer | [4] | |
17 | Mifepristone | Drug Info | Approved | Cushing disease | [21], [22], [4] | |
18 | Mometasone | Drug Info | Approved | Skin allergy | [6] | |
19 | Prednisolone | Drug Info | Approved | Solid tumour/cancer | [4] | |
20 | Prednisone | Drug Info | Approved | Inflammation | [23], [11] | |
21 | Triamcinolone | Drug Info | Approved | Allergic rhinitis | [4] | |
Clinical Trial Drug(s) | [+] 18 Clinical Trial Drugs | + | ||||
1 | CORT-125134 | Drug Info | Phase 3 | Cushing disease | [24] | |
2 | FST-201 | Drug Info | Phase 3 | Otitis externa | [25] | |
3 | Mapracorat | Drug Info | Phase 3 | Ocular disease | [26], [27] | |
4 | TLC599 | Drug Info | Phase 3 | Knee osteoarthritis | [28] | |
5 | BAY 86-5044 | Drug Info | Phase 2 | Breast cancer | [29] | |
6 | CORT113176 | Drug Info | Phase 2 | Amyotrophic lateral sclerosis | [30] | |
7 | DE-110 | Drug Info | Phase 2 | Xerophthalmia | [31] | |
8 | ETIPREDNOL DICLOACETATE | Drug Info | Phase 2 | Rhinitis | [32] | |
9 | GW-870086-X | Drug Info | Phase 2 | Asthma | [33], [34] | |
10 | GW-870086-X | Drug Info | Phase 2 | Atopic dermatitis | [33], [34] | |
11 | IONIS-GCCRRX | Drug Info | Phase 2 | Type-2 diabetes | [35] | |
12 | LAS-41002 | Drug Info | Phase 2 | Eczema | [36] | |
13 | ORG 34517/34850 | Drug Info | Phase 2 | Solid tumour/cancer | [37], [38] | |
14 | ORG-34517 | Drug Info | Phase 2 | Depression | [39] | |
15 | TPI-1020 | Drug Info | Phase 2 | Chronic obstructive pulmonary disease | [40] | |
16 | IBI-20089 | Drug Info | Phase 1 | Diabetic macular edema | [35] | |
17 | NCX-1015 | Drug Info | Phase 1 | Rheumatoid arthritis | [41] | |
18 | PT-150 | Drug Info | Phase 1 | Alcohol use disorder | [42] | |
Discontinued Drug(s) | [+] 6 Discontinued Drugs | + | ||||
1 | AZD-5423 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [43] | |
2 | GSK870086 | Drug Info | Discontinued in Phase 2 | Asthma | [44] | |
3 | NM-135 | Drug Info | Discontinued in Phase 2 | Dermatitis | [45] | |
4 | WC-3027 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [46] | |
5 | PF-251802 | Drug Info | Discontinued in Phase 1 | Rheumatoid arthritis | [47] | |
6 | Org-34116 | Drug Info | Terminated | Anxiety disorder | [48] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Agonist | [+] 17 Agonist drugs | + | ||||
1 | Betamethasone | Drug Info | [49] | |||
2 | Dexamethasone | Drug Info | [52], [53] | |||
3 | Dexamethasone sodium phosphate | Drug Info | [54] | |||
4 | Flunisolide | Drug Info | [55] | |||
5 | GW685698X | Drug Info | [58] | |||
6 | Mometasone | Drug Info | [60] | |||
7 | Prednisone | Drug Info | [62] | |||
8 | FST-201 | Drug Info | [65] | |||
9 | Mapracorat | Drug Info | [66] | |||
10 | TLC599 | Drug Info | [67] | |||
11 | DE-110 | Drug Info | [70] | |||
12 | GW-870086-X | Drug Info | [72] | |||
13 | GW-870086-X | Drug Info | [72] | |||
14 | IBI-20089 | Drug Info | [35] | |||
15 | AZD-5423 | Drug Info | [78] | |||
16 | WC-3027 | Drug Info | [81] | |||
17 | PF-251802 | Drug Info | [82] | |||
Modulator | [+] 17 Modulator drugs | + | ||||
1 | Betamethasone Benzoate | Drug Info | [50] | |||
2 | Betamethasone Valerate | Drug Info | [50] | |||
3 | Deflazacort | Drug Info | [50] | |||
4 | Fluocinolone Acetonide | Drug Info | [50] | |||
5 | Hydrocortamate | Drug Info | [50] | |||
6 | Hydrocortisone | Drug Info | [50] | |||
7 | Meprednisone | Drug Info | [50] | |||
8 | Methylprednisolone | Drug Info | [50] | |||
9 | Mifepristone | Drug Info | [59] | |||
10 | Prednisolone | Drug Info | [61] | |||
11 | Triamcinolone | Drug Info | [50] | |||
12 | CORT113176 | Drug Info | [69] | |||
13 | ETIPREDNOL DICLOACETATE | Drug Info | [71] | |||
14 | LAS-41002 | Drug Info | [73] | |||
15 | NCX-1015 | Drug Info | [41] | |||
16 | GSK870086 | Drug Info | [79] | |||
17 | NM-135 | Drug Info | [80] | |||
Antagonist | [+] 9 Antagonist drugs | + | ||||
1 | Budesonide | Drug Info | [1], [51] | |||
2 | Fluticasone | Drug Info | [51], [57] | |||
3 | CORT-125134 | Drug Info | [63], [64] | |||
4 | IONIS-GCCRRX | Drug Info | [35] | |||
5 | ORG 34517/34850 | Drug Info | [74] | |||
6 | ORG-34517 | Drug Info | [75] | |||
7 | TPI-1020 | Drug Info | [76] | |||
8 | PT-150 | Drug Info | [77] | |||
9 | Org-34116 | Drug Info | [83] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | Fluorometholone | Drug Info | [56] | |||
Inhibitor | [+] 3 Inhibitor drugs | + | ||||
1 | BAY 86-5044 | Drug Info | [68] | |||
2 | B-Octylglucoside | Drug Info | [84] | |||
3 | Hexane-1,6-Diol | Drug Info | [84] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
Drug Binding Sites of Target | Top | |||||
---|---|---|---|---|---|---|
Ligand Name: Symbicort | Ligand Info | |||||
Structure Description | Glucocorticoid Receptor in complex with budesonide | PDB:5NFP | ||||
Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | Yes | [85] |
PDB Sequence |
PTLVSLLEVI
539 EPEVLYAGYD549 SSVPDSTWRI559 MTTLNMLGGR569 QMIAAVKWAK579 AIPGFRNLHL 589 DDQMTLLQYS599 WMSLMAFALG609 WRSYRQSSAN619 LLCFAPDLII629 NEQRMTLPDM 639 YDQCKHMLYV649 SSELHRLQVS659 YEEYLCMKTL669 LLLSSVPKDG679 LKSQELFDEI 689 RMTYIKELGK699 AIVKREGNSS709 QNWQRFYQLT719 KLLDSMHEVV729 ENLLNYCFQT 739 FLDKTMSIEF749 PEMLAEIITN759 QIPKYSNGNI769 KKLLFHQ
|
|||||
|
ILE559
4.304
MET560
3.394
LEU563
3.330
ASN564
2.974
LEU566
4.111
GLY567
3.611
GLN570
2.977
TRP600
4.079
MET601
3.712
MET604
3.616
ALA605
4.118
LEU608
4.362
ARG611
2.845
|
|||||
Ligand Name: Allermist | Ligand Info | |||||
Structure Description | Ligand binding domain of the glucocorticoid receptor complexed with fluticazone furoate | PDB:3CLD | ||||
Method | X-ray diffraction | Resolution | 2.84 Å | Mutation | Yes | [86] |
PDB Sequence |
PQLTPTLVSL
535 LEVIEPEVLY545 AGYDSSVPDS555 TWRIMTTLNM565 LGGRQVIAAV575 KWAKAIPGFR 585 NLHLDDQMTL595 LQYSWMYLMA605 FALGWRSYRQ615 NLLCFAPDLI628 INEQRMTLPG 638 MYDQCKHMLY648 VSSELHRLQV658 SYEEYLCMKT668 LLLLSSVPKD678 GLKSQELFDE 688 IRMTYIKELG698 KAIVKRQNWQ713 RFYQLTKLLD723 SMHEVVENLL733 NYCFQTFLDK 743 TMSIEFPEML753 AEIITNQIPK763 YSNGNIKKLL773 FHQ
|
|||||
|
ILE559
4.830
MET560
3.283
LEU563
3.181
ASN564
3.019
LEU566
3.990
GLY567
3.625
GLN570
2.733
TRP600
3.994
MET601
3.749
MET604
3.399
ALA605
3.284
LEU608
3.778
ARG611
3.013
PHE623
3.321
|
|||||
Click to View More Binding Site Information of This Target with Different Ligands |
Different Human System Profiles of Target | Top |
---|---|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
|
There is no similarity protein (E value < 0.005) for this target
|
Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy |
Degree | 35 | Degree centrality | 3.76E-03 | Betweenness centrality | 1.01E-03 |
---|---|---|---|---|---|
Closeness centrality | 2.61E-01 | Radiality | 1.45E+01 | Clustering coefficient | 2.02E-01 |
Neighborhood connectivity | 5.90E+01 | Topological coefficient | 6.06E-02 | Eccentricity | 11 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) | ||||||
Drug Resistance Mutation (DRM) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
1 | IL2 Signaling Pathway | |||||
2 | TCR Signaling Pathway | |||||
PID Pathway | [+] 6 PID Pathways | + | ||||
1 | Regulation of nuclear SMAD2/3 signaling | |||||
2 | Signaling events mediated by HDAC Class II | |||||
3 | FOXA2 and FOXA3 transcription factor networks | |||||
4 | Glucocorticoid receptor regulatory network | |||||
5 | Regulation of Androgen receptor activity | |||||
6 | AP-1 transcription factor network | |||||
Reactome | [+] 1 Reactome Pathways | + | ||||
1 | BMAL1:CLOCK,NPAS2 activates circadian gene expression | |||||
WikiPathways | [+] 8 WikiPathways | + | ||||
1 | Serotonin Receptor 4/6/7 and NR3C Signaling | |||||
2 | SIDS Susceptibility Pathways | |||||
3 | Nuclear Receptors Meta-Pathway | |||||
4 | Endoderm Differentiation | |||||
5 | Hair Follicle Development: Cytodifferentiation (Part 3 of 3) | |||||
6 | Adipogenesis | |||||
7 | Circadian Clock | |||||
8 | Nuclear Receptors |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | PXR-mediated induction of human CYP3A4 and mouse Cyp3a11 by the glucocorticoid budesonide. Eur J Pharm Sci. 2009 Mar 2;36(4-5):565-71. | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7061). | |||||
REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019137. | |||||
REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7434). | |||||
REF 6 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 7 | ClinicalTrials.gov (NCT01817322) Kidney Graft Function Under the Immunosuppression Strategies. U.S. National Institutes of Health. | |||||
REF 8 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018 | |||||
REF 9 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
REF 10 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3447). | |||||
REF 11 | Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54. | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033526) | |||||
REF 13 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7076). | |||||
REF 14 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074805. | |||||
REF 15 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7077). | |||||
REF 16 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019452. | |||||
REF 17 | ClinicalTrials.gov (NCT00539006) Comparator Study Evaluating Patient Preference Of FFNS vs. FPNS. U.S. National Institutes of Health. | |||||
REF 18 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 19 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010554. | |||||
REF 20 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2868). | |||||
REF 21 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2805). | |||||
REF 22 | ClinicalTrials.gov (NCT02342002) Mifepristone and Misoprostol Versus Misoprostol Alone for Missed Abortion: A Randomized-controlled Trial. U.S. National Institutes of Health. | |||||
REF 23 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7096). | |||||
REF 24 | ClinicalTrials.gov (NCT03697109) A Study of the Efficacy and Safety of Relacorilant in Patients With Endogenous Cushing Syndrome (GRACE). U.S. National Institutes of Health. | |||||
REF 25 | ClinicalTrials.gov (NCT00945646) FST-201 In The Treatment of Acute Fungal Otitis Externa. U.S. National Institutes of Health. | |||||
REF 26 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8643). | |||||
REF 27 | ClinicalTrials.gov (NCT01298752) Mapracorat Ophthalmic Suspension, 3% for the Treatment of Ocular Inflammation Following Cataract Surgery. U.S. National Institutes of Health. | |||||
REF 28 | ClinicalTrials.gov (NCT04123561) A Phase 3, Randomized, Double-blind, Placebo- and Active-controlled Study to Evaluate the Efficacy and Safety of TLC599 in Patients With Osteoarthritis of the Knee. U.S.National Institutes of Health. | |||||
REF 29 | ClinicalTrials.gov (NCT00555919) ZK 230211 in Postmenopausal Woman With Metastatic Breast Cancer. U.S. National Institutes of Health. | |||||
REF 30 | ClinicalTrials.gov (NCT05407324) A Phase 2, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study Evaluating Safety and Efficacy of CORT113176 (Dazucorilant) in Patients With Amyotrophic Lateral Sclerosis (DAZALS). U.S.National Institutes of Health. | |||||
REF 31 | ClinicalTrials.gov (NCT01239069) Safety and Efficacy Study of DE-110 Ophthalmic Suspension for the Treatment of Dry Eye Disease. U.S. National Institutes of Health. | |||||
REF 32 | ClinicalTrials.gov (NCT00035503) Multicenter Trial For Patients With Acute Crohn's Disease. U.S. National Institutes of Health. | |||||
REF 33 | ClinicalTrials.gov (NCT01299610) A Study to Test the Effect of 2 Different Doses of Topical GW870086X on Atopic Dermatitis Also Including a Postive Control and a Placebo. U.S. National Institutes of Health. | |||||
REF 34 | ClinicalTrials.gov (NCT00549497) A Randomized Study Evaluating Steroid Hormone Levels, Safety And Tolerability Of GW870086X In Healthy Volunteers. U.S. National Institutes of Health. | |||||
REF 35 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 36 | ClinicalTrials.gov (NCT01119313) Study to Investigate Skin Conditions and Patient Assessment of LAS 41002 in the Treatment of Atopic Eczema. U.S. National Institutes of Health. | |||||
REF 37 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5268). | |||||
REF 38 | S-adenosylmethionine decarboxylase as an enzyme target for therapy. Pharmacol Ther. 1992 Dec;56(3):359-77. | |||||
REF 39 | ClinicalTrials.gov (NCT00212797) A Study to Determine the Efficacy and Safety of 2 Doses of Org 34517 as Adjunctive Therapy in Subjects With Psychotic Major Depression (28130)(P05845). U.S. National Institutes of Health. | |||||
REF 40 | ClinicalTrials.gov (NCT00483743) Safety, Tolerability and PD Activity of Inhaled TPI 1020 Versus Inhaled Budesonide in COPD Patients. U.S. National Institutes of Health. | |||||
REF 41 | Glucocorticoid receptor nitration leads to enhanced anti-inflammatory effects of novel steroid ligands. J Immunol. 2003 Sep 15;171(6):3245-52. | |||||
REF 42 | ClinicalTrials.gov (NCT04331288) Effects of Ethanol on the Pharmacokinetics of PT-150 (Formerly ORG34517) (PT150 PK Study). U.S. National Institutes of Health. | |||||
REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031497) | |||||
REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024246) | |||||
REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011462) | |||||
REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021444) | |||||
REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029003) | |||||
REF 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011369) | |||||
REF 49 | The cannabinoid CB2 receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis. Eur J Pharmacol. 2006 Aug 7;542(1-3):179-83. | |||||
REF 50 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 51 | Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | |||||
REF 52 | Interaction between the glucocorticoid and erythropoietin receptors in human erythroid cells. Exp Hematol. 2009 May;37(5):559-72. | |||||
REF 53 | Functional mineralocorticoid receptor (MR) gene variation influences the cortisol awakening response after dexamethasone. Psychoneuroendocrinology. 2010 Apr;35(3):339-49. | |||||
REF 54 | Dexamethasone rapidly increases GABA release in the dorsal motor nucleus of the vagus via retrograde messenger-mediated enhancement of TRPV1 activity. PLoS One. 2013 Jul 30;8(7):e70505. | |||||
REF 55 | The glucocorticoid receptor heterocomplex gene STIP1 is associated with improved lung function in asthmatic subjects treated with inhaled corticost... J Allergy Clin Immunol. 2009 Jun;123(6):1376-83.e7. | |||||
REF 56 | Loteprednol etabonate: a soft steroid for the treatment of allergic diseases of the airways. Drugs Today (Barc). 2000 May;36(5):313-20. | |||||
REF 57 | Fluticasone furoate nasal spray in allergic rhinitis. Drugs Today (Barc). 2008 Apr;44(4):251-60. | |||||
REF 58 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
REF 59 | The glucocorticoid agonist activities of mifepristone (RU486) and progesterone are dependent on glucocorticoid receptor levels but not on EC50 values. Steroids. 2007 Jun;72(6-7):600-8. | |||||
REF 60 | Mometasone furoate is a less specific glucocorticoid than fluticasone propionate. Eur Respir J. 2002 Dec;20(6):1386-92. | |||||
REF 61 | Aldosterone (mineralocorticoid) equivalent to prednisolone (glucocorticoid) in reversing hearing loss in MRL/MpJ-Fas1pr autoimmune mice. Laryngoscope. 2000 Nov;110(11):1902-6. | |||||
REF 62 | Cytochromes P450 (CYP) in the Poeciliopsis lucida hepatocellular carcinoma cell line (PLHC-1): dose- and time-dependent glucocorticoid potentiation of CYP1A induction without induction of CYP3A. ArchBiochem Biophys. 1996 May 1;329(1):113-22. | |||||
REF 63 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 64 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 65 | A combination povidone-iodine 0.4%/dexamethasone 0.1% ophthalmic suspension in the treatment of adenoviral conjunctivitis. Adv Ther. 2009 Aug;26(8):776-83. | |||||
REF 66 | Characterization of ZK 245186, a novel, selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases. Br J Pharmacol. 2009 Oct;158(4):1088-103. | |||||
REF 67 | TLC599 in patients with osteoarthritis of the knee: a phase IIa, randomized, placebo-controlled, dose-finding study. Arthritis Res Ther. 2022 Feb 21;24(1):52. | |||||
REF 68 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6. | |||||
REF 69 | Long-term effects of the glucocorticoid receptor modulator CORT113176 in murine motoneuron degeneration. Brain Res. 2020 Jan 15;1727:146551. | |||||
REF 70 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031667) | |||||
REF 71 | Advances in corticosteroid therapy for ocular inflammation: loteprednol etabonate.Int J Inflam.2012;2012:789623. | |||||
REF 72 | Unique response profile of trabecular meshwork cells to the novel selective glucocorticoid receptor agonist, GW870086X. Invest Ophthalmol Vis Sci. 2013 Mar 1;54(3):2100-7. | |||||
REF 73 | Barrier-Restoring Therapies in Atopic Dermatitis: Current Approaches and Future Perspectives. Dermatol Res Pract. 2012; 2012: 923134. | |||||
REF 74 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
REF 75 | Differential effects of the new glucocorticoid receptor antagonist ORG 34517 and RU486 (mifepristone) on glucocorticoid receptor nuclear translocation in the AtT20 cell line. Ann N Y Acad Sci. 2008 Dec;1148:536-41. | |||||
REF 76 | Bronchoprotection in conscious guinea pigs by budesonide and the NO-donating analogue, TPI 1020, alone and combined with tiotropium or formoterol. Br J Pharmacol. 2012 Oct;167(3):515-26. | |||||
REF 77 | CRF(1) but not glucocorticoid receptor antagonists reduce separation-induced distress vocalizations in guinea pig pups and CRF overexpressing mouse pups. A combination study with paroxetine. Pharmacol Biochem Behav. 2017 Mar;154:11-19. | |||||
REF 78 | A nonsteroidal glucocorticoid receptor agonist inhibits allergen-induced late asthmatic responses. Am J Respir Crit Care Med. 2015 Jan 15;191(2):161-7. | |||||
REF 79 | CN patent application no. 102388025, Pyrimidopyridazine derivatives useful as p38 mapk inhibitors. | |||||
REF 80 | Local anti-inflammatory activity and systemic side effects of NM-135, a new prodrug glucocorticoid, in an experimental inflammatory rat model. Jpn J Pharmacol. 1998 Dec;78(4):505-9. | |||||
REF 81 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021444) | |||||
REF 82 | Glucocorticoids Pharmacology: Past, Present and Future. Current Pharmaceutical Design. VOLUME 16, ISSUE 32, Page(3540-3553), DOI: 10.2174/138161210793797915. | |||||
REF 83 | Blockade of glucocorticoid receptors with ORG 34116 does not normalize stress-induced symptoms in male tree shrews. Eur J Pharmacol. 2002 Dec 20;457(2-3):207-16. | |||||
REF 84 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
REF 85 | Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. J Med Chem. 2017 Oct 26;60(20):8591-8605. | |||||
REF 86 | X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain. J Med Chem. 2008 Jun 26;51(12):3349-52. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.