Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01436

Target Information
NamemRNA of glucocorticoid receptor    
Type of targetResearch target    
SynonymsmRNA of GR    
mRNA of GRL    
mRNA of NR3C1    
mRNA of Nuclear receptor subfamily 3 group C member 1    
DiseaseType 2 Diabetes
[ICD9: 250.00, 250.02   ICD10: E11]
[1]
Drug(s)ISIS-GCCRPreclinicalType 2 Diabetes[1]
UniProt IDP04150
PDB Structure1M2Z; 1NHZ; 1P93; 3BQD; 3CLD; 3E7C; 3H52; 3K22; 3K23; 4HN5; 4HN6.    
FunctionReceptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE) and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. 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. Involved in chromatin remodeling. Plays a significant role in transactivation. Involved in nuclear translocation (By similarity).    
SequenceMDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
Target ValidationClick to Find Target Validation Information.    
Inhibitor1- (2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-[2]
1- (3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-[2]
1-Methoxy-6-phenyl-6H-benzo[c]chromen-8-ylamine[3]
1-Methoxy-6-phenyl-6H-benzo[c]chromene[3]
2,2,2-TRIFLUORO-1- (4-FLUOROPHENYL)-1-[2]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[4]
A-348441[5]
AL-43[6]
CP-394531[7]
CP-409069[7]
DI-O-METHYLENDIANDRIN A[8]
ENDIANDRIN A[8]
EPIERENONE[9]
LG-120838[10]
LGD-5552[11]
Methanesulfonamide derivative[12]
Methanesulfonamide derivative[12]
Methanesulfonamide derivative[12]
Methanesulfonamide derivative[12]
Methanesulfonamide derivative[12]
Methanesulfonamide derivative[12]
Methanesulfonamide derivative[12]
ONAPRISTONE[13]
OXDEX[14]
RU-43044[7]
WAY-214950[15]
WAY-252623[15]
AntisenseISIS-GCCR[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 12011 Pipeline of ISIS Pharm. To Reference
Ref 2Bioorg Med Chem Lett. 2010 May 15;20(10):3017-20. Epub 2010 Apr 11.5-Functionalized indazoles as glucocorticoid receptor agonists. To Reference
Ref 3Bioorg Med Chem Lett. 2004 May 3;14(9):2079-82.Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists. To Reference
Ref 4J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 5Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90. Epub 2006 Sep 20.Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists. To Reference
Ref 6Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7.Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators. To Reference
Ref 7J Med Chem. 2010 Apr 22;53(8):3065-74.Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators. To Reference
Ref 8J Nat Prod. 2007 Jul;70(7):1118-21. Epub 2007 Jun 21.Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum. To Reference
Ref 9J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.(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. To Reference
Ref 10J Med Chem. 1998 Oct 22;41(22):4354-9.5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. To Reference
Ref 11Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. Epub 2007 Nov 21.Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. To Reference
Ref 12Bioorg Med Chem Lett. 2004 Aug 16;14(16):4179-83.Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator. To Reference
Ref 13Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8.Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. To Reference
Ref 14J Med Chem. 2009 Aug 13;52(15):4604-12.Investigation of the relative cellular permeability of DNA-binding pyrrole-imidazole polyamides. To Reference
Ref 15J Med Chem. 2008 Nov 27;51(22):7161-8.Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543