FXR/RXR Activation
The farnesoid X receptor (FXR) is a member of the nuclear family of receptors and has emerged as a key player in the control of numerous metabolic pathways. Bile acids and their intermediates activate FXR, which thus serves as a sensor of bile acid levels. Along with retinoid X receptor (RXR), FXR plays a crucial role in linking bile acid regulation with lipoprotein, lipid and glucose metabolism. The concentration of bile acids and their intermediates can be elevated in conditions like cholestasis or inborn metabolic disorders. The metabolic syndrome is characterized by insulin resistance and glucose tolerance, abdominal obesity, hypertension, low high-density lipoproteins (HDL) and hypertriglyceridemia...
Pathway Summary
The farnesoid X receptor (FXR) is a member of the nuclear family of receptors and has emerged as a key player in the control of numerous metabolic pathways. Bile acids and their intermediates activate FXR, which thus serves as a sensor of bile acid levels. Along with retinoid X receptor (RXR), FXR plays a crucial role in linking bile acid regulation with lipoprotein, lipid and glucose metabolism. The concentration of bile acids and their intermediates can be elevated in conditions like cholestasis or inborn metabolic disorders. The metabolic syndrome is characterized by insulin resistance and glucose tolerance, abdominal obesity, hypertension, low high-density lipoproteins (HDL) and hypertriglyceridemia. As a modulator of bile, lipid and glucose homeostasis, FXR is an interesting pharmacological target for therapeutic applications.
FXR/RXR Activation Genes list
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A1BGalpha-1-B glycoprotein ABCB11ATP binding cassette subfamily B member 11 ABCB4ATP binding cassette subfamily B member 4 ABCC2ATP binding cassette subfamily C member 2 ABCG5ATP binding cassette subfamily G member 5 ABCG8ATP binding cassette subfamily G member 8 AGTangiotensinogen AHSGalpha 2-HS glycoprotein AKT1AKT serine/threonine kinase 1 AKT2AKT serine/threonine kinase 2 AKT3AKT serine/threonine kinase 3 ALBalbumin AMBPalpha-1-microglobulin/bikunin precursor APOA1apolipoprotein A1 APOA2apolipoprotein A2 APOA4apolipoprotein A4 APOBapolipoprotein B APOC1apolipoprotein C1 APOC2apolipoprotein C2 APOC3apolipoprotein C3 APOC4apolipoprotein C4 APODapolipoprotein D APOEapolipoprotein E APOFapolipoprotein F APOHapolipoprotein H APOL1apolipoprotein L1 APOMapolipoprotein M BAATbile acid-CoA:amino acid N-acyltransferase C3complement C3 C9complement C9 CAMPcathelicidin antimicrobial peptide CETPcholesteryl ester transfer protein CLUclusterin CREBBPCREB binding protein CYP27A1cytochrome P450 family 27 subfamily A member 1 CYP7A1cytochrome P450 family 7 subfamily A member 1 CYP8B1cytochrome P450 family 8 subfamily B member 1 FABP6fatty acid binding protein 6 FASNfatty acid synthase FBP1fructose-bisphosphatase 1 FETUBfetuin B FGAfibrinogen alpha chain FGF19fibroblast growth factor 19 FGFR4fibroblast growth factor receptor 4 FOXA1forkhead box A1 FOXA2forkhead box A2 FOXA3forkhead box A3 FOXO1forkhead box O1 G6PC1glucose-6-phosphatase catalytic subunit 1 G6PC2glucose-6-phosphatase catalytic subunit 2 G6PC3glucose-6-phosphatase catalytic subunit 3 GCGC vitamin D binding protein HNF1AHNF1 homeobox A HNF4Ahepatocyte nuclear factor 4 alpha HPRhaptoglobin-related protein HPXhemopexin IL18interleukin 18 IL1Ainterleukin 1 alpha IL1Binterleukin 1 beta IL1F10interleukin 1 family member 10 IL1RNinterleukin 1 receptor antagonist IL33interleukin 33 IL36Ainterleukin 36 alpha IL36Binterleukin 36 beta IL36Ginterleukin 36 gamma IL36RNinterleukin 36 receptor antagonist IL37interleukin 37 INSinsulin ITIH4inter-alpha-trypsin inhibitor heavy chain 4 KNG1kininogen 1 LCATlecithin-cholesterol acyltransferase LIPClipase C, hepatic type LPLlipoprotein lipase MAP2K4mitogen-activated protein kinase kinase 4 MAPK10mitogen-activated protein kinase 10 MAPK12mitogen-activated protein kinase 12 MAPK8mitogen-activated protein kinase 8 MAPK9mitogen-activated protein kinase 9 MLXIPLMLX interacting protein like MTTPmicrosomal triglyceride transfer protein NR0B2nuclear receptor subfamily 0 group B member 2 NR1H3nuclear receptor subfamily 1 group H member 3 NR1H4nuclear receptor subfamily 1 group H member 4 NR1I2nuclear receptor subfamily 1 group I member 2 NR5A2nuclear receptor subfamily 5 group A member 2 ORM1orosomucoid 1 ORM2orosomucoid 2 PCK2phosphoenolpyruvate carboxykinase 2, mitochondrial PCYOX1prenylcysteine oxidase 1 PKLRpyruvate kinase L/R PLTPphospholipid transfer protein PON1paraoxonase 1 PON3paraoxonase 3 PPARAperoxisome proliferator activated receptor alpha PPARGperoxisome proliferator activated receptor gamma PPARGC1APPARG coactivator 1 alpha RARAretinoic acid receptor alpha RBP4retinol binding protein 4 RXRAretinoid X receptor alpha SAA1serum amyloid A1 SAA2serum amyloid A2 SAA4serum amyloid A4, constitutive SCARB1scavenger receptor class B member 1 SDC1syndecan 1 SERPINA1serpin family A member 1 SERPINF1serpin family F member 1 SERPINF2serpin family F member 2 SLC10A1solute carrier family 10 member 1 SLC10A2solute carrier family 10 member 2 SLC22A7solute carrier family 22 member 7 SLC27A5solute carrier family 27 member 5 SLC4A2solute carrier family 4 member 2 SLC51Asolute carrier family 51 subunit alpha SLC51Bsolute carrier family 51 subunit beta SLCO1B1solute carrier organic anion transporter family member 1B1 SLCO1B3solute carrier organic anion transporter family member 1B3 SULT2A1sulfotransferase family 2A member 1 TFtransferrin TNFtumor necrosis factor TTRtransthyretin UGT2B4UDP glucuronosyltransferase family 2 member B4 VLDLRvery low density lipoprotein receptor VTNvitronectin
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