Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00420

Target Information
NameOxysterols receptor LXR-alpha    
Type of targetResearch target    
SynonymsLXRalpha    
Liver X receptor alpha    
Nuclear orphan receptor LXR-alpha    
Nuclear receptor LXRalpha    
DiseaseAtherosclerosis
[ICD9: 414.0, 440   ICD10: I70]
[1]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[2]
BioChemical ClassZinc-finger    
PathwayPPAR signaling pathway
UniProt IDQ13133
PDB Structure1UHL.    
FunctionOrphan receptor. Interaction with rxr shifts rxr from its role as a silent dna-binding partner to an active ligand- binding subunit in mediating retinoid responses through target genes defined by lxres. Lxres are dr4-type response elements.    
SequenceMSLWLGAPVPDIPPDSAVELWKPGAQDASSQAQGGSSCILREEARMPHSAGGTAGVGLEA AEPTALLTRAEPPSEPTEIRPQKRKKGPAPKMLGNELCSVCGDKASGFHYNVLSCEGCKG FFRRSVIKGAHYICHSGGHCPMDTYMRRKCQECRLRKCRQAGMREECVLSEEQIRLKKLK RQEEEQAHATSLPPRASSPPQILPQLSPEQLGMIEKLVAAQQQCNRRSFSDRLRVTPWPM APDPHSREARQQRFAHFTELAIVSVQEIVDFAKQLPGFLQLSREDQIALLKTSAIEVMLL ETSRRYNPGSESITFLKDFSYNREDFAKAGLQVEFINPIFEFSRAMNELQLNDAEFALLI AISIFSADRPNVQDQLQVERLQHTYVEALHAYVSIHHPHDRLMFPRMLMKLVSLRTLSSV HSEQVFALRLQDKKLPPLLSEIWDVHE
Target ValidationClick to Find Target Validation Information.    
Inhibitor12,17-dehydroxyriccardin C[3]
12-dehydroxyriccardin C[3]
17-dehydroxyriccardin C[3]
2- (2-hexylphenyl)isoindoline-1,3-dione[3]
2- (2-phenethylphenyl)isoindoline-1,3-dione[4]
2-Benzyl-3-phenyl-7- (trifluoromethyl)-2H-indazole[5]
2-benzyl-4,5,6,7-tetrachloroisoindoline-1,3-dione[6]
4,12,17-dehydroxyriccardin C[3]
4,17-dehydroxyriccardin C[3]
4-dehydroxyriccardin C[3]
5-chloro-2- (4-phenylbutyl)isoindoline-1,3-dione[6]
GSK-9772[7]
GW-3965[5]
Guttiferone I[8]
N-{4-[2- (3-Hydroxyphenyl)ethyl]phenyl}phthalimide[4]
N-{4-[2- (3-Methoxyphenyl)ethyl]phenyl}phthalimide[4]
N-{4-[2- (4-Hydroxyphenyl)ethyl]phenyl}phthalimide[4]
N-{4-[2- (4-Methoxyphenyl)ethyl]phenyl}phthalimide[4]
WAY-214950[5]
WAY-252623[5]
WAY-254011[9]
WAY-254011[10]
riccardin C[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1A novel liver X receptor agonist establishes species differences in the regulation of cholesterol 7alpha-hydroxylase (CYP7a). Endocrinology. 2002 Jul;143(7):2548-58. To Reference
Ref 2The nuclear receptors FXR and LXRalpha: potential targets for the development of drugs affecting lipid metabolism and neoplastic diseases. Curr Pharm Des. 2001 Mar;7(4):231-59. To Reference
Ref 3Bioorg Med Chem. 2008 Apr 15;16(8):4272-85. Epub 2008 Feb 29.Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development. To Reference
Ref 4Bioorg Med Chem. 2009 Jul 15;17(14):5001-14. Epub 2009 Jun 2.Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists. To Reference
Ref 5J 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
Ref 6Bioorg Med Chem Lett. 2007 Jul 15;17(14):3957-61. Epub 2007 Apr 30.Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors. To Reference
Ref 7J Med Chem. 2008 Sep 25;51(18):5758-65.Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. To Reference
Ref 8J Nat Prod. 2005 Apr;68(4):617-9.Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand. To Reference
Ref 9Bioorg Med Chem. 2009 May 15;17(10):3519-27. Epub 2009 Apr 12.Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta. To Reference
Ref 10Bioorg Med Chem. 2009 Dec 1;17(23):8086-92. Epub 2009 Oct 4.4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists. To Reference



 

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