Suchergebnisse - "Leysen, Seppe"

Characterization and small-molecule stabilization of the multisite tandem binding between 14-3-3 and the R domain of CFTR von Stevers, Loes M, Lam, Chan V, Leysen, Seppe F R, Meijer, Femke A, van Scheppingen, Daphne S, de Vries, Rens M J M, Carlile, Graeme W, Milroy, Lech G, Thomas, David Y, Brunsveld, Luc, Ottmann, Christian

“… Cystic fibrosis is a fatal genetic disease, most frequently caused by the retention of the CFTR (cystic fibrosis transmembrane conductance regulator) mutant …”
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Small‐molecule stabilization of the p53 – 14‐3‐3 protein‐protein interaction von Doveston, Richard G., Kuusk, Ave, Andrei, Sebastian A., Leysen, Seppe, Cao, Qing, Castaldi, Maria P., Hendricks, Adam, Brunsveld, Luc, Chen, Hongming, Boyd, Helen, Ottmann, Christian

“… 14‐3‐3 proteins are positive regulators of the tumor suppressor p53, the mutation of which is implicated in many human cancers. Current strategies for …”
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Guards of the great wall: bacterial lysozyme inhibitors von Callewaert, Lien, Van Herreweghe, Joris M., Vanderkelen, Lise, Leysen, Seppe, Voet, Arnout, Michiels, Chris W.

“… Peptidoglycan is the major structural component of the bacterial cell wall. It provides resistance against turgor and its cleavage by hydrolases such as …”
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Designed Spiroketal Protein Modulation von Scheepstra, Marcel, Andrei, Sebastian A., Unver, M. Yagiz, Hirsch, Anna K. H., Leysen, Seppe, Ottmann, Christian, Brunsveld, Luc, Milroy, Lech‐Gustav

“… Spiroketals are structural motifs found in many biologically active natural products, which has stimulated considerable efforts toward their synthesis and …”
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Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation von Sunden, Henrik, Schafer, Anja, Scheepstra, Marcel, Leysen, Seppe, Malo, Marcus, Ma, Jian-Nong, Burstein, Ethan S., Ottmann, Christian, Brunsveld, Luc, Olsson, Roger

“… The nuclear receptor Nurr1 can be activated by RXR. via heterodimerization (RXR Nurr1) and is a promising target for treating neurodegenerative diseases. We …”
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A Natural-Product Switch for a Dynamic Protein Interface von Scheepstra, Marcel, Nieto, Lidia, Hirsch, Anna K. H., Fuchs, Sascha, Leysen, Seppe, Lam, Chan Vinh, in het Panhuis, Leslie, van Boeckel, Constant A. A., Wienk, Hans, Boelens, Rolf, Ottmann, Christian, Milroy, Lech-Gustav, Brunsveld, Luc

“… Small ligands are a powerful way to control the function of protein complexes via dynamic binding interfaces. The classic example is found in gene …”
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Structural characterization of the PliG lysozyme inhibitor family von Leysen, Seppe, Vanderkelen, Lise, Van Asten, Kathleen, Vanheuverzwijn, Steven, Theuwis, Veronique, Michiels, Chris W., Strelkov, Sergei V.

“… Several Gram-negative bacteria protect themselves against the lytic action of host lysozymes by producing specific proteinaceous inhibitors. So far, four …”
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Molecular glues to stabilise protein–protein interactions von Soini, Lorenzo, Leysen, Seppe, Davis, Jeremy, Ottmann, Christian

“… Targeting protein–protein interactions (PPIs) has become a common approach to tackle various diseases whose pathobiology is driven by their mis-regulation in …”
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A biophysical and structural analysis of the interaction of BLNK with 14-3-3 proteins von Soini, Lorenzo, Leysen, Seppe, Davis, Jeremy, Ottmann, Christian

“… [Display omitted] •Phosphorylation of BLNK at Thr152 is important for 14-3-3 binding.•A 14-3-3σ/BLNKpT152 crystal structure confirms the binding …”
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The 14‐3‐3/SLP76 protein–protein interaction in T‐cell receptor signalling: a structural and biophysical characterization von Soini, Lorenzo, Leysen, Seppe, Davis, Jeremy, Westwood, Marta, Ottmann, Christian

“… The SH2 domain‐containing protein of 76 kDa, SLP76, is an important adaptor protein that coordinates a complex protein network downstream of T‐cell receptors …”
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Site-Directed Fragment-Based Screening for the Discovery of Protein-Protein Interaction Stabilizers von Sijbesma, Eline, Hallenbeck, Kenneth K, Leysen, Seppe, de Vink, Pim J, Skóra, Lukasz, Jahnke, Wolfgang, Brunsveld, Luc, Arkin, Michelle R, Ottmann, Christian

“… Modulation of protein-protein interactions (PPIs) by small molecules has emerged as a valuable approach in drug discovery. Compared to direct inhibition, PPI …”
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Molecular basis and dual ligand regulation of tetrameric estrogen receptor α/14-3-3ζ protein complex von Somsen, Bente A., Sijbesma, Eline, Leysen, Seppe, Honzejkova, Karolina, Visser, Emira J., Cossar, Peter J., Obšil, Tomáš, Brunsveld, Luc, Ottmann, Christian

“… Therapeutic strategies targeting nuclear receptors (NRs) beyond their endogenous ligand binding pocket have gained significant scientific interest driven by a …”
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Identification of Two Secondary Ligand Binding Sites in 14-3-3 Proteins Using Fragment Screening von Sijbesma, Eline, Skora, Lukasz, Leysen, Seppe, Brunsveld, Luc, Koch, Uwe, Nussbaumer, Peter, Jahnke, Wolfgang, Ottmann, Christian

“… Proteins typically interact with multiple binding partners, and often different parts of their surfaces are employed to establish these protein-protein …”
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The identification and structural analysis of potential 14‐3‐3 interaction sites on the bone regulator protein Schnurri‐3 von Soini, Lorenzo, Leysen, Seppe, Crabbe, Tom, Davis, Jeremy, Ottmann, Christian

“… 14‐3‐3 proteins regulate many intracellular processes and their ability to bind in subtly different fashions to their numerous partner proteins provides …”
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Identification of molecular glues of the SLP76/14-3-3 protein-protein interaction von Soini, Lorenzo, Redhead, Martin, Westwood, Marta, Leysen, Seppe, Davis, Jeremy, Ottmann, Christian

“… The stabilisation of protein-protein interactions (PPIs) through molecular glues is a novel and promising approach in drug discovery. In stark contrast to …”
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Fragment-based Differential Targeting of PPI Stabilizer Interfaces von Guillory, Xavier, Wolter, Madita, Leysen, Seppe, Neves, Joao Filipe, Kuusk, Ave, Genet, Sylvia, Somsen, Bente, Morrow, John Kenneth, Rivers, Emma, van Beek, Lotte, Patel, Joe, Goodnow, Robert, Schoenherr, Heike, Fuller, Nathan, Cao, Qing, Doveston, Richard G., Brunsveld, Luc, Arkin, Michelle R., Castaldi, Paola, Boyd, Helen, Landrieu, Isabelle, Chen, Hongming, Ottmann, Christian

“… Stabilization of protein-protein interactions (PPIs) holds great potential for therapeutic agents, as illustrated by the successful drugs rapamycin and …”
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A Structural Study of the Cytoplasmic Chaperone Effect of 14-3-3 Proteins on Ataxin-1 von Leysen, Seppe, Burnley, Rebecca Jane, Rodriguez, Elizabeth, Milroy, Lech-Gustav, Soini, Lorenzo, Adamski, Carolyn J., Nitschke, Larissa, Davis, Rachel, Obsil, Tomas, Brunsveld, Lucas, Crabbe, Tom, Zoghbi, Huda Yahya, Ottmann, Christian, Davis, Jeremy Martin

“… [Display omitted] •14-3-3 was postulated to prevent cytoplasmic aggregation of Ataxin-1.•Experimental support for an anti-aggregation effect of 14-3-3 on …”
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Identification of an allosteric binding site for RORγt inhibition von Scheepstra, Marcel, Leysen, Seppe, van Almen, Geert C., Miller, J. Richard, Piesvaux, Jennifer, Kutilek, Victoria, van Eenennaam, Hans, Zhang, Hongjun, Barr, Kenneth, Nagpal, Sunil, Soisson, Stephen M., Kornienko, Maria, Wiley, Kristen, Elsen, Nathaniel, Sharma, Sujata, Correll, Craig C., Trotter, B. Wesley, van der Stelt, Mario, Oubrie, Arthur, Ottmann, Christian, Parthasarathy, Gopal, Brunsveld, Luc

“… RORγt is critical for the differentiation and proliferation of Th17 cells associated with several chronic autoimmune diseases. We report the discovery of a …”
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Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists von Meijer, Femke A., Doveston, Richard G., de Vries, Rens M. J. M., Vos, Gael M., Vos, Alex A. A., Leysen, Seppe, Scheepstra, Marcel, Ottmann, Christian, Milroy, Lech-Gustav, Brunsveld, Luc

“… Retinoic acid receptor-related orphan receptor gamma t (ROR gamma t) is a nuclear receptor associated with the pathogenesis of autoimmune diseases. Allosteric …”
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Characterization of Coding/Noncoding Variants for SHROOM3 in Patients with CKD von Prokop, Jeremy W, Yeo, Nan Cher, Ottmann, Christian, Chhetri, Surya B, Florus, Kacie L, Ross, Emily J, Sosonkina, Nadiya, Link, Brian A, Freedman, Barry I, Coppola, Candice J, McDermott-Roe, Chris, Leysen, Seppe, Milroy, Lech-Gustav, Meijer, Femke A, Geurts, Aron M, Rauscher, 3rd, Frank J, Ramaker, Ryne, Flister, Michael J, Jacob, Howard J, Mendenhall, Eric M, Lazar, Jozef

“… Interpreting genetic variants is one of the greatest challenges impeding analysis of rapidly increasing volumes of genomic data from patients. For example, is …”
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