Search Results - "Vivat, Valerie"

Make the right measurement: Discovery of an allosteric inhibition site for p300-HAT by Gardberg, Anna S., Huhn, Annissa J., Cummings, Richard, Bommi-Reddy, Archana, Poy, Florence, Setser, Jeremy, Vivat, Valerie, Brucelle, Francois, Wilson, Jonathan

“…Histone acetyltransferases (HATs) and histone deacetylases (HDACs) catalyze the dynamic and reversible acetylation of proteins, an epigenetic regulatory…”
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765 The first-in-class small molecule TREX1 inhibitor CPI-381 demonstrates type I IFN induction and sensitization of tumors to immune checkpoint blockade by Salojin, Costa, Gardberg, Anna, Vivat, Valerie, Cui, Lei, Lauer, Jeffrey, Cantone, Nico, Stuckey, Jacob, Poy, Florence, Almeciga, Ingrid, Cummings, Richard, Wilson, Jonathan, Levell, Julian, Rocnik, Jennifer, Trojer, Patrick

“…BackgroundTREX1 is an exonuclease that functions as a negative regulator of innate immunity. TREX1 controls dsDNA sensing in tumor and immune cells by…”
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Synergistic activation of human pregnane X receptor by binary cocktails of pharmaceutical and environmental compounds by Delfosse, Vanessa, Dendele, Béatrice, Huet, Tiphaine, Grimaldi, Marina, Boulahtouf, Abdelhay, Gerbal-Chaloin, Sabine, Beucher, Bertrand, Roecklin, Dominique, Muller, Christina, Rahmani, Roger, Cavaillès, Vincent, Daujat-Chavanieu, Martine, Vivat, Valérie, Pascussi, Jean-Marc, Balaguer, Patrick, Bourguet, William

“…Humans are chronically exposed to multiple exogenous substances, including environmental pollutants, drugs and dietary components. Many of these compounds are…”
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Activation of RXR-PPAR heterodimers by organotin environmental endocrine disruptors by le Maire, Albane, Grimaldi, Marina, Roecklin, Dominique, Dagnino, Sonia, Vivat-Hannah, Valérie, Balaguer, Patrick, Bourguet, William

“…The nuclear receptor retinoid X receptor‐α (RXR‐α)–peroxisome proliferator‐activated receptor‐γ (PPAR‐γ) heterodimer was recently reported to have a crucial…”
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Native MS: an 'ESI' way to support structure- and fragment-based drug discovery by Vivat Hannah, Valerie, Atmanene, C, Zeyer, D, Van Dorsselaer, A, Sanglier-Cianférani, Sarah

“…The success of early drug-discovery programs depends on the adequate combination of complementary and orthogonal technologies allowing hit/lead compounds to be…”
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Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism by Marcotte, Douglas, Zeng, Weike, Hus, Jean-Christophe, McKenzie, Andres, Hession, Cathy, Jin, Ping, Bergeron, Chris, Lugovskoy, Alexey, Enyedy, Istvan, Cuervo, Hernan, Wang, Deping, Atmanene, Cédric, Roecklin, Dominique, Vecchi, Malgorzata, Vivat, Valérie, Kraemer, Joachim, Winkler, Dirk, Hong, Victor, Chao, Jianhua, Lukashev, Matvey, Silvian, Laura

“…Keap1 binds to the Nrf2 transcription factor to promote its degradation, resulting in the loss of gene products that protect against oxidative stress. While…”
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Interplay of Protein Disorder in Retinoic Acid Receptor Heterodimer and Its Corepressor Regulates Gene Expression by Cordeiro, Tiago N., Sibille, Nathalie, Germain, Pierre, Barthe, Philippe, Boulahtouf, Abdelhay, Allemand, Fréderic, Bailly, Rémy, Vivat, Valérie, Ebel, Christine, Barducci, Alessandro, Bourguet, William, le Maire, Albane, Bernadó, Pau

“…In its unliganded form, the retinoic acid receptor (RAR) in heterodimer with the retinoid X receptor (RXR) exerts a strong repressive activity facilitated by…”
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Design and in vitro characterization of RXR variants as tools to investigate the biological role of endogenous rexinoids by le Maire, Albane, Rey, Martial, Vivat, Valérie, Guée, Laura, Blanc, Pauline, Malosse, Christian, Chamot-Rooke, Julia, Germain, Pierre, Bourguet, William

“…Retinoid X receptors (RXRα, β, and γ) are essential members of the nuclear receptor (NR) superfamily of ligand-dependent transcriptional regulators that bind…”
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Biophysical and structural characterization of mono/di-arylated lactosamine derivatives interaction with human galectin-3 by Atmanene, Cédric, Ronin, Céline, Téletchéa, Stéphane, Gautier, François-Moana, Djedaïni-Pilard, Florence, Ciesielski, Fabrice, Vivat, Valérie, Grandjean, Cyrille

“…Combination of biophysical and structural techniques allowed characterizing and uncovering the mechanisms underlying increased binding affinity of lactosamine…”
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An Unexpected Mode Of Binding Defines BMS948 as A Full Retinoic Acid Receptor β (RARβ, NR1B2) Selective Agonist by Nadendla, Eswarkumar, Teyssier, Catherine, Delfosse, Vanessa, Vivat, Valérie, Krishnasamy, Gunasekaran, Gronemeyer, Hinrich, Bourguet, William, Germain, Pierre

“…Retinoic acid is an important regulator of cell differentiation which plays major roles in embryonic development and tissue remodeling. The biological action…”
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One Question, Multiple Answers: Biochemical and Biophysical Screening Methods Retrieve Deviating Fragment Hit Lists by Schiebel, Johannes, Radeva, Nedyalka, Köster, Helene, Metz, Alexander, Krotzky, Timo, Kuhnert, Maren, Diederich, Wibke E., Heine, Andreas, Neumann, Lars, Atmanene, Cedric, Roecklin, Dominique, Vivat-Hannah, Valérie, Renaud, Jean-Paul, Meinecke, Robert, Schlinck, Nina, Sitte, Astrid, Popp, Franziska, Zeeb, Markus, Klebe, Gerhard

“…Fragment‐based lead discovery is gaining momentum in drug development. Typically, a hierarchical cascade of several screening techniques is consulted to…”
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Separation of Retinoid X Receptor Homo- and Heterodimerization Functions by Vivat-Hannah, Valerie, Bourguet, William, Gottardis, Marco, Gronemeyer, Hinrich

“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Exploring Key Parameters to Detect Subtle Ligand-Induced Protein Conformational Changes Using Traveling Wave Ion Mobility Mass Spectrometry by Atmanene, Cédric, Petiot-Bécard, Stéphanie, Zeyer, Denis, Van Dorsselaer, Alain, Vivat Hannah, Valérie, Sanglier-Cianférani, Sarah

“…Evidencing subtle conformational transitions in proteins occurring upon small modulator binding usually requires atomic resolution techniques (X-ray…”
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Selective retinoids and rexinoids in cancer therapy and chemoprevention by Zusi, F.Christopher, Lorenzi, Matthew V, Vivat-Hannah, Valerie

“…Natural and synthetic retinoids are effective inhibitors of tumor cell growth in vitro and in vivo. However, the toxicity of natural derivatives of vitamin A…”
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Crystal Structure of a Heterodimeric Complex of RAR and RXR Ligand-Binding Domains by Bourguet, William, Vivat, Valérie, Wurtz, Jean-Marie, Chambon, Pierre, Gronemeyer, Hinrich, Moras, Dino

“…The crystal structure of a heterodimer between the ligand-binding domains (LBDs) of the human RARα bound to a selective antagonist and the constitutively…”
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Characterization of the Interaction between Retinoic Acid Receptor/Retinoid X Receptor (RAR/RXR) Heterodimers and Transcriptional Coactivators through Structural and Fluorescence Anisotropy Studies by Pogenberg, Vivian, Guichou, Jean-François, Vivat-Hannah, Valérie, Kammerer, Sabrina, Pérez, Efrén, Germain, Pierre, de Lera, Angel R., Gronemeyer, Hinrich, Royer, Catherine A., Bourguet, William

“…Retinoid receptors (RARs and RXRs) are ligand-activated transcription factors that regulate the transcription of target genes by recruiting coregulator…”
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Retinoids as therapeutic agents: today and tomorrow by Vivat-Hannah, Valerie, Zusi, F Christopher

“…Retinoids have shown beneficial therapeutic effects in pre-clinical and animal models for multiple pathologic indications, however severe adverse effects,…”
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Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity by Stuckey, Jacob I., Cantone, Nico R., Côté, Alexandre, Arora, Shilpi, Vivat, Valerie, Ramakrishnan, Ashwin, Mertz, Jennifer A., Khanna, Avinash, Brenneman, Jehrod, Gehling, Victor S., Moine, Ludivine, Sims, Robert J., Audia, James E., Trojer, Patrick, Levell, Julian R., Cummings, Richard T.

“…The histone methyltransferase EZH2 has been the target of numerous small-molecule inhibitor discovery efforts over the last 10+ years. Emerging clinical data…”
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Early Drug‐Discovery Efforts towards the Identification of EP300/CBP Histone Acetyltransferase (HAT) Inhibitors by Huhn, Annissa J., Gardberg, Anna S., Poy, Florence, Brucelle, Francois, Vivat, Valerie, Cantone, Nico, Patel, Gaurav, Patel, Chirag, Cummings, Richard, Sims, Robert, Levell, Julian, Audia, James E., Bommi‐Reddy, Archana, Wilson, Jonathan E.

“…EP300 and CBP (KAT3A/3B) are two highly homologous, multidomain, epigenetic coregulators that play central roles in transcription through the acetylation of…”
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Make the right measurement – discovery of an allosteric inhibition site for p300-HAT by Gardberg, Anna S., Wilson, Jonathan, Huhn, Annissa J., Reddy, Archana, Poy, Florence, Setser, Jeremy, Vivat, Valerie, Brucelle, Francois

“…Abstract only…”
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