Drug General Information
Drug ID
D0Q9FZ
Former ID
DIB020212
Drug Name
LG100754
Synonyms
LG 100754; LG754
Drug Type
Small molecular drug
Indication Discovery agent Investigative [539856]
Structure
Download
2D MOL
Formula
C26H36O3
InChI
InChI=1S/C26H36O3/c1-8-14-29-23-17-22-21(25(4,5)12-13-26(22,6)7)16-20(23)19(3)11-9-10-18(2)15-24(27)28/h9-11,15-17H,8,12-14H2,1-7H3,(H,27,28)/b10-9+,18-15+,19-11-
InChIKey
HNODNXQAYXJFMQ-LQUSFLDPSA-N
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Retinoid X receptor-beta Target Info Antagonist [534228]
Retinoic acid receptor RXR-alpha Target Info Antagonist [526108]
mRNA of PPAR-gamma Target Info Agonist [526284]
Retinoic acid receptor RXR-gamma Target Info Antagonist [534228]
KEGG Pathway PPAR signaling pathway
PI3K-Akt signaling pathway
Thyroid hormone signaling pathway
Adipocytokine signaling pathway
Non-alcoholic fatty liver disease (NAFLD)
Bile secretion
Hepatitis C
Pathways in cancer
Transcriptional misregulation in cancer
Thyroid cancer
Small cell lung cancer
Non-small cell lung cancerhsa03320:PPAR signaling pathway
AMPK signaling pathway
Osteoclast differentiation
Huntington's disease
Thyroid cancerhsa03320:PPAR signaling pathway
Non-small cell lung cancer
NetPath Pathway IL1 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Leptin Signaling Pathway
PANTHER Pathway Vitamin D metabolism and pathwayP06959:CCKR signaling map ST
Pathway Interaction Database Regulation of Androgen receptor activity
RXR and RAR heterodimerization with other nuclear receptor
Retinoic acid receptors-mediated signaling
a6b1 and a6b4 Integrin signalingwnt_noncanonical_pathway:Noncanonical Wnt signaling pathway
Calcineurin-regulated NFAT-dependent transcription in lymphocytes
Signaling events mediated by HDAC Class I
Regulation of retinoblastoma proteinar_tf_pathway:Regulation of Androgen receptor activity
a6b1 and a6b4 Integrin signaling
Reactome RORA activates gene expression
BMAL1:CLOCK,NPAS2 activates circadian gene expression
Recycling of bile acids and salts
PPARA activates gene expression
Import of palmitoyl-CoA into the mitochondrial matrix
YAP1- and WWTR1 (TAZ)-stimulated gene expression
Regulation of pyruvate dehydrogenase (PDH) complex
Endogenous sterols
Transcriptional activation of mitochondrial biogenesis
Activation of gene expression by SREBF (SREBP)
Transcriptional regulation of white adipocyte differentiation
Nuclear Receptor transcription pathway
Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Circadian ClockR-HSA-1989781:PPARA activates gene expression
Nuclear Receptor transcription pathwayR-HSA-383280:Nuclear Receptor transcription pathway
WikiPathways Vitamin A and Carotenoid Metabolism
NRF2 pathway
Nuclear Receptors Meta-Pathway
Farnesoid X Receptor Pathway
PPAR Alpha Pathway
Vitamin D Receptor Pathway
Pregnane X Receptor pathway
Constitutive Androstane Receptor Pathway
Liver X Receptor Pathway
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Transcriptional Regulation of White Adipocyte Differentiation
YAP1- and WWTR1 (TAZ)-stimulated gene expression
Activation of Gene Expression by SREBP (SREBF)
Integrated Pancreatic Cancer Pathway
Adipogenesis
Circadian Clock
Nuclear Receptors
Vitamin D MetabolismWP363:Wnt Signaling Pathway Netpath
Nuclear Receptors in Lipid Metabolism and Toxicity
Differentiation of white and brown adipocyte
SREBP signalling
Nuclear ReceptorsWP716:Vitamin A and Carotenoid Metabolism
References
Ref 539856(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: 2814).
Ref 526108The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo. Mol Endocrinol. 2001 Aug;15(8):1360-9.
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 534228Activation of specific RXR heterodimers by an antagonist of RXR homodimers. Nature. 1996 Oct 3;383(6599):450-3.

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