All Stories

  1. New structural insights into the control of the retinoic acid receptors RAR/RXR by DNA, ligands, and transcriptional coregulators

    Article • Nucleic Acids Research, September 2025, Oxford University Press (OUP)

    William Bourguet

  2. Targeting pregnane X receptor with a potent agonist-based PROTAC to delay colon cancer relapse

    Article • Oncogenesis, August 2025, Springer Science + Business Media

    William Bourguet

  3. A mechanism for ligand-dependent activation of AHR

    Article • Trends in Pharmacological Sciences, April 2025, Elsevier

    William Bourguet

  4. A two-in-one expression construct for biophysical and structural studies of the human pregnane X receptor ligand-binding domain, a pharmaceutical and environmental target

    Article • Acta Crystallographica Section F Structural Biology Communications, February 2025, International Union of Crystallography

    William Bourguet

  5. An abundant ginger compound furanodienone alleviates gut inflammation via the xenobiotic nuclear receptor PXR in mice

    Article • Nature Communications, February 2025, Springer Science + Business Media

    William Bourguet

  6. What Structural Biology Tells Us About the Mode of Action and Detection of Toxicants

    Article • The Annual Review of Pharmacology and Toxicology, January 2025, Annual Reviews

    William Bourguet

  7. Structural Insights into the Activation of Human Aryl Hydrocarbon Receptor by the Environmental Contaminant Benzo[a]pyrene and Structurally Related Compounds

    Article • Journal of Molecular Biology, February 2024, Elsevier

    William Bourguet

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

    Article • Frontiers in Toxicology, June 2023, Frontiers

    William Bourguet

  9. 2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors

    Article • Endocrinology, February 2023, Endocrine Society

    William Bourguet

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

    Article • Nature Communications, November 2022, Springer Science + Business Media

    William Bourguet

  11. Design and in vitro characterization of RXR variants as tools to investigate the biological role of endogenous rexinoids

    Article • Journal of Molecular Endocrinology, October 2022, Bioscientifica

    William Bourguet

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

    Article • Journal of Medicinal Chemistry, December 2021, American Chemical Society (ACS)

    William Bourguet

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

    Article • Environmental Science & Technology, November 2021, American Chemical Society (ACS)

    William Bourguet

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

    Article • BMC Biology, November 2021, Springer Science + Business Media

    William Bourguet

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

    Article • Essays in Biochemistry, November 2021, Portland Press Ltd.

    William Bourguet

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

    Article • Frontiers in Endocrinology, May 2021, Frontiers

    William Bourguet

  17. Structural Insights into the Interaction of the Intrinsically Disordered Co-activator TIF2 with Retinoic Acid Receptor Heterodimer (RXR/RAR)

    Article • Journal of Molecular Biology, April 2021, Elsevier

    Dr Michael Schubert, William Bourguet

  18. How chemical pollutants can become more harmful when combined

    Article • Proceedings of the National Academy of Sciences, December 2020, Proceedings of the National Academy of Sciences

    William Bourguet

  19. Two Novel Cases of Resistance to Thyroid Hormone Due to THRA Mutation

    Article • Thyroid, August 2020, Mary Ann Liebert Inc

    William Bourguet

  20. Human and Zebrafish Nuclear Progesterone Receptors Are Differently Activated by Manifold Progestins

    Article • Environmental Science & Technology, July 2020, American Chemical Society (ACS)

    William Bourguet

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

    Article • Cells, June 2020, MDPI AG

    William Bourguet

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

    Article • Journal of Cellular and Molecular Medicine, June 2020, Wiley

    William Bourguet

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

    Article • International Journal of Molecular Sciences, May 2020, MDPI AG

    William Bourguet

  24. Structural and Functional Specialization of OSBP-Related Proteins

    Article • Contact The Journal of Inter-Organelle Communication, January 2020, SAGE Publications

    William Bourguet

  25. IDPs and their complexes in GPCR and nuclear receptor signaling

    Article • January 2020, Elsevier

    William Bourguet

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

    Article • January 2020, Elsevier

    William Bourguet

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

    Article • Cells, November 2019, MDPI AG

    William Bourguet

  28. Mechanisms of endocrine disruption through nuclear receptors and related pathways

    Article • Current Opinion in Endocrine and Metabolic Research, August 2019, Elsevier

    William Bourguet

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

    Article • Structure, August 2019, Elsevier

    William Bourguet

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

    Article • Bioinformatics, July 2019, Oxford University Press (OUP)

    William Bourguet

  31. In Silico Predictions of Endocrine Disruptors Properties

    Article • Endocrinology, July 2019, Endocrine Society

    William Bourguet

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

    Article • Cellular and Molecular Life Sciences, May 2019, Springer Science + Business Media

    William Bourguet

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

    Article • Acta Crystallographica Section F Structural Biology Communications, January 2019, International Union of Crystallography

    William Bourguet

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

    Article • Thyroid, December 2018, Mary Ann Liebert Inc

    William Bourguet

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

    Article • Science Advances, February 2018, American Association for the Advancement of Science

    Dr Michael Schubert, William Bourguet

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

    Article • Sexual Development, January 2018, Karger Publishers

    William Bourguet

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

    Article • Comptes Rendus Biologies, September 2017, Cellule MathDoc/CEDRAM

    William Bourguet

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

    Article • PLOS One, November 2016, PLOS

    Dr Michael Schubert, William Bourguet

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

    Article • Nature Communications, September 2016, Springer Science + Business Media

    William Bourguet

  40. L’association fait le poison

    Article • médecine/sciences, April 2016, EDP Sciences

    William Bourguet

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

    Article • Royal Society Open Science, March 2016, Royal Society Publishing

    Dr Michael Schubert, Romain A Studer, William Bourguet

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

    Article • Nature Communications, September 2015, Springer Science + Business Media

    William Bourguet

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

    Article • Bioinformatics, August 2015, Oxford University Press (OUP)

    William Bourguet

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

    Article • The Journal of Clinical Endocrinology & Metabolism, August 2015, Endocrine Society

    William Bourguet

  45. Combining `dry' co-crystallization andin situdiffraction to facilitate ligand screening by X-ray crystallography

    Article • Acta Crystallographica Section D Biological Crystallography, July 2015, International Union of Crystallography

    William Bourguet

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

    Article • Science, July 2015, American Association for the Advancement of Science

    Dr Stefano Vanni, William Bourguet

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

    Article • Frontiers in Neuroscience, June 2015, Frontiers

    William Bourguet

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

    Article • Frontiers in Endocrinology, May 2015, Frontiers

    William Bourguet

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

    Article • PLOS One, May 2015, PLOS

    William Bourguet

  50. Structural and Functional Profiling of Environmental Ligands for Estrogen Receptors

    Article • Environmental Health Perspectives, December 2014, Environmental Health Perspectives

    William Bourguet

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

    Article • Hepatology, November 2014, Wolters Kluwer Health

    Professor Bart Staels, William Bourguet

  52. A Mollusk Retinoic Acid Receptor (RAR) Ortholog Sheds Light on the Evolution of Ligand Binding

    Article • Endocrinology, November 2014, Endocrine Society

    Dr Michael Schubert, William Bourguet

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

    Article • Toxicology and Applied Pharmacology, October 2014, Elsevier

    Maria Bondesson, William Bourguet

  54. Estrogen‐related receptor γ is an in vivo receptor of bisphenol A

    Article • The FASEB Journal, April 2014, Wiley

    William Bourguet

  55. Nuclear Receptor Profiling of Bisphenol-A and Its Halogenated Analogues

    Article • January 2014, Elsevier

    William Bourguet

  56. Retinoic Acid Receptors: Structural Basis for Coregulator Interaction and Exchange

    Article • January 2014, Springer Science + Business Media

    William Bourguet

  57. Diosgenin relieves goiter via the inhibition of thyrocyte proliferation in a mouse model of Graves' disease

    Article • Acta Pharmacologica Sinica, November 2013, Springer Science + Business Media

    William Bourguet

  58. Dimerization of Nuclear Receptors

    Article • January 2013, Elsevier

    William Bourguet

  59. Vers des bisphénols sans effets hormonaux

    Article • médecine/sciences, January 2013, EDP Sciences

    William Bourguet

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

    Article • Proceedings of the National Academy of Sciences, August 2012, Proceedings of the National Academy of Sciences

    William Bourguet

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

    Article • Molecular and Cellular Endocrinology, April 2012, Elsevier

    William Bourguet

  62. Retinoid Receptors and Therapeutic Applications of RAR/RXR Modulators

    Article • Current Topics in Medicinal Chemistry, March 2012, Bentham Science Publishers

    William Bourguet

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

    Article • Proceedings of the National Academy of Sciences, February 2012, Proceedings of the National Academy of Sciences

    William Bourguet

  64. Modulation of RXR function through ligand design

    Article • Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, January 2012, Elsevier

    William Bourguet

  65. Osh4p exchanges sterols for phosphatidylinositol 4-phosphate between lipid bilayers

    Article • Journal of Cell Biology, December 2011, Rockefeller University Press

    William Bourguet

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

    Article • Environmental Health Perspectives, September 2011, Environmental Health Perspectives

    William Bourguet

  67. Characterization of Novel Ligands of ERα, Erβ, and PPARγ: The Case of Halogenated Bisphenol A and Their Conjugated Metabolites

    Article • Toxicological Sciences, May 2011, Oxford University Press (OUP)

    William Bourguet

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

    Article • Expert Opinion on Therapeutic Patents, November 2010, Informa Healthcare

    William Bourguet

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

    Article • Molecular Endocrinology, July 2010, Endocrine Society

    William Bourguet

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

    Article • Nature Structural & Molecular Biology, June 2010, Springer Science + Business Media

    William Bourguet

  71. A structural view of nuclear hormone receptor: endocrine disruptor interactions

    Article • Cellular and Molecular Life Sciences, January 2010, Springer Science + Business Media

    William Bourguet

  72. Inverse Agonists and Antagonists of Retinoid Receptors

    Article • January 2010, Elsevier

    William Bourguet

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

    Article • Science Signaling, June 2009, American Association for the Advancement of Science

    William Bourguet

  74. Structure of the Third Intracellular Loop of the Vasopressin V2 Receptor and Conformational Changes upon Binding to gC1qR

    Article • Journal of Molecular Biology, May 2009, Elsevier

    William Bourguet

  75. Differential Action on Coregulator Interaction Defines Inverse Retinoid Agonists and Neutral Antagonists

    Article • Chemistry & Biology, May 2009, Elsevier

    William Bourguet

  76. 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

    Article • Journal of Medicinal Chemistry, May 2009, American Chemical Society (ACS)

    William Bourguet

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

    Article • ChemBioChem, April 2009, Wiley

    William Bourguet

  78. Activation of RXR–PPAR heterodimers by organotin environmental endocrine disruptors

    Article • EMBO Reports, March 2009, Springer Science + Business Media

    William Bourguet

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

    Article • Acta Crystallographica Section F Structural Biology and Crystallization Communications, June 2008, International Union of Crystallography

    William Bourguet

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

    Article • Bioorganic & Medicinal Chemistry, April 2008, Elsevier

    William Bourguet

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

    Article • Proceedings of the National Academy of Sciences, October 2007, Proceedings of the National Academy of Sciences

    William Bourguet

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

    Article • Nature Reviews Drug Discovery, October 2007, Springer Science + Business Media

    William Bourguet

  83. 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

    Article • Molecular Pharmacology, September 2007, Elsevier

    William Bourguet

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

    Article • The International Journal of Biochemistry & Cell Biology, July 2007, Elsevier

    William Bourguet

  85. Glutamic Acid 709 Substitutions Highlight the Importance of the Interaction between Androgen Receptor Helices H3 and H12 for Androgen and Antiandrogen Actions

    Article • Molecular Endocrinology, April 2006, Endocrine Society

    William Bourguet

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

    Article • Journal of Biological Chemistry, January 2005, Elsevier

    William Bourguet

  87. Monitoring ligand‐mediated nuclear receptor–coregulator interactions by noncovalent mass spectrometry

    Article • FEBS Journal, December 2004, Wiley

    William Bourguet

  88. A new mutation of the androgen receptor, P817A, causing partial androgen insensitivity syndrome: in vitro and structural analysis

    Article • Journal of Molecular Endocrinology, June 2004, Bioscientifica

    William Bourguet

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

    Article • Acta Crystallographica Section D Biological Crystallography, May 2004, International Union of Crystallography

    William Bourguet

  90. Separation of Retinoid X Receptor Homo- and Heterodimerization Functions

    Article • Molecular and Cellular Biology, November 2003, ASM Journals

    William Bourguet

  91. Mutation of the Androgen Receptor at Amino Acid 708 (Gly→Ala) Abolishes Partial Agonist Activity of Steroidal Antiandrogens

    Article • Molecular Pharmacology, April 2003, Elsevier

    William Bourguet

  92. Pathophysiology of Androgen Insensitivity Syndromes: Molecular and Structural Approaches of Natural and Engineered Androgen Receptor Mutations at Amino Acid 743

    Article • The Journal of Clinical Endocrinology & Metabolism, December 2002, Endocrine Society

    William Bourguet

  93. RAR–RXR Selectivity and Biological Activity of New Retinoic Acid Analogues with Heterocyclic or Polycyclic Aromatic Systems

    Article • Bioorganic & Medicinal Chemistry, July 2002, Elsevier

    William Bourguet

  94. Structural and Functional Evidence for Ligand-Independent Transcriptional Activation by the Estrogen-Related Receptor 3

    Article • Molecular Cell, February 2002, Elsevier

    William Bourguet

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

    Article • Trends in Pharmacological Sciences, October 2000, Elsevier

    William Bourguet

  96. Heterodimeric Complex of RAR and RXR Nuclear Receptor Ligand-Binding Domains: Purification, Crystallization, and Preliminary X-Ray Diffraction Analysis

    Article • Protein Expression and Purification, July 2000, Elsevier

    William Bourguet

  97. Ligand- and DNA-induced dissociation of RXR tetramers

    Article • Journal of Molecular Biology, January 1998, Elsevier

    William Bourguet

  98. Exploring hydrophobic sites in proteins with xenon or krypton

    Article • Proteins Structure Function and Bioinformatics, January 1998, Wiley

    William Bourguet

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

    Article • The EMBO Journal, September 1997, Springer Science + Business Media

    William Bourguet

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

    Article • Nature Structural Biology, February 1996, Springer Science + Business Media

    William Bourguet

  101. Purification, Functional Characterization, and Crystallization of the Ligand Binding Domain of the Retinoid X Receptor

    Article • Protein Expression and Purification, October 1995, Elsevier

    William Bourguet

  102. Synthesis of a biospecific adsorbent for the purification of the three human retinoic acid receptors by affinity chromatography

    Article • Biochemical and Biophysical Research Communications, September 1992, Elsevier

    William Bourguet