Target Information

Target General Infomation
Target ID
T03818
Former ID
TTDR01386
Target Name
mRNA of PPAR-gamma
Gene Name
PPARG
Synonyms
Nuclear receptor subfamily 1 group C member 3 (mRNA); PPARG (mRNA); PPARgamma (mRNA); Peroxisome proliferatoractivated receptor gamma (mRNA); PPARG
Target Type
Research
BioChemical Class
Nuclear hormone receptor
Target Validation
T03818
UniProt ID
P37231
Sequence
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY
Inhibitor (9Z,12E)-12-nitrooctadeca-9,12-dienoic acid Drug Info [530350]
(E)-10-Nitrohexadec-9-enoic Acid Drug Info [530350]
(E)-10-nitrooctadec-9-enoic acid Drug Info [530350]
(E)-12-Nitrooctadec-12-enoic Acid Drug Info [530350]
(E)-13-Nitrooctadec-12-enoic Acid Drug Info [530350]
(E)-5-Nitrooctadec-5-enoic Acid Drug Info [530350]
(E)-6-Nitrooctadec-5-enoic Acid Drug Info [530350]
(E)-9-Nitrohexadec-9-enoicAcid Drug Info [530350]
(E)-9-nitrooctadec-9-enoic acid Drug Info [530350]
2-chloro-5-nitro-N-(pyridin-4-yl)benzamide Drug Info [529363]
BRL-48482 Drug Info [551304]
CHLOROCYCLINONE A Drug Info [529182]
CHLOROCYCLINONE B Drug Info [529182]
CHLOROCYCLINONE C Drug Info [529182]
CHLOROCYCLINONE D Drug Info [529182]
GNF-PF-2893 Drug Info [531262]
GNF-PF-3037 Drug Info [531262]
GW-9662 Drug Info [529363]
L-165461 Drug Info [526582]
L-796449 Drug Info [526582]
L-Tryptophan-L-2-aminoadipic acid Drug Info [529363]
L-Tryptophan-L-arginine Drug Info [529363]
L-Tryptophan-L-asparagine Drug Info [529363]
L-Tryptophan-L-aspartic acid Drug Info [529363]
L-Tryptophan-L-glutamine Drug Info [529363]
L-Tryptophan-L-leucine Drug Info [529363]
PD-068235 Drug Info [529363]
PLOGLITAZONE Drug Info [527158]
SB-213068 Drug Info [551304]
Agonist AD-5061 Drug Info [527124]
BADGE Drug Info [525678]
COOH Drug Info [526520]
DRF 2519 Drug Info [527076]
FMOC-L-Leucine Drug Info [526183]
GW0072 Drug Info [525499]
GW1929 Drug Info [525528]
L-764406 Drug Info [525436]
L-783483 Drug Info [525425]
LG100754 Drug Info [526284]
LY-465608 Drug Info [526080]
MRL20 Drug Info [527337]
MRL24 Drug Info [527337]
nTzDpa Drug Info [526526]
PAT5A Drug Info [525920]
reglitazar Drug Info [534829]
tagitinin A Drug Info [531847]
tirotundin Drug Info [531847]
TZD18 Drug Info [526920]
[125I]SB-236636 Drug Info [534550]
[3H]AD5075 Drug Info [534222]
[3H]GW2331 Drug Info [534367]
Antagonist CDDO-Me Drug Info [525892]
T0070907 Drug Info [526285]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
DRM DRM Info
Pathways
KEGG Pathway PPAR signaling pathway
AMPK signaling pathway
Osteoclast differentiation
Huntington&#039
s disease
Pathways in cancer
Transcriptional misregulation in cancer
Thyroid cancer
NetPath Pathway IL1 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Leptin Signaling Pathway
PANTHER Pathway CCKR signaling map ST
Pathway Interaction Database Noncanonical Wnt signaling pathway
Calcineurin-regulated NFAT-dependent transcription in lymphocytes
Signaling events mediated by HDAC Class I
RXR and RAR heterodimerization with other nuclear receptor
Regulation of retinoblastoma protein
Reactome PPARA activates gene expression
Transcriptional regulation of white adipocyte differentiation
Nuclear Receptor transcription pathway
WikiPathways Wnt Signaling Pathway Netpath
Nuclear Receptors in Lipid Metabolism and Toxicity
Differentiation of white and brown adipocyte
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Transcriptional Regulation of White Adipocyte Differentiation
Adipogenesis
SREBP signalling
Nuclear Receptors
References
Ref 525425Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. J Biol Chem. 1999 Mar 5;274(10):6718-25.
Ref 525436L-764406 is a partial agonist of human peroxisome proliferator-activated receptor gamma. The role of Cys313 in ligand binding. J Biol Chem. 1999 Mar 19;274(12):7913-22.
Ref 525499A peroxisome proliferator-activated receptor gamma ligand inhibits adipocyte differentiation. Proc Natl Acad Sci U S A. 1999 May 25;96(11):6102-6.
Ref 525528A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes. 1999 Jul;48(7):1415-24.
Ref 525678A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation. J Biol Chem. 2000 Jan 21;275(3):1873-7.
Ref 525892A synthetic triterpenoid, 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO), is a ligand for the peroxisome proliferator-activated receptor gamma. Mol Endocrinol. 2000 Oct;14(10):1550-6.
Ref 525920Euglycemic and hypolipidemic activity of PAT5A: a unique thiazolidinedione with weak peroxisome proliferator activated receptor gamma activity. Metabolism. 2000 Nov;49(11):1417-23.
Ref 526080Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists. J Med Chem. 2001 Jun 21;44(13):2061-4.
Ref 526183A unique PPARgamma ligand with potent insulin-sensitizing yet weak adipogenic activity. Mol Cell. 2001 Oct;8(4):737-47.
Ref 526284The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands. J Biol Chem. 2002 Apr 12;277(15):12503-6. Epub 2002 Feb 27.
Ref 526285T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 2002 May 31;277(22):19649-57. Epub 2002 Mar 4.
Ref 526520PPAR-gamma activation mediates adipose depot-specific effects on gene expression and lipoprotein lipase activity: mechanisms for modulation of postprandial lipemia and differential adipose accretion.Diabetes. 2003 Feb;52(2):291-9.
Ref 526526Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator. Mol Endocrinol. 2003 Apr;17(4):662-76. Epub 2003 Jan 16.
Ref 526582Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists.
Ref 526920A novel peroxisome proliferator-activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis. Endocrinology. 2004 Apr;145(4):1640-8. Epub 2003 Dec 30.
Ref 527076Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma. Eur J Pharmacol. 2004 May 3;491(2-3):195-206.
Ref 527124A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26.
Ref 527158J Med Chem. 2004 Aug 12;47(17):4118-27.Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Ref 527337Benzoyl 2-methyl indoles as selective PPARgamma modulators. Bioorg Med Chem Lett. 2005 Jan 17;15(2):357-62.
Ref 529182J Nat Prod. 2007 Dec;70(12):1934-8. Epub 2007 Nov 29.Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation.
Ref 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Ref 530350J Med Chem. 2009 Aug 13;52(15):4631-9.Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531847Sesquiterpene lactones from Tithonia diversifolia act as peroxisome proliferator-activated receptor agonists. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2954-8.
Ref 534222Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-gamma: binding and activation correlate with antidiabetic actions in db/db mice. Endocrinology. 1996 Oct;137(10):4189-95.
Ref 534367Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma. Proc Natl Acad Sci U S A. 1997 Apr 29;94(9):4318-23.
Ref 534550Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma. J Pharmacol Exp Ther. 1998 Feb;284(2):751-9.
Ref 534829Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative. Eur J Pharmacol. 1999 Jan 8;364(2-3):211-9.
Ref 549615US patent application no. 6,159,734, Antisense modulation of peroxisome proliferator-activated receptor gamma expression.
Ref 549674US patent application no. 7,425,545, Modulation of C-reactive protein expression.
Ref 551304Non thiazolidinedione antihyperglycaemic agents. 2: alpha-Carbon substituted beta-phenylpropanoic acids1, Bioorg. Med. Chem. Lett. 6(17):2127-2130 (1996).

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