SlideShare une entreprise Scribd logo
1  sur  10
The nuclear receptor superfamily




                            Mangelsdorf et al, (1995) Cell 83:835-839
Domain structure of nuclear hormone receptors




                              Gronemeyer et al, (2004) Nat Rev Drug Discov 3:950-964




                                             Mangelsdorf et al, (1995) Cell 83:835-839
Mode of action of nuclear receptors (NRs)




                               Gronemeyer et al, (2004) Nat Rev Drug Discov 3:950-964
Nuclear Receptors tissue distribution


                  CNS         Endocrine       GI tract   Adipose   Immune   Reproductive   Respiratory   Structural

    FXR            •              •            •••         •         •           •             •             •

   CAR             •              •            •••         •         •           •             •             •

    PXR            •              •            •••         •         •           •             •             •

   VDR             •             ••            •••         •         •           •             •            ••

    LXR            •              •            •••        •••        •           •             ••            •

  PPARγ            •              •             ••        •••        •           •             •             •

  PPARα            •              •            •••        ••••       •           •             ••            •

 PPAR β/δ         ••             ••            •••         ••        •          ••             ••           ••

    GR           ••••             •            ••••       •••       •••         ••            •••           •••

    TRα           •••             •              •         •         •           •             •             •

    TRβ           •••            ••            •••         ••        •          ••             ••           ••

   RXRα           ••             ••             ••         ••        •          ••             ••           ••

    AR             •             ••              •         •         •          •••            •             •

CNS: Central Nervous System; GI: gastrointestinal


                                                                                                              NURSA
PPARγ




PPARβ/δ




          NURSA
FXR




VDR




      NURSA
CAR




PXR




      NURSA
Nuclear Receptors in immune system

                        PPARγ   FXR         PXR        CAR            VDR
WholeBlood                +      +            +          +             +++
CD14 Monocytes            +     +             +           +       +++++ 
CD33 Myeloid              +     +             +          +        +++++ 
CD56 NKCells              +     +             +           +           +++ 
CD4 Tcells                +     +             +          +            +++ 
CD8 Tcells                +     +             +          +            +++ 
BDCA4 Dentritic Cells     +     +             +          +            +++ 
CD19 BCells.neg.sel.      +     +             +          +            +++ 
X721 B lymphoblasts       +     +             +          +            +++ 
CD105 Endothelial         +     +             +          +            +++ 
CD34                      +     +             +          +            +++ 

                                     Bile acids activated receptors


                                                                      BioGPS The gene portal Hub
Nuclear receptors versus inflammation: 
                                       mechanisms of transrepression-I 




Pascual G, Glass CK Trends Endocrinol Metab. 2006 Oct;17(8):321-7. 
Nuclear receptors versus inflammation:
                                      mechanisms of transrepression-II




Pascual G, Glass CK Trends Endocrinol Metab. 2006 Oct;17(8):321-7.

Contenu connexe

Plus de Attività scientifica

Metabolomic profile of the probiotic of VSL#3 in vitro
Metabolomic profile of the probiotic of VSL#3 in  vitro   Metabolomic profile of the probiotic of VSL#3 in  vitro
Metabolomic profile of the probiotic of VSL#3 in vitro Attività scientifica
 
Nanomedecine - Just accepted for publication. Decoy receptor for CCR5
Nanomedecine - Just accepted for publication. Decoy receptor for CCR5Nanomedecine - Just accepted for publication. Decoy receptor for CCR5
Nanomedecine - Just accepted for publication. Decoy receptor for CCR5Attività scientifica
 
GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages
GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages  GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages
GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages Attività scientifica
 
Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1
Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1
Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1Attività scientifica
 
Digestive Disease Week 2017 The probiotic VSL#3 shows metabolic instability
Digestive Disease Week 2017 The probiotic VSL#3   shows metabolic instability Digestive Disease Week 2017 The probiotic VSL#3   shows metabolic instability
Digestive Disease Week 2017 The probiotic VSL#3 shows metabolic instability Attività scientifica
 
Digestive Disease Week 2017 BAR704 reduces liver fibrosis
Digestive  Disease  Week 2017    BAR704   reduces liver fibrosisDigestive  Disease  Week 2017    BAR704   reduces liver fibrosis
Digestive Disease Week 2017 BAR704 reduces liver fibrosisAttività scientifica
 
BAR501 a selective TGR5 ligand attenuates NASH
BAR501 a selective TGR5 ligand attenuates NASHBAR501 a selective TGR5 ligand attenuates NASH
BAR501 a selective TGR5 ligand attenuates NASHAttività scientifica
 
BILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONS
BILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONSBILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONS
BILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONSAttività scientifica
 
Nanotechnology update A seminar by Prof. Tatiana Tennikova
Nanotechnology update A seminar by Prof. Tatiana TennikovaNanotechnology update A seminar by Prof. Tatiana Tennikova
Nanotechnology update A seminar by Prof. Tatiana TennikovaAttività scientifica
 
Expert opinion on therapeutic patent
Expert opinion on  therapeutic patentExpert opinion on  therapeutic patent
Expert opinion on therapeutic patentAttività scientifica
 

Plus de Attività scientifica (20)

Metabolomic profile of the probiotic of VSL#3 in vitro
Metabolomic profile of the probiotic of VSL#3 in  vitro   Metabolomic profile of the probiotic of VSL#3 in  vitro
Metabolomic profile of the probiotic of VSL#3 in vitro
 
Nanomedecine - Just accepted for publication. Decoy receptor for CCR5
Nanomedecine - Just accepted for publication. Decoy receptor for CCR5Nanomedecine - Just accepted for publication. Decoy receptor for CCR5
Nanomedecine - Just accepted for publication. Decoy receptor for CCR5
 
GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages
GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages  GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages
GPBAR1 (TGR5) regulates il 10 production from intestinal macrophages
 
Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1
Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1
Digestive Disease Week 2017 Discovery of dual LXR/GPBAR1
 
Digestive Disease Week 2017 The probiotic VSL#3 shows metabolic instability
Digestive Disease Week 2017 The probiotic VSL#3   shows metabolic instability Digestive Disease Week 2017 The probiotic VSL#3   shows metabolic instability
Digestive Disease Week 2017 The probiotic VSL#3 shows metabolic instability
 
Digestive Disease Week 2017 BAR704 reduces liver fibrosis
Digestive  Disease  Week 2017    BAR704   reduces liver fibrosisDigestive  Disease  Week 2017    BAR704   reduces liver fibrosis
Digestive Disease Week 2017 BAR704 reduces liver fibrosis
 
BAR501 a selective TGR5 ligand attenuates NASH
BAR501 a selective TGR5 ligand attenuates NASHBAR501 a selective TGR5 ligand attenuates NASH
BAR501 a selective TGR5 ligand attenuates NASH
 
NAFLD/NASH - 3 febbraio 2017-
NAFLD/NASH - 3  febbraio 2017-NAFLD/NASH - 3  febbraio 2017-
NAFLD/NASH - 3 febbraio 2017-
 
New official web site
New  official web siteNew  official web site
New official web site
 
Tgr5 and gastric cancer ddw2016
Tgr5 and gastric cancer  ddw2016Tgr5 and gastric cancer  ddw2016
Tgr5 and gastric cancer ddw2016
 
Bar501 and inflammation ddw 2016
Bar501 and inflammation ddw 2016Bar501 and inflammation ddw 2016
Bar501 and inflammation ddw 2016
 
Shp and liver fibrosis ddw 2016
Shp and liver fibrosis  ddw 2016Shp and liver fibrosis  ddw 2016
Shp and liver fibrosis ddw 2016
 
Ccr5 and colitis ddw 2016
Ccr5 and  colitis ddw 2016Ccr5 and  colitis ddw 2016
Ccr5 and colitis ddw 2016
 
BILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONS
BILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONSBILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONS
BILE ACID ACTIVATED RECEPTORS: FROM MEDICINAL CHEMISTRY TO CLINICAL APPLICATIONS
 
Research gate fiorucci citations
Research gate fiorucci citationsResearch gate fiorucci citations
Research gate fiorucci citations
 
Update emorragie digestive 2015
Update emorragie digestive  2015Update emorragie digestive  2015
Update emorragie digestive 2015
 
Nanotechnology update A seminar by Prof. Tatiana Tennikova
Nanotechnology update A seminar by Prof. Tatiana TennikovaNanotechnology update A seminar by Prof. Tatiana Tennikova
Nanotechnology update A seminar by Prof. Tatiana Tennikova
 
Trends in Molecular Medicine
Trends in Molecular Medicine Trends in Molecular Medicine
Trends in Molecular Medicine
 
Fiorucci’s lab sci report 2015
Fiorucci’s lab sci report 2015Fiorucci’s lab sci report 2015
Fiorucci’s lab sci report 2015
 
Expert opinion on therapeutic patent
Expert opinion on  therapeutic patentExpert opinion on  therapeutic patent
Expert opinion on therapeutic patent
 

Dernier

MYCOBACTERIES 2019hhhhhhhhhhhhhhhhhhhhh
MYCOBACTERIES  2019hhhhhhhhhhhhhhhhhhhhhMYCOBACTERIES  2019hhhhhhhhhhhhhhhhhhhhh
MYCOBACTERIES 2019hhhhhhhhhhhhhhhhhhhhhorthopediedentofacia
 
PRESERVATIFS MASCULIN ET FEMININ ok.pptx
PRESERVATIFS MASCULIN ET FEMININ ok.pptxPRESERVATIFS MASCULIN ET FEMININ ok.pptx
PRESERVATIFS MASCULIN ET FEMININ ok.pptxOuedraogoSoumaila3
 
cardiac manifestations in auto-immune diseases by Dr Silini.pptx
cardiac manifestations in auto-immune diseases by Dr Silini.pptxcardiac manifestations in auto-immune diseases by Dr Silini.pptx
cardiac manifestations in auto-immune diseases by Dr Silini.pptxsilinianfel
 
Souffrance fœtale aigue ou asphyxie périnatale
Souffrance fœtale aigue ou asphyxie périnataleSouffrance fœtale aigue ou asphyxie périnatale
Souffrance fœtale aigue ou asphyxie périnataleabedelazizkaraa
 
Brevets et innovation contre le cancer -
Brevets et innovation contre le cancer -Brevets et innovation contre le cancer -
Brevets et innovation contre le cancer -benj_2
 
CAT devant une Thrombose veineuse superficielle .pptx
CAT devant une Thrombose veineuse superficielle .pptxCAT devant une Thrombose veineuse superficielle .pptx
CAT devant une Thrombose veineuse superficielle .pptxsilinianfel
 

Dernier (6)

MYCOBACTERIES 2019hhhhhhhhhhhhhhhhhhhhh
MYCOBACTERIES  2019hhhhhhhhhhhhhhhhhhhhhMYCOBACTERIES  2019hhhhhhhhhhhhhhhhhhhhh
MYCOBACTERIES 2019hhhhhhhhhhhhhhhhhhhhh
 
PRESERVATIFS MASCULIN ET FEMININ ok.pptx
PRESERVATIFS MASCULIN ET FEMININ ok.pptxPRESERVATIFS MASCULIN ET FEMININ ok.pptx
PRESERVATIFS MASCULIN ET FEMININ ok.pptx
 
cardiac manifestations in auto-immune diseases by Dr Silini.pptx
cardiac manifestations in auto-immune diseases by Dr Silini.pptxcardiac manifestations in auto-immune diseases by Dr Silini.pptx
cardiac manifestations in auto-immune diseases by Dr Silini.pptx
 
Souffrance fœtale aigue ou asphyxie périnatale
Souffrance fœtale aigue ou asphyxie périnataleSouffrance fœtale aigue ou asphyxie périnatale
Souffrance fœtale aigue ou asphyxie périnatale
 
Brevets et innovation contre le cancer -
Brevets et innovation contre le cancer -Brevets et innovation contre le cancer -
Brevets et innovation contre le cancer -
 
CAT devant une Thrombose veineuse superficielle .pptx
CAT devant une Thrombose veineuse superficielle .pptxCAT devant une Thrombose veineuse superficielle .pptx
CAT devant une Thrombose veineuse superficielle .pptx
 

Prof Stefano Fiorucci - The nuclear receptor superfamily

  • 1. The nuclear receptor superfamily Mangelsdorf et al, (1995) Cell 83:835-839
  • 2. Domain structure of nuclear hormone receptors Gronemeyer et al, (2004) Nat Rev Drug Discov 3:950-964 Mangelsdorf et al, (1995) Cell 83:835-839
  • 3. Mode of action of nuclear receptors (NRs) Gronemeyer et al, (2004) Nat Rev Drug Discov 3:950-964
  • 4. Nuclear Receptors tissue distribution CNS Endocrine GI tract Adipose Immune Reproductive Respiratory Structural FXR • • ••• • • • • • CAR • • ••• • • • • • PXR • • ••• • • • • • VDR • •• ••• • • • • •• LXR • • ••• ••• • • •• • PPARγ • • •• ••• • • • • PPARα • • ••• •••• • • •• • PPAR β/δ •• •• ••• •• • •• •• •• GR •••• • •••• ••• ••• •• ••• ••• TRα ••• • • • • • • • TRβ ••• •• ••• •• • •• •• •• RXRα •• •• •• •• • •• •• •• AR • •• • • • ••• • • CNS: Central Nervous System; GI: gastrointestinal NURSA
  • 6. FXR VDR NURSA
  • 7. CAR PXR NURSA
  • 8. Nuclear Receptors in immune system   PPARγ FXR PXR CAR VDR WholeBlood + +  + + +++ CD14 Monocytes  +  +   +   +  +++++  CD33 Myeloid  +  +   +  + +++++  CD56 NKCells  +  +   +   +  +++  CD4 Tcells  +  +   +  +  +++  CD8 Tcells  +  +   +  +  +++  BDCA4 Dentritic Cells  +  +   +  +  +++  CD19 BCells.neg.sel.  +  +   +  +  +++  X721 B lymphoblasts  +  +   +  +  +++  CD105 Endothelial  +  +   +  +  +++  CD34  +  +   +  +  +++  Bile acids activated receptors BioGPS The gene portal Hub
  • 9. Nuclear receptors versus inflammation:  mechanisms of transrepression-I  Pascual G, Glass CK Trends Endocrinol Metab. 2006 Oct;17(8):321-7. 
  • 10. Nuclear receptors versus inflammation: mechanisms of transrepression-II Pascual G, Glass CK Trends Endocrinol Metab. 2006 Oct;17(8):321-7.