Integrative Biophysics of Membranes

6SSQ 6STI 6I65 6I66
X-RAY (2019) 2.30 Ang. X-RAY (2019) 1.89 Ang. X-RAY (2018) 1.50 Ang. X-RAY (2018) 1.60 Ang.
CRYSTAL STRUCTURE OF RARBETA LBD IN COMPLEX WITH LG 100754 CRYSTAL STRUCTURE OF RXRALPHA LBD IN COMPLEX WITH LG 100754 AND A COACTIVATOR PEPTIDE CRYSTAL STRUCTURE OF HUMAN ERRG LBD IN COMPLEX WITH 4-ISO-PROPYLPHENOL CRYSTAL STRUCTURE OF HUMAN ERRG LBD IN COMPLEX WITH 4-SEC-BUTYLPHENOL
A.LE MAIRE, C.TEYSSIER, P.GERMAIN, W.BOURGUET A.LE MAIRE, C.TEYSSIER, P.GERMAIN, W.BOURGUET V.DELFOSSE, P.BLANC, W.BOURGUET V.DELFOSSE, P.BLANC, W.BOURGUET
6I63 6I61 6I62 6HN6
X-RAY (2018) 2.23 Ang. X-RAY (2018) 1.65 Ang. X-RAY (2018) 1.65 Ang. X-RAY (2018) 2.71 Ang.
CRYSTAL STRUCTURE OF HUMAN ERRG LBD IN COMPLEX WITH BISPHENOL-A CRYSTAL STRUCTURE OF HUMAN ERRG LBD IN COMPLEX WITH BISPHENOL-B CRYSTAL STRUCTURE OF HUMAN ERRG LBD IN COMPLEX WITH HPTE A REVISITED VERSION OF THE APO STRUCTURE OF THE LIGAND-BINDING DOMAIN OF THE HUMAN NUCLEAR RECEPTOR RXR-ALPHA
V.DELFOSSE, P.BLANC, W.BOURGUET V.DELFOSSE, P.BLANC, W.BOURGUET V.DELFOSSE, P.BLANC, W.BOURGUET J.EBERHARDT, A.G.MCEWEN, W.BOURGUET, D.MORAS, A.DEJAEGERE
6I67 6I64 6AN1 5JMM
X-RAY (2018) 1.75 Ang. X-RAY (2018) 1.91 Ang. X-RAY (2017) 2.69 Ang. X-RAY (2016) 2.10 Ang.
CRYSTAL STRUCTURE OF HUMAN ERRG LBD IN COMPLEX WITH TETRAHYDRO-2- NAPHTOL CRYSTAL STRUCTURE OF HUMAN ERRG LBD IN COMPLEX WITH BISPHENOL-E CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN PPARGAMMA LBD AND THE LIGAND AM-879 CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH BIOCHANIN A
V.DELFOSSE, P.BLANC, W.BOURGUET V.DELFOSSE, P.BLANC, W.BOURGUET H.VERAS, A.C.FIGUEIRA, A.LE MAIRE V.DELFOSSE, W.BOURGUET
5HT6 4TUZ 4TV1 4XAO
X-RAY (2016) 2.09 Ang. X-RAY (2014) 1.90 Ang. X-RAY (2014) 1.85 Ang. X-RAY (2014) 2.58 Ang.
CRYSTAL STRUCTURE OF THE SET DOMAIN OF THE HUMAN MLL5 METHYLTRANSFERAS-E CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH ALPHA-ZEARALENOL CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH PROPYLPARABEN CRYSTAL STRUCTURE OF THE HPXR-LBD OBTAINED IN PRESENCE OF THE PESTICIDE TRANS-NONACHLOR
A.LE MAIRE, S.MAS-Y-MAS, C.DUMAS, A.LEBEDEV V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, T.HUET, W.BOURGUET
4X1G 4PH7 4X1F 4MGA
X-RAY (2014) 2.25 Ang. X-RAY (2014) 2.55 Ang. X-RAY (2014) 2.00 Ang. X-RAY (2013) 1.80 Ang.
CRYSTAL STRUCTURE OF THE HPXR-LBD IN COMPLEX WITH THE SYNTHETIC ESTROGEN 17ALPHA-ETHINYLESTRADIO-L AND THE PESTICIDE TRANS-NONACHLOR STRUCTURE OF OSH6P IN COMPLEX WITH PHOSPHATIDYLINOS-ITOL 4-PHOSPHATE CRYSTAL STRUCTURE OF THE HPXR-LBD IN COMPLEX WITH THE SYNTHETIC ESTROGEN 17ALPHA-ETHINYLESTRADIO-L CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH 4-TERT- OCTYLPHENOL
V.DELFOSSE, T.HUET, W.BOURGUET V.DELFOSSE, J.MOSER VON FILSECK, B.ANTONNY, W.BOURGUET, G.DRIN V.DELFOSSE, T.HUET, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET
4MG9 4MG7 4JYH 4MGD
X-RAY (2013) 2.00 Ang. X-RAY (2013) 2.15 Ang. X-RAY (2013) 2.60 Ang. X-RAY (2013) 1.90 Ang.
CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH BUTYLPARABEN CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH FERUTININE CRYSTAL STRUCTURE OF RARBETA LBD IN COMPLEX WITH SELECTIVE AGONIST BMS948 [4-{[(8-PHENYLNAPHTHALE-N-2-YL)CARBONYL]AMI-NO}BENZOIC ACID] CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH HPTE
V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET E.K.NADENDLA, C.TEYSSIER, P.GERMAIN, V.DELFOSSE, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET
4JYG 4MG6 4MGC 4MG8
X-RAY (2013) 2.35 Ang. X-RAY (2013) 2.10 Ang. X-RAY (2013) 2.15 Ang. X-RAY (2013) 1.85 Ang.
CRYSTAL STRUCTURE OF RARBETA LBD IN COMPLEX WITH AGONIST BMS411 [4- {[(5,5-DIMETHYL-8-PHENYL-5,6-DIHYDRONAPHTHAL-EN-2-YL) CARBONYL]AMINO}B-ENZOIC ACID] CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH BENZYLBUTYLPHTAL-ATE CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH BENZOPHENONE-2 CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH ALPHA-ZEARALANOL
E.K.NADENDLA, C.TEYSSIER, P.GERMAIN, V.DELFOSSE, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET
4MGB 4MG5 4JYI 4DM8
X-RAY (2013) 1.85 Ang. X-RAY (2013) 2.05 Ang. X-RAY (2013) 1.90 Ang. X-RAY (2012) 2.30 Ang.
CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH TCBPA CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH CHLORDECONE CRYSTAL STRUCTURE OF RARBETA LBD IN COMPLEX WITH SELECTIVE PARTIAL AGONIST BMS641 [3-CHLORO-4-[(E)-2-(5,5-DIMETHYL-8-PHENYL-5,6- DIHYDRONAPHTHALE-N-2-YL)ETHENYL]BENZ-OIC ACID] CRYSTAL STRUCTURE OF RARB LBD IN COMPLEX WITH 9CIS RETINOIC ACID
V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET E.K.NADENDLA, C.TEYSSIER, P.GERMAIN, V.DELFOSSE, W.BOURGUET J.OSZ, Y.BR LIVET, C.PELUSO-ILTIS, V.CURA, S.EILER, M.RUFF, W.BOURGUET, N.ROCHEL, D.MORAS
4DM6 4DMA 3UUD 3UUA
X-RAY (2012) 1.90 Ang. X-RAY (2012) 2.30 Ang. X-RAY (2011) 1.60 Ang. X-RAY (2011) 2.05 Ang.
CRYSTAL STRUCTURE OF RARB LBD HOMODIMER IN COMPLEX WITH TTNPB CRYSTAL STRUCTURE OF ERA LBD IN COMPLEX WITH RU100132 CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH ESTRADIOL CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH BISPHENOL-AF
J.OSZ, Y.BRELIVET, C.PELUSO-ILTIS, V.CURA, S.EILER, M.RUFF, W.BOURGUET, N.ROCHEL, D.MORAS J.OSZ, Y.BRELIVET, C.PELUSO-ILTIS, V.CURA, S.EILER, M.RUFF, W.BOURGUET, N.ROCHEL, D.MORAS V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET
3UU7 3UUC 3SPW 3PO9
X-RAY (2011) 2.20 Ang. X-RAY (2011) 2.10 Ang. X-RAY (2011) 2.60 Ang. X-RAY (2010) 2.35 Ang.
CRYSTAL STRUCTURE OF HERA-LBD (Y537S) IN COMPLEX WITH BISPHENOL-A CRYSTAL STRUCTURE OF HERA-LBD (WT) IN COMPLEX WITH BISPHENOL-C STRUCTURE OF OSH4P/KES1P IN COMPLEX WITH PHOSPHATIDYLINOS-ITOL 4- PHOSPHATE CRYSTAL STRUCTURE OF PPARGAMMA LIGAND BINDING DOMAIN IN COMPLEX WITH TRIPROPYLTIN
V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.GRIMALDI, W.BOURGUET V.DELFOSSE, M.DE SAINT-JEAN, D.DOUGUET, B.ANTONNY, G.DRIN, W.BOURGUET A.LE MAIRE, W.BOURGUET
3OSI 3OSW 3PBA 3KWY
X-RAY (2010) 2.70 Ang. X-RAY (2010) 2.55 Ang. X-RAY (2010) 2.30 Ang. X-RAY (2009) 2.30 Ang.
CRYSTAL STRUCTURE OF PPARGAMMA LIGAND BINDING DOMAIN IN COMPLEX WITH TETRACHLORO-BISPHENOL A (TCBPA) CRYSTAL STRUCTURE OF PPARGAMMA LIGAND BINDING DOMAIN IN COMPLEX WITH TETRABROMO-BISPHENOL A (TBBPA) CRYSTAL STRUCTURE OF PPARGAMMA LIGAND BINDING DOMAIN IN COMPLEX WITH MONOSULFATE TETRABROMO-BISPHENOL A (MONOTBBPA) CRYSTAL STRUCTURE OF RXRALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH TRIPHENYLTIN AND A COACTIVATOR FRAGMENT
A.LE MAIRE, W.BOURGUET A.LE MAIRE, W.BOURGUET A.LE MAIRE, W.BOURGUET A.LE MAIRE, W.BOURGUET
3FUG 3KMZ 3KMR 3E94
X-RAY (2009) 2.00 Ang. X-RAY (2009) 2.10 Ang. X-RAY (2009) 1.80 Ang. X-RAY (2008) 1.90 Ang.
CRYSTAL STRUCTURE OF THE RETINOID X RECEPTOR LIGAND BINDING DOMAIN BOUND TO THE SYNTHETIC AGONIST 3-[4-HYDROXY-3-(3,5, 5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRONAPHT-HALEN-2-YL)- PHENYL]ACRYLIC ACID CRYSTAL STRUCTURE OF RARALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH THE INVERSE AGONIST BMS493 AND A COREPRESSOR FRAGMENT CRYSTAL STRUCTURE OF RARALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH AN AGONIST LIGAND (AM580) AND A COACTIVATOR FRAGMENT CRYSTAL STRUCTURE OF RXRALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH TRIBUTYLTIN AND A COACTIVATOR FRAGMENT
W.BOURGUET W.BOURGUET, A.LE MAIRE W.BOURGUET, C.TEYSSIER W.BOURGUET, A.LE MAIRE
2V1N 2P1T 2P1U 2P1V
SOLUTION NMR (2007) X-RAY (2007) 1.80 Ang. X-RAY (2007) 2.20 Ang. X-RAY (2007) 2.20 Ang.
SOLUTION STRUCTURE OF THE REGION 51-160 OF HUMAN KIN17 REVEALS A WINGED HELIX FOLD CRYSTAL STRUCTURE OF THE LIGAND BINDING DOMAIN OF THE RETINOID X RECEPTOR ALPHA IN COMPLEX WITH 3-(2'-METHOXY)- TETRAHYDRONAPHTY-L CINNAMIC ACID AND A FRAGMENT OF THE COACTIVATOR TIF-2 CRYSTAL STRUCTURE OF THE LIGAND BINDING DOMAIN OF THE RETINOID X RECEPTOR ALPHA IN COMPLEX WITH 3-(2'-ETHOXY)- TETRAHYDRONAPHTY-L CINNAMIC ACID AND A FRAGMENT OF THE COACTIVATOR TIF-2 CRYSTAL STRUCTURE OF THE LIGAND BINDING DOMAIN OF THE RETINOID X RECEPTOR ALPHA IN COMPLEX WITH 3-(2'-PROPOXY)- TETRAHYDRONAPHTY-L CINNAMIC ACID AND A FRAGMENT OF THE COACTIVATOR TIF-2
L.CARLIER, A.LE MAIRE, M.GONDRY, L.GUILHAUDIS, I.MILAZZO, D.DAVOUST, J.COUPRIE, B.GILQUIN, S.ZINN-JUSTIN W.BOURGUET, V.NAHOUM W.BOURGUET, V.NAHOUM W.BOURGUET, V.NAHOUM
2CKK 1XAP 1XDK 1S1N
X-RAY (2006) 1.45 Ang. X-RAY (2004) 2.10 Ang. X-RAY (2004) 2.90 Ang. SOLUTION NMR (2004)
HIGH RESOLUTION CRYSTAL STRUCTURE OF THE HUMAN KIN17 C-TERMINAL DOMAIN CONTAINING A KOW MOTIF STRUCTURE OF THE LIGAND BINDING DOMAIN OF THE RETINOIC ACID RECEPTOR BETA CRYSTAL STRUCTURE OF THE RARBETA/RXRALPHA LIGAND BINDING DOMAIN HETERODIMER IN COMPLEX WITH 9-CIS RETINOIC ACID AND A FRAGMENT OF THE TRAP220 COACTIVATOR SH3 DOMAIN OF HUMAN NEPHROCYSTIN
A.LE MAIRE, M.SCHILTZ, G.PINON-LATAILLADE, E.STURA, J.COUPRIE, M.GONDRY, J.ANGULO-MORA, S.ZINN-JUSTIN P.GERMAIN, S.KAMMERER, C.PELUSO-ILTIS, D.TORTOLANI, F.C.ZUSI, J.STARRETT, P.LAPOINTE, J.P.DARIS, A.MARINIER, A.R.DE LERA, N.ROCHEL, H.GRONEMEYER V.POGENBERG, J.F.GUICHOU, V.VIVAT-HANNAH, S.KAMMERER, E.PEREZ, P.GERMAIN, A.R.DE LERA, H.GRONEMEYER, C.A.ROYER, W.BOURGUET A.LE MAIRE, T.WEBER, S.SAUNIER, C.ANTIGNAC, A.DUCRUIX, F.DARDEL
1KV6 1C10 1C1M 1DKF
X-RAY (2002) 2.70 Ang. X-RAY (1999) 2.03 Ang. X-RAY (1999) 2.20 Ang. X-RAY (1999) 2.50 Ang.
X-RAY STRUCTURE OF THE ORPHAN NUCLEAR RECEPTOR ERR3 LIGAND- BINDING DOMAIN IN THE CONSTITUTIVELY ACTIVE CONFORMATION CRYSTAL STRUCTURE OF HEW LYSOZYME UNDER PRESSURE OF XENON (8 BAR) PORCINE ELASTASE UNDER XENON PRESSURE (8 BAR) CRYSTAL STRUCTURE OF A HETERODIMERIC COMPLEX OF RAR AND RXR LIGAND- BINDING DOMAINS
H.GRESCHIK, J.-M.WURTZ, S.SANGLIER, W.BOURGUET, A.VAN DORSSELAER, D.MORAS, J.-P.RENAUD, STRUCTURAL PROTEOMICS IN EUROPE (SPINE) T.PRANGE, M.SCHILTZ, L.PERNOT, N.COLLOC'H, S.LONGHI, W.BOURGUET, R.FOURME T.PRANGE, M.SCHILTZ, L.PERNOT, N.COLLOC'H, S.LONGHI, W.BOURGUET, R.FOURME W.BOURGUET, V.VIVAT, J.M.WURTZ, P.CHAMBON, H.GRONEMEYER, D.MORAS, STRUCTURAL PROTEOMICS IN EUROPE (SPINE)
1QTK
X-RAY (1999) 2.03 Ang.
CRYSTAL STRUCTURE OF HEW LYSOZYME UNDER PRESSURE OF KRYPTON (55 BAR)
T.PRANGE, M.SCHILTZ, L.PERNOT, N.COLLOC'H, S.LONGHI, W.BOURGUET, R.FOURME

Presentation

Team leader William Bourguet and Albane Le Maire

TeamA5 250121 small

Nuclear receptors (NRs) are master regulators of gene expression in humans. Their biological functions depend on their ability to bind other molecules such as ligands (hormones, vitamins, etc.), DNA and transcriptional coregulators. They are also the primary targets of many environmental endocrine disruptors that mimic the action of endogenous ligands and cause a wide range of diseases. A major interest of the group is to reach a detailed understanding of the mechanisms involved in the (de)regulation of nuclear receptor signaling.

A5 presentation

The research work of the team is organized into 5 major thematic areas:

  1. Mechanisms of gene regulation by nuclear receptors
  2. Novel nuclear receptor-based therapeutic strategies
  3. Nuclear receptors as targets of environmental endocrine disruptors
  4. Structure and function of the aryl hydrocarbon receptor (ATIP-Avenir Gruszczyk)
  5. Lipids homeostasis

 

Financial support:

A5 presentation support

 

 

Scientific awards:

 A5 awards

Theme 4: Structure and function of the aryl hydrocarbon receptor (ATIP-Avenir)

J Gruszczyk

Each day our body comes into close contact with myriads of various chemical substances also known as xenobiotics. Since some of them can trigger long-lasting effects that can potentially be quite harmful, the impact they have on our organism should not be overlooked. Understanding the processes governing recognition, metabolism and removal of foreign substances is critical to fully comprehend their toxicity. Aryl hydrocarbon receptor (AHR) is one of the crucial chemosensory proteins involved in the metabolism of many pollutants. AHR binds a selection of xenobiotics and regulates expression of numerous genes involved in their detoxification. So far, we are lacking the in-depth structural and biochemical analyses of this essential signalling pathway. Most importantly, no high-resolution structure has been reported for the region encompassing ligand-binding domain of AHR. Therefore, the details of the ligand-dependent regulation of the protein remain obscure and our grasp of the underlying mechanism is very limited.

A5 theme4 new

The canonical AHR activation pathway. The unliganded AHR resides in the cytoplasm in the form of the multiprotein complex including Hsp90, XAP2 and p23. Upon ligand binding, AHR undergoes translocation into cell nucleus where the chaperone complex is displaced by AHR-nuclear translocator protein (ARNT). The AHR-ARNT heterodimer recognises a dioxin-responsive element (DRE) with the consensus DNA sequence 5'T/G/TCGTGA/CG/TA/T-3' localised in the promoter region of many genes. AHR and ARNT can recruit different coactivator proteins, thus enabling efficient gene transcription. The best studied target gene of AHR is cytochrome P450 1A1 (CYP1A1). CYP1A1 is an aryl hydrocarbon hydroxylase involved in biotransformation and metabolism of multiple chemical pollutants. RNA Pol II - RNA polymerase II.

Our project aims to structurally and biochemically characterise particular steps of the AHR-dependent signalling pathway. We would like to focus our attention not only on understanding how a single receptor is capable of binding many various chemical compounds but also on the exact role of its different protein partners. We hope that by methodically dissecting particular steps of this signalling pathway we will be able to provide a detailed molecular mechanism underlying the processes of detection and detoxification of chemical pollutants in our body and, as a result, to shed more light on the essential aspect of human physiology..

Principal collaborations: Ch Bechara (IGF Montpellier), Ch Savva (Univeristy of Leicester), M Amblard (IBMM Montpellier), P Balaguer (IRCM Montpellier)

 

Financial support:

A5 theme4 support

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