W. Bourguet

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Modulation of RXR function through ligand design.

William Bourguet, Angel R de Lera, Hinrich Gronemeyer, 2012, Biochimica et biophysica acta.

Combining 'dry' co-crystallization and in situ diffraction to facilitate ligand screening by X-ray crystallography.

G. Labesse, J. Ferrer, F. Hoh, 2015, Acta crystallographica. Section D, Biological crystallography.

Activation of RXR–PPAR heterodimers by organotin environmental endocrine disruptors

William Bourguet, Marina Grimaldi, W. Bourguet, 2009, EMBO reports.

Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications.

H. Gronemeyer, W. Bourguet, P. Germain, 2000, Trends in pharmacological sciences.

Interplay of Protein Disorder in Retinoic Acid Receptor Heterodimer and Its Corepressor Regulates Gene Expression.

Alessandro Barducci, Nathalie Sibille, Pau Bernadó, 2019, Structure.

A canonical structure for the ligand-binding domain of nuclear receptors

William Bourguet, Jean-Paul Renaud, Pierre Chambon, 1996, Nature Structural Biology.

The structure of Staphylococcus aureus epidermolytic toxin A, an atypic serine protease, at 1.7 A resolution.

B Chevrier, D. Moras, L. Mourey, 1997, Structure.

Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-α

William Bourguet, Pierre Chambon, Dino Moras, 1995, Nature.

Exploring hydrophobic sites in proteins with xenon or krypton

M Schiltz, N. Colloc'h, T. Prangé, 1998, Proteins.

Structural insights into the cooperative interaction of the intrinsically disordered co-activator TIF2 with retinoic acid receptor heterodimer (RXR/RAR)

João E. Carvalho, P. Bernadó, N. Sibille, 2020, bioRxiv.

Structural and functional evidences for the interactions between nuclear hormone receptors and endocrine disruptors at low doses.

W. Bourguet, V. Delfosse, Marina Grimaldi, 2017, Comptes rendus biologies.

Reporter Cell Lines for the Characterization of the Interactions between Human Nuclear Receptors and Endocrine Disruptors

William Bourguet, Marina Grimaldi, W. Bourguet, 2015, Front. Endocrinol..

A Comparative Study of Human and Zebrafish Pregnane X Receptor Activities of Pesticides and Steroids Using In Vitro Reporter Gene Assays

W. Bourguet, Marina Grimaldi, P. Balaguer, 2021, Frontiers in Endocrinology.

Discovery of a Highly Active Ligand of Human Pregnane X Receptor: A Case Study from Pharmacophore Modeling and Virtual Screening to “In Vivo” Biological Activity

Virginie Nahoum, William Bourguet, Jean-François Guichou, 2007, Molecular Pharmacology.

Mechanistic insights into the synergistic activation of the RXR–PXR heterodimer by endocrine disruptor mixtures

S. Cianférani, D. Harrus, B. Demeneix, 2020, Proceedings of the National Academy of Sciences.

The GOLIATH Project: Towards an Internationally Harmonised Approach for Testing Metabolism Disrupting Compounds

D. Zalko, F. Jourdan, B. Fromenty, 2020, International journal of molecular sciences.

Ligand- and DNA-induced dissociation of RXR tetramers.

P. Chambon, H. Gronemeyer, W. Bourguet, 1998, Journal of molecular biology.

High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride as a Selective and Competitive Antagonist of the Androgen Receptor

C. Gongora, P. Pourquier, W. Bourguet, 2020, Cells.

Evolutionary diversification of retinoic acid receptor ligand-binding pocket structure by molecular tinkering

V. Laudet, S. Kuraku, W. Bourguet, 2016, Royal Society Open Science.

Heterodimeric complex of RAR and RXR nuclear receptor ligand-binding domains: purification, crystallization, and preliminary X-ray diffraction analysis.

P. Chambon, H. Gronemeyer, D. Moras, 2000, Protein expression and purification.

Sequences in the ligand-binding domains of the human androgen and progesterone receptors which determine their distinct ligand identities.

H. Gronemeyer, J. Wurtz, W. Bourguet, 1997, Journal of molecular endocrinology.

In Silico Predictions of Endocrine Disruptors Properties

G. Labesse, J. Pons, W. Bourguet, 2019, Endocrinology.

The ancestral retinoic acid receptor was a low-affinity sensor triggering neuronal differentiation

Jace W. Jones, P. Tomançak, V. Laudet, 2018, Science Advances.

The Human Mixed Lineage Leukemia 5 (MLL5), a Sequentially and Structurally Divergent SET Domain-Containing Protein with No Intrinsic Catalytic Activity

João E. Carvalho, L. Bird, C. Dumas, 2016, PloS one.

Functional analyses of phosphatidylserine/PI(4)P exchangers with diverse lipid species and membrane contexts set unanticipated rules on lipid transfer

G. Drin, W. Bourguet, V. Delfosse, 2021, bioRxiv.

Cryo-EM structure of the agonist-bound Hsp90-XAP2-AHR cytosolic complex

A. Barducci, Loïc GrandVuillemin, W. Bourguet, 2022, bioRxiv.

Peroxisome Proliferator-Activated Receptor γ Is a Target for Halogenated Analogs of Bisphenol A

D. Zalko, A. Riu, E. Perdu, 2011, Environmental health perspectives.

Human and zebrafish nuclear progesterone receptors are differently activated by manifold progestins.

W. Bourguet, F. Brion, P. Balaguer, 2020, Environmental science & technology.

Toxicant Actions: Mode of Action of Endocrine Disruptors

W. Bourguet, P. Balaguer, 2014 .

[Towards bisphenols without hormonal effects].

W. Bourguet, V. Delfosse, Marina Grimaldi, 2013, Medecine sciences : M/S.

Retinoid Receptors: Protein Structure, DNA Recognition and Structure-Function Relationships

D. Moras, W. Bourguet, 2015 .

Dimerization of nuclear receptors.

W. Bourguet, P. Germain, 2013, Methods in cell biology.

Peroxisome proliferator‐activated receptor gamma‐ligand‐binding domain mutations associated with familial partial lipodystrophy type 3 disrupt human trophoblast fusion and fibroblast migration

C. Vigouroux, W. Bourguet, S. Degrelle, 2020, Journal of cellular and molecular medicine.

Mechanisms of endocrine disruption through nuclear receptors and related pathways

W. Bourguet, V. Delfosse, P. Balaguer, 2019, Current Opinion in Endocrine and Metabolic Research.

Modulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers.

H. Gronemeyer, W. Bourguet, A. D. de Lera, 2009, Journal of medicinal chemistry.

Purification, functional characterization, and crystallization of the ligand binding domain of the retinoid X receptor.

P. Chambon, H. Gronemeyer, D. Moras, 1995, Protein expression and purification.

Structure of the third intracellular loop of the vasopressin V2 receptor and conformational changes upon binding to gC1qR.

R. Seyer, B. Mouillac, R. Rahmeh, 2009, Journal of molecular biology.

Nuclear receptor ligand-binding domains: reduction of helix H12 dynamics to favour crystallization.

Efrén Pérez, W. Bourguet, A. D. de Lera, 2008, Acta crystallographica. Section F, Structural biology and crystallization communications.

Androgen and estrogen receptors: potential of crystallography in the fight against cancer.

W. Bourguet, V. Nahoum, 2007, The international journal of biochemistry & cell biology.

A mollusk retinoic acid receptor (RAR) ortholog sheds light on the evolution of ligand binding.

Jace W. Jones, V. Laudet, M. Kane, 2014, Endocrinology.

2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors

B. Blumberg, W. Bourguet, A. Amato, 2022, bioRxiv.

A Novel Mutation in THRA Gene Associated With an Atypical Phenotype of Resistance to Thyroid Hormone.

G. Pinto, F. Savagner, W. Bourguet, 2015, The Journal of clinical endocrinology and metabolism.

Ligands and DNA in the allosteric control of retinoid receptors function.

N. Rochel, W. Bourguet, P. Germain, 2021, Essays in biochemistry.

Insights into the activation mechanism of human estrogen-related receptor γ by environmental endocrine disruptors

A. Barducci, W. Bourguet, V. Delfosse, 2019, Cellular and Molecular Life Sciences.

A unique secondary-structure switch controls constitutive gene repression by retinoic acid receptor

H. Gronemeyer, A. Lera, C. Royer, 2010, Nature Structural &Molecular Biology.

SMRTε, a corepressor variant, interacts with a restricted subset of nuclear receptors, including the retinoic acid receptors α and β

W. Bourguet, M. Goodson, M. Privalsky, 2012, Molecular and Cellular Endocrinology.

Structural basis for a molecular allosteric control mechanism of cofactor binding to nuclear receptors

D. Moras, N. Rochel, J. Ősz, 2012, Proceedings of the National Academy of Sciences.

Selectivity of natural, synthetic and environmental estrogens for zebrafish estrogen receptors.

J. Gustafsson, W. Bourguet, F. Brion, 2014, Toxicology and applied pharmacology.

Purification and crystallization of the heterodimeric complex of RARβ and RXRα ligand-binding domains in the active conformation

W. Bourguet, V. Pogenberg, J. Guichou, 2004 .

Separation of Retinoid X Receptor Homo- and Heterodimerization Functions

H. Gronemeyer, M. Gottardis, W. Bourguet, 2003, Molecular and Cellular Biology.

A mutation mimicking ligand‐induced conformational change yields a constitutive RXR that senses allosteric effects in heterodimers

P. Chambon, H. Gronemeyer, D. Moras, 1997, The EMBO journal.

Design of selective nuclear receptor modulators: RAR and RXR as a case study

Lucia Altucci, William Bourguet, Angel R. de Lera, 2007, Nature Reviews Drug Discovery.

Structural and mechanistic insights into bisphenols action provide guidelines for risk assessment and discovery of bisphenol A substitutes

Jean-Luc Pons, Gilles Labesse, William Bourguet, 2012, Proceedings of the National Academy of Sciences.

A structural perspective on nuclear receptors as targets of environmental compounds

W. Bourguet, V. Delfosse, P. Balaguer, 2014, Acta Pharmacologica Sinica.

Nuclear receptor profiling of bisphenol-A and its halogenated analogues.

William Bourguet, Marina Grimaldi, W. Bourguet, 2014, Vitamins and hormones.

Characterization of novel ligands of ERα, Erβ, and PPARγ: the case of halogenated bisphenol A and their conjugated metabolites.

D. Zalko, A. Riu, W. Bourguet, 2011, Toxicological sciences : an official journal of the Society of Toxicology.

Characterization of Novel Ligands of ER{alpha}, Er{beta}, and PPAR{gamma}: The Case of Halogenated Bisphenol A and Their Conjugated Metabolites.

D. Zalko, A. Riu, W. Bourguet, 2011 .

Functional and Structural Study of the Amino Acid Substitution in a Novel Familial Androgen Receptor Mutation (W752G) Responsible for Complete Androgen Insensitivity Syndrome

N. Kalfa, C. Sultan, W. Bourguet, 2018, Sexual Development.

An Unexpected Mode Of Binding Defines BMS948 as A Full Retinoic Acid Receptor β (RARβ, NR1B2) Selective Agonist

H. Gronemeyer, W. Bourguet, V. Delfosse, 2015, PloS one.

Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function

H. Gronemeyer, C. Royer, Efrén Pérez, 2007, Proceedings of the National Academy of Sciences.

Fragment-based discovery of a new family of non-peptidic small-molecule cyclophilin inhibitors with potent antiviral activities

J. Pawlotsky, D. Douguet, W. Bourguet, 2016, Nature Communications.

Nuclear receptor superfamily: Principles of signaling

Lucia Altucci, William Bourguet, Hinrich Gronemeyer, 2003 .

Topic 1 . 1 Nuclear receptor superfamily : Principles of signaling *

L. Altucci, H. Gronemeyer, W. Bourguet, 2003 .

Mutation of the androgen receptor at amino acid 708 (Gly-->Ala) abolishes partial agonist activity of steroidal antiandrogens.

W. Bourguet, B. Térouanne, C. Sultan, 2003, Molecular pharmacology.

Signal Transduction and Structure of Nuclear Receptors

H. Gronemeyer, W. Bourguet, P. Germain, 2002 .

An integrated structure- and system-based framework to identify new targets of metabolites and known drugs

Xin Gao, Hammad Naveed, William Bourguet, 2015, Bioinform..

IDPs and their complexes in GPCR and nuclear receptor signaling.

P. Bernadó, N. Sibille, W. Bourguet, 2020, Progress in molecular biology and translational science.

Characterization of the Interaction between Retinoic Acid Receptor/Retinoid X Receptor (RAR/RXR) Heterodimers and Transcriptional Coactivators through Structural and Fluorescence Anisotropy Studies*

H. Gronemeyer, C. Royer, Efrén Pérez, 2005, Journal of Biological Chemistry.

Protein-protein interactions in the regulation of RAR-RXR heterodimers transcriptional activity.

W. Bourguet, A. le Maire, P. Germain, 2020, Methods in enzymology.

Differential action on coregulator interaction defines inverse retinoid agonists and neutral antagonists.

H. Gronemeyer, M. Lazar, C. Royer, 2009, Chemistry & biology.

Monitoring ligand-mediated nuclear receptor-coregulator interactions by noncovalent mass spectrometry.

H. Gronemeyer, D. Moras, A. van Dorsselaer, 2004, European journal of biochemistry.

Structural and functional evidence for ligand-independent transcriptional activation by the estrogen-related receptor 3.

D. Moras, J. Wurtz, A. van Dorsselaer, 2002, Molecular cell.

Meeting report: nuclear receptors: transcription factors and drug targets connecting basic research with translational medicine.

S. Mandrup, J. Tuckermann, W. Bourguet, 2010, Molecular endocrinology.

Synergistic activation of human pregnane X receptor by binary cocktails of pharmaceutical and environmental compounds

J. Pascussi, W. Bourguet, V. Delfosse, 2015, Nature Communications.

Interplay of protein disorder in retinoic acid receptor heterodimer and its corepressor regulates gene expression

A. Barducci, P. Barthe, P. Bernadó, 2018, bioRxiv.

Retinoic acid receptors: structural basis for coregulator interaction and exchange.

W. Bourguet, A. le Maire, 2014, Sub-cellular biochemistry.

Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding.

G. Labesse, J. Pons, W. Bourguet, 2021, Journal of medicinal chemistry.

Structural and Functional Profiling of Environmental Ligands for Estrogen Receptors

W. Bourguet, V. Delfosse, Marina Grimaldi, 2014, Environmental health perspectives.

Retinoid Receptor‐Selective Modulators

H. Gronemeyer, A. Lera, M. Mendoza-Parra, 2015 .

Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains.

P. Chambon, H. Gronemeyer, D. Moras, 2000, Molecular cell.

The transrepressive activity of peroxisome proliferator‐activated receptor alpha is necessary and sufficient to prevent liver fibrosis in mice

B. Staels, W. Bourguet, A. Tailleux, 2014, Hepatology.

Structural and Functional Specialization of OSBP-Related Proteins

G. Drin, W. Bourguet, V. Delfosse, 2020, Contact.

Phosphatidylserine transport by ORP/Osh proteins is driven by phosphatidylinositol 4-phosphate

S. Vanni, G. Drin, C. L. Jackson, 2015, Science.

Structural insights into the interaction of the intrinsically disordered co-activator TIF2 with retinoic acid receptor heterodimer (RXR/RAR).

João E. Carvalho, P. Bernadó, N. Sibille, 2021, Journal of molecular biology.

Reporter cell lines to evaluate the selectivity of chemicals for human and zebrafish estrogen and peroxysome proliferator activated γ receptors

W. Bourguet, V. Delfosse, Marina Grimaldi, 2015, Front. Neurosci..

Retinoid receptors and therapeutic applications of RAR/RXR modulators.

H. Gronemeyer, A. Lera, P. Shankaranarayanan, 2012, Current topics in medicinal chemistry.

A structural view of nuclear hormone receptor: endocrine disruptor interactions

William Bourguet, W. Bourguet, P. Balaguer, 2010, Cellular and Molecular Life Sciences.

Regulation of RXR-RAR Heterodimers by RXR- and RAR-Specific Ligands and Their Combinations

W. Bourguet, A. le Maire, P. Balaguer, 2019, Cells.

Pyrazine Arotinoids with Inverse Agonist Activities on the Retinoid and Rexinoid Receptors

H. Gronemeyer, W. Bourguet, A. D. de Lera, 2009, Chembiochem : a European journal of chemical biology.

Inverse agonists and antagonists of retinoid receptors.

H. Gronemeyer, W. Bourguet, A. D. de Lera, 2010, Methods in enzymology.

RAR-RXR selectivity and biological activity of new retinoic acid analogues with heterocyclic or polycyclic aromatic systems.

H. Gronemeyer, W. Bourguet, D. Ivanova, 2002, Bioorganic & medicinal chemistry.

Osh4p exchanges sterols for phosphatidylinositol 4-phosphate between lipid bilayers

D. Douguet, G. Drin, B. Antonny, 2011, The Journal of cell biology.

V. Laudet, F. Brunet, W. Bourguet, 2014, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

Retinoic acid receptor modulators: a perspective on recent advances and promises

William Bourguet, Hinrich Gronemeyer, H. Gronemeyer, 2011, Expert opinion on therapeutic patents.

Interspecies Differences in Activation of Peroxisome Proliferator-Activated Receptor γ by Pharmaceutical and Environmental Chemicals.

M. J. den Broeder, W. Bourguet, Marina Grimaldi, 2021, Environmental science & technology.

LIGAND-BINDING DOMAIN OF THE HUMAN NUCLEAR RECEPTOR RXR-ALPHA

D. Moras, W. Bourguet, Structural Proteomics in Europe, 1996 .

A revisited version of the apo structure of the ligand-binding domain of the human nuclear receptor RXR-ALPHA

D. Moras, A. Dejaegere, W. Bourguet, 2019 .

A revisited version of the apo structure of the ligand-binding domain of the human nuclear receptor retinoic X receptor α.

D. Moras, A. Dejaegere, W. Bourguet, 2019, Acta crystallographica. Section F, Structural biology communications.

Pathological Interactions Between Mutant Thyroid Hormone Receptors and Corepressors and Their Modulation by a Thyroid Hormone Analogue with Therapeutic Potential.

D. Harrus, W. Bourguet, A. le Maire, 2018, Thyroid : official journal of the American Thyroid Association.

N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists.

J. Pascussi, A. Mallavialle, W. Bourguet, 2008, Bioorganic & medicinal chemistry.

Pathophysiology of androgen insensitivity syndromes: molecular and structural approaches of natural and engineered androgen receptor mutations at amino acid 743.

W. Bourguet, S. Lumbroso, J. Lobaccaro, 2002, The Journal of clinical endocrinology and metabolism.

Towards accurate high-throughput ligand affinity prediction by exploiting structural ensembles, docking metrics and ligand similarity

Jean-Luc Pons, Gilles Labesse, Melanie Schneider, 2019, bioRxiv.

Glutamic acid 709 substitutions highlight the importance of the interaction between androgen receptor helices H3 and H12 for androgen and antiandrogen actions.

J. Nicolas, W. Bourguet, S. Lumbroso, 2006, Molecular endocrinology.

Connecting Basic Research with Translational Medicine Meeting Report: Nuclear Receptors: Transcription Factors and Drug Targets

S. Mandrup, J. Tuckermann, W. Bourguet, 2010 .

Functional analyses of phosphatidylserine/PI(4)P exchangers with diverse lipid species and membrane contexts reveal unanticipated rules on lipid transfer

G. Drin, W. Bourguet, V. Delfosse, 2021, BMC Biology.

Allosteric Effects Govern Nuclear Receptor Action: DNA Appears as a Player

William Bourguet, Hinrich Gronemeyer, H. Gronemeyer, 2009, Science Signaling.

Crystal structure of human ERRg LBD in complex with bisphenol-B

A. Barducci, W. Bourguet, V. Delfosse, 2019 .

Insights into the activation mechanism of human estrogen-related receptor γ by environmental endocrine disruptors

A. Barducci, W. Bourguet, V. Delfosse, 2019, Cellular and Molecular Life Sciences.

Development of new approach methods for the identification and characterization of endocrine metabolic disruptors—a PARC project

D. Zalko, O. Spjuth, A. Braeuning, 2023, Frontiers in Toxicology.

Modulation of RXR function through ligand design.

H. Gronemeyer, Efrén Pérez, W. Bourguet, 2012, Biochimica et biophysica acta.

The transrepressive activity of peroxisome proliferator‐activated receptor alpha is necessary and sufficient to prevent liver fibrosis in mice

B. Staels, W. Bourguet, A. Tailleux, 2014, Hepatology.

N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists.

J. Pascussi, W. Bourguet, J. Guichou, 2008, Bioorganic & medicinal chemistry.

Functional analyses of phosphatidylserine/PI(4)P exchangers with diverse lipid species and membrane contexts reveal unanticipated rules on lipid transfer

G. Drin, W. Bourguet, V. Delfosse, 2021, BMC Biology.

Structural insights into the activation of human aryl hydrocarbon receptor by the environmental contaminant benzo[a]pyrene and structurally related compounds.

T. J. Ragan, W. Bourguet, E. Hesketh, 2023, Journal of molecular biology.

2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors

B. Blumberg, W. Bourguet, A. Amato, 2023, Endocrinology.

Endocrine disruptors Structural and functional evidences for the interactions between nuclear hormone receptors and endocrine disruptors at low doses

W. Bourguet, V. Delfosse, Marina Grimaldi, 2022 .

Erratum: A canonical structure for the ligand-binding domain of nuclear receptors

P. Chambon, H. Gronemeyer, D. Moras, 1996, Nature Structural Biology.