Structure-function relationships of nuclear receptors and their co-regulators

Presentation
Projects
Members
Collaborations
Teams
Publications

Structure-function relationships of nuclear receptors and their co-regulators

Numerical simulation studies of the structural dynamics of nuclear receptors

SUBGROUP LEADER

Nuclear receptors are ligand-regulated transcription factors that control nearly all aspects of human physiology. We are studying several members of the nuclear receptor family including the vitamin D receptor (VDR), peroxisome-activated receptors (PPARs) and retinoid receptors (RARs and RXRs). The objective of our research is to understand how the activation and repression of nuclear receptor transcription are regulated at the structural and molecular level using X-ray crystallography and other structural, biophysical and cellular methods.

Current projects

Structural studies of nuclear receptors-coregulators complexes
Mechanisms involved in the deregulation of nuclear receptor signaling
Structural pharmacology

Members

Collaborations and networks

D. Metzger and G. Laverny (IGBMC)
A. Mourino (University Santiago de Compostella, Espagne)
I. Bernard-Pierrot and F. Radvanyi (Institut Curie, Paris)
G. Guichard (IECB Bordeaux)
V. Torbeev (ESBS, Strasbourg)
B. Kieffer and C. Deville (IGBMC)

Teams

Chemical biophysics of transcriptional signaling
Team Leader : Annick DEJAEGERE
Department : Integrated structural biology

Publications

2010
- Design and synthesis of active vitamin D analogs
  - Silvina Eduardo-Canosa
  - Ramón Fraga
  - Rita Sigüeiro
  - Maria Marco
  - Natacha Rochel
  - Dino Moras
  - Antonio Mouriño
  Journal of Steroid Biochemistry and Molecular Biology ; Volume: 121 ; Page: 7-12
  HAL DOI
2009
- Silicon analogues of the RXR-selective retinoid agonist SR11237 (BMS649): chemistry and biology.
  - W Peter Lippert
  - Christian Burschka
  - Kathrin Götz
  - Martin Kaupp
  - Diana Ivanova
  - Claudine Gaudon
  - Yoshiteru Sato
  - Pierre Antony
  - Natacha Rochel
  - Dino Moras
  - Hinrich Gronemeyer
  - Reinhold Tacke
  ChemMedChem ; Volume: 4 ; Page: 1143-52
  HAL DOI
- A set of baculovirus transfer vectors for screening of affinity tags and parallel expression strategies.
  - Wassim Abdulrahman
  - Muriel Uhring
  - Isabelle Kolb-Cheynel
  - Jean-Marie Garnier
  - Dino Moras
  - Natacha Rochel
  - Didier Busso
  - Arnaud Poterszman
  Analytical Biochemistry ; Volume: 385 ; Page: 383-5
  HAL DOI
- Structural and Functional Insights into the Ligand-binding Domain of a Nonduplicated Retinoid X Nuclear Receptor from the Invertebrate Chordate Amphioxus.
  - Giuseppe D. Tocchini-Valentini
  - Natacha Rochel
  - Hector Escriva
  - Pierre Germain
  - Carole Peluso-Iltis
  - Mathilde Paris
  - Sarah Sanglier-Cianferani
  - Alain van Dorsselaer
  - Dino Moras
  - Vincent Laudet
  Journal of Biological Chemistry ; Volume: 284 ; Page: 1938-1948
  HAL DOI
2008
- Superagonistic fluorinated vitamin D3 analogs stabilize helix 12 of the vitamin D receptor.
  - Guy Eelen
  - Noelia Valle
  - Yoshiteru Sato
  - Natacha Rochel
  - Lieve Verlinden
  - Pierre de Clercq
  - Dino Moras
  - Roger Bouillon
  - Alberto Muñoz
  - Annemieke Verstuyf
  Chemistry & Biology / Chemistry and Biology; CHEMISTRY & BIOLOGY ; Volume: 15 ; Page: 1029-34
  HAL DOI
- Communication between the ERRalpha homodimer interface and the PGC-1alpha binding surface via the helix 8-9 loop.
  - Holger Greschik
  - Magnus Althage
  - Ralf Flaig
  - Yoshiteru Sato
  - Virginie Chavant
  - Carole Peluso-Iltis
  - Laurence Choulier
  - Philippe Cronet
  - Natacha Rochel
  - Roland Schüle
  - Per-Erik Strömstedt
  - Dino Moras
  Journal of Biological Chemistry ; Volume: 283 ; Page: 20220-30
  HAL DOI
- Communication between the ERRα Homodimer Interface and the PGC-1α Binding Surface via the Helix 8–9 Loop
  - Holger Greschik
  - Magnus Althage
  - Ralf Flaig
  - Yoshiteru Sato
  - Virginie Chavant
  - Carole Peluso-Iltis
  - Laurence Choulier
  - Philippe Cronet
  - Natacha Rochel
  - Roland Schüle
  - Per-Erik Strömstedt
  - Dino Moras
  Journal of Biological Chemistry ; Volume: 283 ; Page: 20220-20230
  HAL DOI
- Structure-based design of a superagonist ligand for the vitamin D nuclear receptor.
  - Shinji Hourai
  - Luis Cezar Rodrigues
  - Pierre Antony
  - Bernardo Reina-San-Martin
  - Fabrice Ciesielski
  - Benjamin Claude Magnier
  - Kristina Schoonjans
  - Antonio Mouriño
  - Natacha Rochel
  - Dino Moras
  Chemistry & Biology / Chemistry and Biology; CHEMISTRY & BIOLOGY ; Volume: 15 ; Page: 383-92
  HAL DOI
2007
- Silicon analogues of the retinoid agonists TTNPB and 3-methyl-TTNPB, disila-TTNPB and disila-3-methyl-TTNPB: chemistry and biology.
  - Matthias W Büttner
  - Christian Burschka
  - Jürgen O Daiss
  - Diana Ivanova
  - Natacha Rochel
  - Sabrina Kammerer
  - Carole Peluso-Iltis
  - Audrey Bindler
  - Claudine Gaudon
  - Pierre Germain
  - Dino Moras
  - Hinrich Gronemeyer
  - Reinhold Tacke
  ChemBioChem ; Volume: 8 ; Page: 1688-99
  HAL DOI
- Crystal structure of the vitamin D nuclear receptor ligand binding domain in complex with a locked side chain analog of calcitriol.
  - Natacha Rochel
  - Shinji Hourai
  - Xenxo Pérez-García
  - Antonio Rumbo
  - Antonio Mourino
  - Dino Moras
  Archives of Biochemistry and Biophysics ; Volume: 460 ; Page: 172-6
  HAL DOI