Publications
2023
Structural Insights into the Activation of Human Aryl Hydrocarbon Receptor by the Environmental Contaminant Benzo[a]pyrene and Structurally Related Compounds
Kwong HS, Paloni M, Grandvuillemin L, Sirounian S, Ancelin A, Lai-Kee-Him J, Grimaldi M, Carivenc C, Lancey C, Ragan TJ, Hesketh EL, Balaguer P, Barducci A, Gruszczyk J, Bourguet W, J Mol Biol, 2023
Development of new approach methods for the identification and characterization of endocrine metabolic disruptors-a PARC project
Braeuning A, Balaguer P, Bourguet W, Carreras-Puigvert J, Feiertag K, Kamstra JH, Knapen D, Lichtenstein D, Marx-Stoelting P, Rietdijk J, Schubert K, Spjuth O, Stinckens E, Thedieck K, van den Boom R, Vergauwen L, von Bergen M, Wewer N, Zalko D, Front Toxicol, 2023
Retinoic Acid and Retinoid X Receptors
Schubert M, Germain P, Cells, 2023
2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors
Ren XM, Chang RC, Huang Y, Amorim Amato A, Carivenc C, Grimaldi M, Kuo Y, Balaguer P, Bourguet W, Blumberg B, Endocrinology, 2023
2022
Cryo-EM structure of the agonist-bound Hsp90-XAP2-AHR cytosolic complex
Gruszczyk J, Grandvuillemin L, Lai-Kee-Him J, Paloni M, Savva CG, Germain P, Grimaldi M, Boulahtouf A, Kwong HS, Bous J, Ancelin A, Bechara C, Barducci A, Balaguer P, Bourguet W, Nat Commun, 2022
Design and in vitro characterization of RXR variants as tools to investigate the biological role of endogenous rexinoids
le Maire A, Rey M, Vivat V, Guee L, Blanc P, Malosse C, Chamot-Rooke J, Germain P, Bourguet W, J Mol Endocrinol, 2022
Ligands and DNA in the allosteric control of retinoid receptors function
Germain P, Rochel N, Bourguet W, Essays Biochem, 2022
2021
Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding
Schneider M, Delfosse V, Gelin M, Grimaldi M, Granell M, Heriaud L, Pons JL, Cohen Gonsaud M, Balaguer P, Bourguet W, Labesse G, J Med Chem, 2021
Interspecies Differences in Activation of Peroxisome Proliferator-Activated Receptor gamma by Pharmaceutical and Environmental Chemicals
Garoche C, Boulahtouf A, Grimaldi M, Chiavarina B, Toporova L, den Broeder MJ, Legler J, Bourguet W, Balaguer P, Environ Sci Technol, 2021
Functional analyses of phosphatidylserine/PI(4)P exchangers with diverse lipid species and membrane contexts reveal unanticipated rules on lipid transfer
Ikhlef S, Lipp NF, Delfosse V, Fuggetta N, Bourguet W, Magdeleine M, Drin G, BMC Biol, 2021
A Comparative Study of Human and Zebrafish Pregnane X Receptor Activities of Pesticides and Steroids Using In Vitro Reporter Gene Assays
Creusot N, Garoche C, Grimaldi M, Boulahtouf A, Chiavarina B, Bourguet W, Balaguer P, Front Endocrinol (Lausanne), 2021
Mechanistic insights into the synergistic activation of the RXR-PXR heterodimer by endocrine disruptor mixtures
Delfosse V, Huet T, Harrus D, Granell M, Bourguet M, Gardia-Parege C, Chiavarina B, Grimaldi M, Le Mevel S, Blanc P, Huang D, Gruszczyk J, Demeneix B, Cianferani S, Fini JB, Balaguer P, Bourguet W, Proc Natl Acad Sci U S A, 2021
Structural Insights into the Interaction of the Intrinsically Disordered Co-activator TIF2 with Retinoic Acid Receptor Heterodimer (RXR/RAR)
Senicourt L, le Maire A, Allemand F, Carvalho JE, Guee L, Germain P, Schubert M, Bernado P, Bourguet W, Sibille N, J Mol Biol, 2021
2020
Human and Zebrafish Nuclear Progesterone Receptors Are Differently Activated by Manifold Progestins
Garoche C, Aut-Aussa S, Boulahtouf A, Creusot N, Hinfray N, Bourguet W, Balaguer P, Brion F, Environ Sci Technol, 2020
Two Novel Cases of Resistance to Thyroid Hormone Due to
le Maire A, Bouhours-Nouet N, Soamalala J, Mirebeau-Prunier D, Paloni M, Guee L, Heron D, Mignot C, Illouz F, Joubert F, Briet C, Rodien P, Bourguet W, Flamant F, Guyot R, Thyroid, 2020
Peroxisome proliferator-activated receptor gamma-ligand-binding domain mutations associated with familial partial lipodystrophy type 3 disrupt human trophoblast fusion and fibroblast migration
Shoaito H, Chauveau S, Gosseaume C, Bourguet W, Vigouroux C, Vatier C, Pienkowski C, Fournier T, Degrelle SA, J Cell Mol Med, 2020
High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride as a Selective and Competitive Antagonist of the Androgen Receptor
Dellal H, Boulahtouf A, Alaterre E, Cuenant A, Grimaldi M, Bourguet W, Gongora C, Balaguer P, Pourquier P, Cells, 2020
The GOLIATH Project: Towards an Internationally Harmonised Approach for Testing Metabolism Disrupting Compounds
Legler J, Zalko D, Jourdan F, Jacobs M, Fromenty B, Balaguer P, Bourguet W, Munic Kos V, Nadal A, Beausoleil C, Cristobal S, Remy S, Ermler S, Margiotta-Casaluci L, Griffin JL, Blumberg B, Chesne C, Hoffmann S, Andersson PL, Kamstra JH, Int J Mol Sci, 2020
Towards accurate high-throughput ligand affinity prediction by exploiting structural ensembles, docking metrics and ligand similarity
Schneider M, Pons JL, Bourguet W, Labesse G, Bioinformatics, 2020
Structural and Functional Specialization of OSBP-Related Proteins
Delfosse V, Bourguet W, Drin G, Contact, 2020
Protein-protein interactions in the regulation of RAR-RXR heterodimers transcriptional activity
le Maire A, Germain P, Bourguet W, Meth Enzymol, 2020
IDPs and their complexes in GPCR and nuclear receptor signaling
Guillien M, le Maire A, Mouhand A, Bernado P, Bourguet W, Baneres JL, Sibille N, Prog Mol Biol Transl Sci, 2020
2019
Insights into the activation mechanism of human estrogen-related receptor gamma by environmental endocrine disruptors
Thouennon E, Delfosse V, Bailly R, Blanc P, Boulahtouf A, Grimaldi M, Barducci A, Bourguet W, Balaguer P, Cell Mol Life Sci, 2019
Regulation of RXR-RAR Heterodimers by RXR- and RAR-Specific Ligands and Their Combinations
le Maire A, Teyssier C, Balaguer P, Bourguet W, Germain P, Cells, 2019
In silico predictions of endocrine disruptors properties
Schneider M, Pons JL, Labesse G, Bourguet W, Endocrinology, 2019
Interplay of Protein Disorder in Retinoic Acid Receptor Heterodimer and Its Corepressor Regulates Gene Expression
Cordeiro TN, Sibille N, Germain P, Barthe P, Boulahtouf A, Allemand F, Bailly R, Vivat V, Ebel C, Barducci A, Bourguet W, le Maire A, Bernado P, Structure, 2019
A revisited version of the apo structure of the ligand-binding domain of the human nuclear receptor retinoic X receptor alpha
Eberhardt J, McEwen AG, Bourguet W, Moras D, Dejaegere A, Acta Crystallogr F Struct Biol Commun, 2019
Mechanisms of endocrine disruption through nuclear receptors and related pathways
Balaguer P, Delfosse V, Bourguet W, Curr Opin Endocr Metab Res, 2019
2018
Pathological interactions between mutant thyroid hormone receptors and corepressors and their modulation by a thyroid hormone analogue with therapeutic potential
Harrus D, Demene H, Vasquez EF, Boulahtouf A, Germain P, Figueira AC, Privalsky ML, Bourguet W, le Maire A, Thyroid, 2018
Functional and Structural Study of the Amino Acid Substitution in a Novel Familial Androgen Receptor Mutation (W752G) Responsible for Complete Androgen Insensitivity Syndrome
Paris F, Boulahtouf A, Kalfa N, Guibal MP, Gaspari L, Servant N, Bourguet W, Sultan C, Balaguer P, Sex Dev, 2018
The ancestral retinoic acid receptor was a low-affinity sensor triggering neuronal differentiation
Handberg-Thorsager M, Gutierrez-Mazariegos J, Arold ST, Kumar Nadendla E, Bertucci PY, Germain P, Tomancak P, Pierzchalski K, Jones JW, Albalat R, Kane MA, Bourguet W, Laudet V, Arendt D, Schubert M, Sci Adv, 2018
2017
2016
The Human Mixed Lineage Leukemia 5 (MLL5), a Sequentially and Structurally Divergent SET Domain-Containing Protein with No Intrinsic Catalytic Activity
Mas-Y-Mas S, Barbon M, Teyssier C, Demene H, Carvalho JE, Bird LE, Lebedev A, Fattori J, Schubert M, Dumas C, Bourguet W, Le Maire A, PLoS One, 2016
Fragment-based discovery of a new family of non-peptidic small-molecule cyclophilin inhibitors with potent antiviral activities
Ahmed-Belkacem A, Colliandre L, Ahnou N, Nevers Q, Gelin M, Bessin Y, Brillet R, Cala O, Douguet D, Bourguet W, Krimm I, Pawlotsky JM, Guichou JF, Nat Commun, 2016
[The association makes the poison: new perspective on the cocktail effect of xenobiotics and drug interactions]
Delfosse V, Balaguer P, Bourguet W, Med Sci (Paris), 2016
Evolutionary diversification of retinoic acid receptor ligand-binding pocket structure by molecular tinkering
Gutierrez-Mazariegos J, Nadendla EK, Studer RA, Alvarez S, de Lera AR, Kuraku S, Bourguet W, Schubert M, Laudet V, R Soc Open Sci, 2016
2015
Synergistic activation of human pregnane X receptor by binary cocktails of pharmaceutical and environmental compounds
Delfosse V, Dendele B, Huet T, Grimaldi M, Boulahtouf A, Gerbal-Chaloin S, Beucher B, Roecklin D, Muller C, Rahmani R, Cavailles V, Daujat-Chavanieu M, Vivat V, Pascussi JM, Balaguer P, Bourguet W, Nat Commun, 2015
An integrated structure- and system-based framework to identify new targets of metabolites and known drugs
Naveed H, Hameed US, Harrus D, Bourguet W, Arold ST, Gao X, Bioinformatics, 2015
Combining `dry' co-crystallization and in situ diffraction to facilitate ligand screening by X-ray crystallography
Gelin M, Delfosse V, Allemand F, Hoh F, Sallaz-Damaz Y, Pirocchi M, Bourguet W, Ferrer JL, Labesse G, Guichou JF, Acta Crystallogr D Biol Crystallogr, 2015
Reporter cell lines to evaluate the selectivity of chemicals for human and zebrafish estrogen and peroxysome proliferator activated gamma receptors
Grimaldi M, Boulahtouf A, Delfosse V, Thouennon E, Bourguet W, Balaguer P, Front Neurosci, 2015
Reporter Cell Lines for the Characterization of the Interactions between Human Nuclear Receptors and Endocrine Disruptors
Grimaldi M, Boulahtouf A, Delfosse V, Thouennon E, Bourguet W, Balaguer P, Front Endocrinol (Lausanne), 2015
INTRACELLULAR TRANSPORT. Phosphatidylserine transport by ORP/Osh proteins is driven by phosphatidylinositol 4-phosphate
Moser von Filseck J, Copic A, Delfosse V, Vanni S, Jackson CL, Bourguet W, Drin G, Science, 2015
An Unexpected Mode Of Binding Defines BMS948 as A Full Retinoic Acid Receptor beta (RARbeta, NR1B2) Selective Agonist
Nadendla E, Teyssier C, Delfosse V, Vivat V, Krishnasamy G, Gronemeyer H, Bourguet W, Germain P, PLoS ONE, 2015
A novel mutation in THRA gene associated with an atypical phenotype of resistance to thyroid hormone
Espiard S, Savagner F, Flamant F, Vlaeminck-Guillem V, Guyot R, Munier M, d'Herbomez M, Bourguet W, Pinto G, Rose C, Rodien P, Wemeau JL, J Clin Endocrinol Metab, 2015
2014
Structural and Functional Profiling of Environmental Ligands for Estrogen Receptors
Delfosse V, Grimaldi M, Cavailles V, Balaguer P, Bourguet W, Environ Health Perspect, 2014
Nuclear receptor profiling of bisphenol-a and its halogenated analogues
Delfosse V, Grimaldi M, le Maire A, Bourguet W, Balaguer P, Vitam Horm, 2014
A structural perspective on nuclear receptors as targets of environmental compounds
Delfosse V, Maire AL, Balaguer P, Bourguet W, Acta Pharmacol Sin, 2014
A mollusk Retinoic Acid Receptor (RAR) ortholog sheds light on the evolution of ligand binding
Gutierrez-Mazariegos J, Kumar Nadendla E, Lima D, Pierzchalski K, Jones JW, Kane M, Nishikawa JI, Hiromori Y, Nakanishi T, Santos MM, Castro LF, Bourguet W, Schubert M, Laudet V, Endocrinology, 2014
Retinoic Acid receptors: structural basis for coregulator interaction and exchange
le Maire A, Bourguet W, Subcell Biochem, 2014
The transrepressive activity of Pparalpha is necessary and sufficient to prevent liver fibrosis
Pawlak M, Bauge E, Bourguet W, De Bosscher K, Lalloyer F, Tailleux A, Lebherz C, Lefebvre P, Staels B, Hepatology, 2014
Selectivity of natural, synthetic and environmental estrogens for zebrafish estrogen receptors
Pinto C, Grimaldi M, Boulahtouf A, Pakdel F, Brion F, Aut-Aussa S, Cavailles V, Bourguet W, Gustafsson JA, Bondesson M, Balaguer P, Toxicol Appl Pharmacol, 2014
Estrogen-related receptor gamma is an in vivo receptor of bisphenol A
Tohme M, Prud'homme SM, Boulahtouf A, Samarut E, Brunet F, Bernard L, Bourguet W, Gibert Y, Balaguer P, Laudet V, FASEB J, 2014
2013
Dimerization of nuclear receptors
Germain P, Bourguet W, Methods Cell Biol, 2013
[Towards bisphenols without hormonal effects]
Balaguer P, Delfosse V, Grimaldi M, Bourguet W, Med Sci (Paris), 2013
2012
Structural and mechanistic insights into bisphenols action provide guidelines for risk assessment and discovery of bisphenol A substitutes
Delfosse V, Grimaldi M, Pons JL, Boulahtouf A, le Maire A, Cavailles V, Labesse G, Bourguet W, Balaguer P, Proc Natl Acad Sci U S A, 2012
Modulation of RXR function through ligand design
Perez E, Bourguet W, Gronemeyer H, de Lera AR, Biochim Biophys Acta, 2012
Structural basis for a molecular allosteric control mechanism of cofactor binding to nuclear receptors
Osz J, Brelivet Y, Peluso-Iltis C, Cura V, Eiler S, Ruff M, Bourguet W, Rochel N, Moras D, Proc Natl Acad Sci U S A, 2012
Retinoid receptors and therapeutic applications of RAR/RXR modulators.
Maire Al, Alvarez S, Shankaranarayanan P, Lera AR, Bourguet W, Gronemeyer H, Curr Top Med Chem, 2012
SMRTepsilon, a corepressor variant, interacts with a restricted subset of nuclear receptors, including the retinoic acid receptors alpha and beta
Mengeling BJ, Goodson ML, Bourguet W, Privalsky ML, Mol Cell Endocrinol, 2012
2011
Retinoic acid receptor modulators: a perspective on recent advances and promises
Alvarez S, Bourguet W, Gronemeyer H, de Lera AR, Expert Opin Ther Pat, 2011
Osh4p exchanges sterols for phosphatidylinositol 4-phosphate between lipid bilayers
de Saint-Jean M, Delfosse V, Douguet D, Chicanne G, Payrastre B, Bourguet W, Antonny B, Drin G, J Cell Biol, 2011
Peroxisome proliferator-activated receptor gamma is a target for halogenated analogs of bisphenol A
Riu A, Grimaldi M, le Maire A, Bey G, Phillips K, Boulahtouf A, Perdu E, Zalko D, Bourguet W, Balaguer P, Environ Health Perspect, 2011
Characterization of novel ligands of ERalpha, Erbeta, and PPARgamma: the case of halogenated bisphenol A and their conjugated metabolites
Riu A, le Maire A, Grimaldi M, Audebert M, Hillenweck A, Bourguet W, Balaguer P, Zalko D, Toxicol Sci, 2011
IUPHAR-DB: new receptors and tools for easy searching and visualization of pharmacological data
Sharman JL, Mpamhanga CP, Spedding M, Germain P, Staels B, Dacquet C, Laudet V, Harmar AJ, Nucleic Acids Res, 2011
2010
Inverse agonists and antagonists of retinoid receptors
Bourguet W, de Lera A, Gronemeyer H, Methods Enzymol., 2010
A structural view of nuclear hormone receptor: endocrine disruptor interactions
le Maire A, Bourguet W, Balaguer P, Cell Mol Life Sci., 2010
A unique secondary-structure switch controls constitutive gene repression by retinoic acid receptor
le Maire A, Teyssier C, Erb C, Grimaldi M, Alvarez S, de Lera AR, Balaguer P, Gronemeyer H, Royer CA, Germain P, Bourguet W, Nat Struct Mol Biol, 2010
Meeting report: nuclear receptors: transcription factors and drug targets connecting basic research with translational medicine
Tuckermann J, Bourguet W, Mandrup S, Mol Endocrinol, 2010
2009
Structure of the third intracellular loop of the vasopressin V2 receptor and conformational changes upon binding to gC1qR
Bellot G, Granier S, Bourguet W, Seyer R, Rahmeh R, Mouillac B, Pascal R, Mendre C, Demene H, J Mol Biol, 2009
Structural and functional insights into the ligand-binding domain of a nonduplicated retinoid X nuclear receptor from the invertebrate chordate amphioxus
Tocchini-Valentini GD, Rochel N, Escriva H, Germain P, Peluso-Iltis C, Paris M, Sanglier-Cianferani S, Van Dorsselaer A, Moras D, Laudet V, J Biol Chem, 2009
Dynamic and combinatorial control of gene expression by nuclear retinoic acid receptors (RARs)
Rochette-Egly C, Germain P, Nucl Recept Signal, 2009
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-y l)phenyl]acrylic acids and their 4-alkoxy isomers
Perez Santin E, Germain P, Quillard F, Khanwalkar H, Rodriguez-Barrios F, Gronemeyer H, de Lera AR, Bourguet W, J Med Chem, 2009
Activation of RXR-PPAR heterodimers by organotin environmental endocrine disruptors
le Maire A, Grimaldi M, Roecklin D, Dagnino S, Vivat-Hannah V, Balaguer P, Bourguet W, EMBO Rep, 2009
Allosteric effects govern nuclear receptor action: DNA appears as a player
Gronemeyer H, Bourguet W, Sci Signal, 2009
Differential action on coregulator interaction defines inverse retinoid agonists and neutral antagonists
Germain P, Gaudon C, Pogenberg V, Sanglier S, Van Dorsselaer A, Royer CA, Lazar MA, Bourguet W, Gronemeyer H, Chem Biol, 2009
Pyrazine arotinoids with inverse agonist activities on the retinoid and rexinoid receptors
Garcia J, Khanwalkar H, Pereira R, Erb C, Voegel JJ, Collette P, Mauvais P, Bourguet W, Gronemeyer H, de Lera AR, Chembiochem, 2009
Retinoid receptor subtype-selective modulators through synthetic modifications of RARgamma agonists
Alvarez S, Alvarez R, Khanwalkar H, Germain P, Lemaire G, Rodriguez-Barrios F, Gronemeyer H, de Lera AR, Bioorg Med Chem, 2009
2008
N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists
Benod C, Subra G, Nahoum V, Mallavialle A, Guichou JF, Milhau J, Robles S, Bourguet W, Pascussi JM, Balaguer P, Chavanieu A, Bioorg Med Chem, 2008
Nuclear receptor ligand-binding domains: reduction of helix H12 dynamics to favour crystallization
Nahoum V, Lipski A, Quillard F, Guichou JF, Boublik Y, Perez E, Germain P, de Lera AR, Bourguet W, Acta Crystallogr Sect F Struct Biol Cryst Commun, 2008
2007
Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function
Nahoum V, Perez E, Germain P, Rodriguez-Barrios F, Manzo F, Kammerer S, Lemaire G, Hirsch O, Royer CA, Gronemeyer H, de Lera AR, Bourguet W, Proc Natl Acad Sci U S A, 2007
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
Lemaire G, Benod C, Nahoum V, Pillon A, Boussioux AM, Guichou JF, Subra G, Pascussi JM, Bourguet W, Chavanieu A, Balaguer P, Mol Pharmacol, 2007
Design of selective nuclear receptor modulators: RAR and RXR as a case study
de Lera AR, Bourguet W, Altucci L, Gronemeyer H, Nat Rev Drug Discov, 2007
Androgen and estrogen receptors: potential of crystallography in the fight against cancer
Nahoum V, Bourguet W, Int J Biochem Cell Biol, 2007
2006
2005
2004
A new mutation of the androgen receptor, P817A, causing partial androgen insensitivity syndrome: in vitro and structural analysis
Lumbroso S, Wagschal A, Bourguet W, Georget V, Mazen I, Servant N, Audran F, Sultan C, Auzou G, J Mol Endocrinol, 2004
Purification and crystallization of the heterodimeric complex of RARbeta and RXRalpha ligand-binding domains in the active conformation
Pogenberg V, Guichou JF, Bourguet W, Acta Crystallogr D Biol Crystallogr, 2004
Monitoring ligand-mediated nuclear receptor-coregulator interactions by noncovalent mass spectrometry
Sanglier S, Bourguet W, Germain P, Chavant V, Moras D, Gronemeyer H, Potier N, Van Dorsselaer A, Eur J Biochem, 2004
2003
Nuclear receptor superfamily: principles of signaling
Germain P, Altucci L, Bourguet W, Rochette-Egly C, Gronemeyer H, Pure Appl Chem, 2003
Mutation of the androgen receptor at amino acid 708 (Gly-->Ala) abolishes partial agonist activity of steroidal antiandrogens
Terouanne B, Nirde P, Rabenoelina F, Bourguet W, Sultan C, Auzou G, Mol Pharmacol, 2003
Separation of retinoid X receptor homo- and heterodimerization functions
Vivat-Hannah V, Bourguet W, Gottardis M, Gronemeyer H, Mol Cell Biol, 2003
2002
RAR-RXR selectivity and biological activity of new retinoic acid analogues with heterocyclic or polycyclic aromatic systems
Ivanova D, Gaudon C, Rossin A, Bourguet W, Gronemeyer H, Bioorg Med Chem, 2002
Pathophysiology of androgen insensitivity syndromes: molecular and structural approaches of natural and engineered androgen receptor mutations at amino acid 743
Poujol N, Lumbroso S, Terouanne B, Lobaccaro JM, Bourguet W, Sultan C, J Clin Endocrinol Metab, 2002
Signal transduction and structure of nuclear receptors
Bourguet W, Germain P, Gronemeyer H, Hormone signaling, 2002
