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Twenty years of Mediator complex structural studies.

Verger A, Monté D, Villeret V.

Biochem Soc Trans. 2019 Feb 7. pii: BST20180608. doi: 10.1042/BST20180608. [Epub ahead of print] Review.


Crystal structure of human Mediator subunit MED23.

Monté D, Clantin B, Dewitte F, Lens Z, Rucktooa P, Pardon E, Steyaert J, Verger A, Villeret V.

Nat Commun. 2018 Aug 23;9(1):3389. doi: 10.1038/s41467-018-05967-y.


Computational characterization of the binding mode between oncoprotein Ets-1 and DNA-repair enzymes.

de Ruyck J, Brysbaert G, Villeret V, Aumercier M, Lensink MF.

Proteins. 2018 Oct;86(10):1055-1063. doi: 10.1002/prot.25578. Epub 2018 Sep 25.


Ets-1 interacts through a similar binding interface with Ku70 and Poly (ADP-Ribose) Polymerase-1.

Choul-Li S, Legrand AJ, Vicogne D, Villeret V, Aumercier M.

Biosci Biotechnol Biochem. 2018 Oct;82(10):1753-1759. doi: 10.1080/09168451.2018.1484276. Epub 2018 Jun 18.


Solution Structure of the N-Terminal Domain of Mediator Subunit MED26 and Molecular Characterization of Its Interaction with EAF1 and TAF7.

Lens Z, Cantrelle FX, Peruzzini R, Hanoulle X, Dewitte F, Ferreira E, Baert JL, Monté D, Aumercier M, Villeret V, Verger A, Landrieu I.

J Mol Biol. 2017 Oct 13;429(20):3043-3055. doi: 10.1016/j.jmb.2017.09.001. Epub 2017 Sep 9.


Structural basis for haem piracy from host haemopexin by Haemophilus influenzae.

Zambolin S, Clantin B, Chami M, Hoos S, Haouz A, Villeret V, Delepelaire P.

Nat Commun. 2016 May 18;7:11590. doi: 10.1038/ncomms11590.


1H, 15N and 13C assignments of the N-terminal domain of the Mediator complex subunit MED26.

Peruzzini R, Lens Z, Verger A, Dewitte F, Ferreira E, Baert JL, Villeret V, Landrieu I, Cantrelle FX.

Biomol NMR Assign. 2016 Apr;10(1):233-6. doi: 10.1007/s12104-016-9673-z. Epub 2016 Feb 9.


Characterization of ERM transactivation domain binding to the ACID/PTOV domain of the Mediator subunit MED25.

Landrieu I, Verger A, Baert JL, Rucktooa P, Cantrelle FX, Dewitte F, Ferreira E, Lens Z, Villeret V, Monté D.

Nucleic Acids Res. 2015 Aug 18;43(14):7110-21. doi: 10.1093/nar/gkv650. Epub 2015 Jun 29.


Conserved Omp85 lid-lock structure and substrate recognition in FhaC.

Maier T, Clantin B, Gruss F, Dewitte F, Delattre AS, Jacob-Dubuisson F, Hiller S, Villeret V.

Nat Commun. 2015 Jun 10;6:7452. doi: 10.1038/ncomms8452.


Virulence regulation with Venus flytrap domains: structure and function of the periplasmic moiety of the sensor-kinase BvgS.

Dupré E, Herrou J, Lensink MF, Wintjens R, Vagin A, Lebedev A, Crosson S, Villeret V, Locht C, Antoine R, Jacob-Dubuisson F.

PLoS Pathog. 2015 Mar 4;11(3):e1004700. doi: 10.1371/journal.ppat.1004700. eCollection 2015 Mar.


A Salmonella type three secretion effector/chaperone complex adopts a hexameric ring-like structure.

Roblin P, Dewitte F, Villeret V, Biondi EG, Bompard C.

J Bacteriol. 2015 Feb 15;197(4):688-98. doi: 10.1128/JB.02294-14. Epub 2014 Nov 17.


Probing the conformation of FhaC with small-angle neutron scattering and molecular modeling.

Gabel F, Lensink MF, Clantin B, Jacob-Dubuisson F, Villeret V, Ebel C.

Biophys J. 2014 Jul 1;107(1):185-96. doi: 10.1016/j.bpj.2014.05.025.


Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches.

Villemagne B, Flipo M, Blondiaux N, Crauste C, Malaquin S, Leroux F, Piveteau C, Villeret V, Brodin P, Villoutreix BO, Sperandio O, Soror SH, Wohlkönig A, Wintjens R, Deprez B, Baulard AR, Willand N.

J Med Chem. 2014 Jun 12;57(11):4876-88. doi: 10.1021/jm500422b. Epub 2014 May 28.


Structure of the secretion domain of HxuA from Haemophilus influenzae.

Baelen S, Dewitte F, Clantin B, Villeret V.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2013 Dec;69(Pt 12):1322-7. doi: 10.1107/S174430911302962X. Epub 2013 Nov 28.


The structural organization of the N-terminus domain of SopB, a virulence factor of Salmonella, depends on the nature of its protein partners.

Roblin P, Lebrun P, Rucktooa P, Dewitte F, Lens Z, Receveur-Brechot V, Raussens V, Villeret V, Bompard C.

Biochim Biophys Acta. 2013 Dec;1834(12):2564-72. doi: 10.1016/j.bbapap.2013.09.014. Epub 2013 Sep 26.


The DivJ, CbrA and PleC system controls DivK phosphorylation and symbiosis in Sinorhizobium meliloti.

Pini F, Frage B, Ferri L, De Nisco NJ, Mohapatra SS, Taddei L, Fioravanti A, Dewitte F, Galardini M, Brilli M, Villeret V, Bazzicalupo M, Mengoni A, Walker GC, Becker A, Biondi EG.

Mol Microbiol. 2013 Oct;90(1):54-71. doi: 10.1111/mmi.12347. Epub 2013 Aug 19.


DNA binding of the cell cycle transcriptional regulator GcrA depends on N6-adenosine methylation in Caulobacter crescentus and other Alphaproteobacteria.

Fioravanti A, Fumeaux C, Mohapatra SS, Bompard C, Brilli M, Frandi A, Castric V, Villeret V, Viollier PH, Biondi EG.

PLoS Genet. 2013 May;9(5):e1003541. doi: 10.1371/journal.pgen.1003541. Epub 2013 May 30.


The Mediator complex subunit MED25 is targeted by the N-terminal transactivation domain of the PEA3 group members.

Verger A, Baert JL, Verreman K, Dewitte F, Ferreira E, Lens Z, de Launoit Y, Villeret V, Monté D.

Nucleic Acids Res. 2013 May;41(9):4847-59. doi: 10.1093/nar/gkt199. Epub 2013 Mar 26.


The level of Ets-1 protein is regulated by poly(ADP-ribose) polymerase-1 (PARP-1) in cancer cells to prevent DNA damage.

Legrand AJ, Choul-Li S, Spriet C, Idziorek T, Vicogne D, Drobecq H, Dantzer F, Villeret V, Aumercier M.

PLoS One. 2013;8(2):e55883. doi: 10.1371/journal.pone.0055883. Epub 2013 Feb 6.


Structural insights into ChpT, an essential dimeric histidine phosphotransferase regulating the cell cycle in Caulobacter crescentus.

Fioravanti A, Clantin B, Dewitte F, Lens Z, Verger A, Biondi EG, Villeret V.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Sep 1;68(Pt 9):1025-9. doi: 10.1107/S1744309112033064. Epub 2012 Aug 29.


Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis.

Flipo M, Willand N, Lecat-Guillet N, Hounsou C, Desroses M, Leroux F, Lens Z, Villeret V, Wohlkönig A, Wintjens R, Christophe T, Kyoung Jeon H, Locht C, Brodin P, Baulard AR, Déprez B.

J Med Chem. 2012 Jul 26;55(14):6391-402. doi: 10.1021/jm300377g. Epub 2012 Jul 17.


Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands.

Carette X, Blondiaux N, Willery E, Hoos S, Lecat-Guillet N, Lens Z, Wohlkönig A, Wintjens R, Soror SH, Frénois F, Dirié B, Villeret V, England P, Lippens G, Deprez B, Locht C, Willand N, Baulard AR.

Nucleic Acids Res. 2012 Apr;40(7):3018-30. doi: 10.1093/nar/gkr1113. Epub 2011 Dec 9.


Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors.

Flipo M, Desroses M, Lecat-Guillet N, Villemagne B, Blondiaux N, Leroux F, Piveteau C, Mathys V, Flament MP, Siepmann J, Villeret V, Wohlkönig A, Wintjens R, Soror SH, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N.

J Med Chem. 2012 Jan 12;55(1):68-83. doi: 10.1021/jm200825u. Epub 2011 Dec 6.


Purification of SUMO-1 modified IκBα and complex formation with NF-κB.

Lens Z, Dewitte F, Van Lint C, de Launoit Y, Villeret V, Verger A.

Protein Expr Purif. 2011 Dec;80(2):211-6. doi: 10.1016/j.pep.2011.06.009. Epub 2011 Jun 25.


Substrate recognition by the POTRA domains of TpsB transporter FhaC.

Delattre AS, Saint N, Clantin B, Willery E, Lippens G, Locht C, Villeret V, Jacob-Dubuisson F.

Mol Microbiol. 2011 Jul;81(1):99-112. doi: 10.1111/j.1365-2958.2011.07680.x. Epub 2011 Jun 14.


Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors.

Flipo M, Desroses M, Lecat-Guillet N, Dirié B, Carette X, Leroux F, Piveteau C, Demirkaya F, Lens Z, Rucktooa P, Villeret V, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N.

J Med Chem. 2011 Apr 28;54(8):2994-3010. doi: 10.1021/jm200076a. Epub 2011 Apr 1.


NMR structure of the human Mediator MED25 ACID domain.

Bontems F, Verger A, Dewitte F, Lens Z, Baert JL, Ferreira E, de Launoit Y, Sizun C, Guittet E, Villeret V, Monté D.

J Struct Biol. 2011 Apr;174(1):245-51. doi: 10.1016/j.jsb.2010.10.011. Epub 2010 Oct 23.


Functional importance of a conserved sequence motif in FhaC, a prototypic member of the TpsB/Omp85 superfamily.

Delattre AS, Clantin B, Saint N, Locht C, Villeret V, Jacob-Dubuisson F.

FEBS J. 2010 Nov;277(22):4755-65. doi: 10.1111/j.1742-4658.2010.07881.x. Epub 2010 Oct 19. Erratum in: FEBS J. 2011 May;278(9):1594.


Periplasmic domain of the sensor-kinase BvgS reveals a new paradigm for the Venus flytrap mechanism.

Herrou J, Bompard C, Wintjens R, Dupré E, Willery E, Villeret V, Locht C, Antoine R, Jacob-Dubuisson F.

Proc Natl Acad Sci U S A. 2010 Oct 5;107(40):17351-5. doi: 10.1073/pnas.1006267107. Epub 2010 Sep 20.


Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator.

Willand N, Desroses M, Toto P, Dirié B, Lens Z, Villeret V, Rucktooa P, Locht C, Baulard A, Deprez B.

ACS Chem Biol. 2010 Nov 19;5(11):1007-13. doi: 10.1021/cb100177g.


Solution structure of the N-terminal transactivation domain of ERM modified by SUMO-1.

Lens Z, Dewitte F, Monté D, Baert JL, Bompard C, Sénéchal M, Van Lint C, de Launoit Y, Villeret V, Verger A.

Biochem Biophys Res Commun. 2010 Aug 13;399(1):104-10. doi: 10.1016/j.bbrc.2010.07.049. Epub 2010 Jul 18.


Structure and plasticity of the peptidyl-prolyl isomerase Par27 of Bordetella pertussis revealed by X-ray diffraction and small-angle X-ray scattering.

Clantin B, Leyrat C, Wohlkönig A, Hodak H, Ribeiro Ede A Jr, Martinez N, Baud C, Smet-Nocca C, Villeret V, Jacob-Dubuisson F, Jamin M.

J Struct Biol. 2010 Mar;169(3):253-65. doi: 10.1016/j.jsb.2009.11.007. Epub 2009 Nov 20.


First structural insights into the TpsB/Omp85 superfamily.

Jacob-Dubuisson F, Villeret V, Clantin B, Delattre AS, Saint N.

Biol Chem. 2009 Aug;390(8):675-84. doi: 10.1515/BC.2009.099. Review.


Phosphorylation of the MET receptor on juxtamembrane tyrosine residue 1001 inhibits its caspase-dependent cleavage.

Deheuninck J, Goormachtigh G, Foveau B, Ji Z, Leroy C, Ancot F, Villeret V, Tulasne D, Fafeur V.

Cell Signal. 2009 Sep;21(9):1455-63. doi: 10.1016/j.cellsig.2009.05.005. Epub 2009 May 18.


Synthetic EthR inhibitors boost antituberculous activity of ethionamide.

Willand N, Dirié B, Carette X, Bifani P, Singhal A, Desroses M, Leroux F, Willery E, Mathys V, Déprez-Poulain R, Delcroix G, Frénois F, Aumercier M, Locht C, Villeret V, Déprez B, Baulard AR.

Nat Med. 2009 May;15(5):537-44. doi: 10.1038/nm.1950. Epub 2009 May 3.


Crystallization and preliminary X-ray diffraction analysis of the peptidylprolyl isomerase Par27 of Bordetella pertussis.

Wohlkönig A, Hodak H, Clantin B, Sénéchal M, Bompard C, Jacob-Dubuisson F, Villeret V.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008 Sep 1;64(Pt 9):809-12. doi: 10.1107/S1744309108024731. Epub 2008 Aug 9.


Deletion of flagellin's hypervariable region abrogates antibody-mediated neutralization and systemic activation of TLR5-dependent immunity.

Nempont C, Cayet D, Rumbo M, Bompard C, Villeret V, Sirard JC.

J Immunol. 2008 Aug 1;181(3):2036-43.


X-ray structure of papaya chitinase reveals the substrate binding mode of glycosyl hydrolase family 19 chitinases.

Huet J, Rucktooa P, Clantin B, Azarkan M, Looze Y, Villeret V, Wintjens R.

Biochemistry. 2008 Aug 12;47(32):8283-91. doi: 10.1021/bi800655u. Epub 2008 Jul 18.


Crystallization and preliminary X-ray analysis of a family 19 glycosyl hydrolase from Carica papaya latex.

Huet J, Azarkan M, Looze Y, Villeret V, Wintjens R.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008 May 1;64(Pt 5):371-4. doi: 10.1107/S1744309108007823. Epub 2008 Apr 5.


Structure-based mechanism of ligand binding for periplasmic solute-binding protein of the Bug family.

Herrou J, Bompard C, Antoine R, Leroy A, Rucktooa P, Hot D, Huvent I, Locht C, Villeret V, Jacob-Dubuisson F.

J Mol Biol. 2007 Nov 2;373(4):954-64. Epub 2007 Aug 19.


Structure of the membrane protein FhaC: a member of the Omp85-TpsB transporter superfamily.

Clantin B, Delattre AS, Rucktooa P, Saint N, Méli AC, Locht C, Jacob-Dubuisson F, Villeret V.

Science. 2007 Aug 17;317(5840):957-61.


Expression and purification in high yield of a functionally active recombinant human Type I inositol(1,4,5)P3 5-phosphatase.

Wohlkönig A, Sénéchal M, Dewitte F, Backers K, Erneux C, Villeret V.

Protein Expr Purif. 2007 Sep;55(1):69-74. Epub 2007 Apr 24.


Crystal structures of two Bordetella pertussis periplasmic receptors contribute to defining a novel pyroglutamic acid binding DctP subfamily.

Rucktooa P, Antoine R, Herrou J, Huvent I, Locht C, Jacob-Dubuisson F, Villeret V, Bompard C.

J Mol Biol. 2007 Jun 29;370(1):93-106. Epub 2007 Apr 25.


Structural analysis of Bordetella pertussis BugE solute receptor in a bound conformation.

Huvent I, Belrhali H, Antoine R, Bompard C, Locht C, Jacob-Dubuisson F, Villeret V.

Acta Crystallogr D Biol Crystallogr. 2006 Nov;62(Pt 11):1375-81. Epub 2006 Oct 18.


Crystallization and preliminary X-ray diffraction analysis of two extracytoplasmic solute receptors of the DctP family from Bordetella pertussis.

Rucktooa P, Huvent I, Antoine R, Lecher S, Jacob-Dubuisson F, Villeret V, Bompard C.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2006 Oct 1;62(Pt 10):970-2. Epub 2006 Sep 19.


The influence of anionic lipids on SHIP2 phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase activity.

Vandeput F, Backers K, Villeret V, Pesesse X, Erneux C.

Cell Signal. 2006 Dec;18(12):2193-9. Epub 2006 May 23.


Secretion signal of the filamentous haemagglutinin, a model two-partner secretion substrate.

Hodak H, Clantin B, Willery E, Villeret V, Locht C, Jacob-Dubuisson F.

Mol Microbiol. 2006 Jul;61(2):368-82. Epub 2006 Jun 12.


Crystallization and preliminary X-ray diffraction studies of the glutaminyl cyclase from Carica papaya latex.

Azarkan M, Clantin B, Bompard C, Belrhali H, Baeyens-Volant D, Looze Y, Villeret V, Wintjens R.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2005 Jan 1;61(Pt 1):59-61. Epub 2004 Oct 23.


Crystal structure of papaya glutaminyl cyclase, an archetype for plant and bacterial glutaminyl cyclases.

Wintjens R, Belrhali H, Clantin B, Azarkan M, Bompard C, Baeyens-Volant D, Looze Y, Villeret V.

J Mol Biol. 2006 Mar 24;357(2):457-70. Epub 2006 Jan 4.


Crystal structure of Bordetella pertussis BugD solute receptor unveils the basis of ligand binding in a new family of periplasmic binding proteins.

Huvent I, Belrhali H, Antoine R, Bompard C, Locht C, Jacob-Dubuisson F, Villeret V.

J Mol Biol. 2006 Mar 3;356(4):1014-26. Epub 2005 Dec 21.


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