Target Information

Target General Infomation
Target ID
T13714
Former ID
TTDR00421
Target Name
Oxysterols receptor LXR-beta
Gene Name
NR1H2
Synonyms
LXRbeta; Liver X receptor beta; Nuclear orphan receptor LXR-beta; Nuclear receptor NER; Ubiquitously-expressed nuclear receptor; NR1H2
Target Type
Research
Disease Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Function
Nuclear receptor. Binds preferentially to double- stranded oligonucleotide direct repeats having the consensus half- site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8; DLDLR and LRP8. Interplays functionally with RORA for the regulation of genes involved in liver metabolism (By similarity).
BioChemical Class
Nuclear hormone receptor
Target Validation
T13714
UniProt ID
P55055
Sequence
MSSPTTSSLDTPLPGNGPPQPGAPSSSPTVKEEGPEPWPGGPDPDVPGTDEASSACSTDW
VIPDPEEEPERKRKKGPAPKMLGHELCRVCGDKASGFHYNVLSCEGCKGFFRRSVVRGGA
RRYACRGGGTCQMDAFMRRKCQQCRLRKCKEAGMREQCVLSEEQIRKKKIRKQQQESQSQ
SQSPVGPQGSSSSASGPGASPGGSEAGSQGSGEGEGVQLTAAQELMIQQLVAAQLQCNKR
SFSDQPKVTPWPLGADPQSRDARQQRFAHFTELAIISVQEIVDFAKQVPGFLQLGREDQI
ALLKASTIEIMLLETARRYNHETECITFLKDFTYSKDDFHRAGLQVEFINPIFEFSRAMR
RLGLDDAEYALLIAINIFSADRPNVQEPGRVEALQQPYVEALLSYTRIKRPQDQLRFPRM
LMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
Inhibitor 12,17-dehydroxyriccardin C Drug Info [529375]
12-dehydroxyriccardin C Drug Info [529375]
17-dehydroxyriccardin C Drug Info [529375]
2-Benzyl-3-phenyl-7-(trifluoromethyl)-2H-indazole Drug Info [529781]
2-benzyl-4,5,6,7-tetrachloroisoindoline-1,3-dione Drug Info [528834]
2-Propanol, Isopropanol Drug Info [551393]
4,17-dehydroxyriccardin C Drug Info [529375]
4-dehydroxyriccardin C Drug Info [529375]
Benzenesulfonyl Drug Info [551393]
GSK-9772 Drug Info [529702]
GW-3965 Drug Info [529781]
N-{4-[2-(3-Methoxyphenyl)ethyl]phenyl}phthalimide Drug Info [530220]
Riccardin C Drug Info [529375]
WAY-214950 Drug Info [529781]
WAY-252623 Drug Info [529781]
WAY-254011 Drug Info [530094]
Agonist 22R-hydroxycholesterol Drug Info [534255]
24(S), 25-epoxycholesterol Drug Info [532179]
24(S)-hydroxycholesterol Drug Info [534311]
27-hydroxycholesterol Drug Info [526122]
acetyl-podocarpic dimer Drug Info [526248]
AZ12260493 Drug Info [543893]
desmosterol Drug Info [528328]
L-783483 Drug Info [535486]
Antagonist GSK2033 Drug Info [530809]
SR9238 Drug Info [532155]
Pathways
Pathway Interaction Database RXR and RAR heterodimerization with other nuclear receptor
Reactome Nuclear Receptor transcription pathway
WikiPathways SREBP signalling
Nuclear Receptors
References
Ref 52612227-hydroxycholesterol is an endogenous ligand for liver X receptor in cholesterol-loaded cells. J Biol Chem. 2001 Oct 19;276(42):38378-87. Epub 2001 Aug 14.
Ref 526248A potent synthetic LXR agonist is more effective than cholesterol loading at inducing ABCA1 mRNA and stimulating cholesterol efflux. J Biol Chem. 2002 Mar 22;277(12):10021-7. Epub 2002 Jan 14.
Ref 528328Sterol intermediates from cholesterol biosynthetic pathway as liver X receptor ligands. J Biol Chem. 2006 Sep 22;281(38):27816-26. Epub 2006 Jul 20.
Ref 528834Bioorg 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.
Ref 529375Bioorg 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.
Ref 529702J 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.
Ref 529781J 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.
Ref 530094Bioorg 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.
Ref 530220Bioorg 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.
Ref 530809Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6.
Ref 532155A liver-selective LXR inverse agonist that suppresses hepatic steatosis. ACS Chem Biol. 2013 Mar 15;8(3):559-67.
Ref 532179Brain endogenous liver X receptor ligands selectively promote midbrain neurogenesis. Nat Chem Biol. 2013 Feb;9(2):126-33.
Ref 534255An oxysterol signalling pathway mediated by the nuclear receptor LXR alpha. Nature. 1996 Oct 24;383(6602):728-31.
Ref 534311Activation of the nuclear receptor LXR by oxysterols defines a new hormone response pathway. J Biol Chem. 1997 Feb 7;272(6):3137-40.
Ref 535486A novel liver X receptor agonist establishes species differences in the regulation of cholesterol 7alpha-hydroxylase (CYP7a). Endocrinology. 2002 Jul;143(7):2548-58.
Ref 543893(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. (Target id: 601).
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.