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10 results on '"Vangrevelinghe, Eric"'

1. NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitro and in vivo

Author

Namoto, Kenji, Baader, Clara, Orsini, Vanessa, Landshammer, Alexandro, Breuer, Eva, Dinh, Kieu Trinh, Ungricht, Rosemarie, Pikiolek, Monika, Laurent, Stephane, Lu, Bo, Aebi, Alexandra, Schönberger, Katharina, Vangrevelinghe, Eric, Evrova, Olivera, Sun, Tianliang, Annunziato, Stefano, Lachal, Julie, Redmond, Emily, Wang, Louis, Wetzel, Kristie, Capodieci, Paola, Turner, Jonathan, Schutzius, Gabi, Unterreiner, Vincent, Trunzer, Markus, Buschmann, Nicole, Behnke, Dirk, Machauer, Rainer, Scheufler, Clemens, Parker, Christian N., Ferro, Magali, Grevot, Armelle, Beyerbach, Armin, Lu, Wei-Yu, Forbes, Stuart J., Wagner, Jürgen, Bouwmeester, Tewis, Liu, Jun, Sohal, Bindi, Sahambi, Sukhdeep, Greenbaum, Linda E., Lohmann, Felix, Hoppe, Philipp, Cong, Feng, Sailer, Andreas W., Ruffner, Heinz, Glatthar, Ralf, Humar, Bostjan, Clavien, Pierre-Alain, Dill, Michael T., George, Elizabeth, Maibaum, Jürgen, Liberali, Prisca, and Tchorz, Jan S.

Published
2024
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2. Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors

Author

Velcicky, Juraj, primary, Janser, Philipp, additional, Gommermann, Nina, additional, Brenneisen, Silke, additional, Ilic, Slavica, additional, Vangrevelinghe, Eric, additional, Stiefl, Nikolaus, additional, Boettcher, Andreas, additional, Arnold, Christelle, additional, Malinverni, Claire, additional, Dawson, Janet, additional, Murgasova, Renata, additional, Desrayaud, Sandrine, additional, Beltz, Karen, additional, Hinniger, Alexandra, additional, Dekker, Carien, additional, Farady, Christopher J., additional, and Mackay, Angela, additional

Published
2024
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3. Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood

Author

Thoma, Gebhard, primary, Decoret, Odile, additional, Vangrevelinghe, Eric, additional, Trunzer, Markus, additional, Decker, Andrea, additional, Orjuela Leon, Anette, additional, Beerli, Christian, additional, Bruno, Sandro, additional, Hauchard, Alice, additional, Paulat, Guido, additional, Zerwes, Hans-Guenter, additional, and Hacini-Rachinel, Feriel, additional

Published
2023
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4. Supplementary Table S2 from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

Author

Andraos, Rita, primary, Qian, Zhiyan, primary, Bonenfant, Débora, primary, Rubert, Joëlle, primary, Vangrevelinghe, Eric, primary, Scheufler, Clemens, primary, Marque, Fanny, primary, Régnier, Catherine H., primary, De Pover, Alain, primary, Ryckelynck, Hugues, primary, Bhagwat, Neha, primary, Koppikar, Priya, primary, Goel, Aviva, primary, Wyder, Lorenza, primary, Tavares, Gisele, primary, Baffert, Fabienne, primary, Pissot-Soldermann, Carole, primary, Manley, Paul W., primary, Gaul, Christoph, primary, Voshol, Hans, primary, Levine, Ross L., primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Radimerski, Thomas, primary

Published
2023
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5. Data from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

Author

Andraos, Rita, primary, Qian, Zhiyan, primary, Bonenfant, Débora, primary, Rubert, Joëlle, primary, Vangrevelinghe, Eric, primary, Scheufler, Clemens, primary, Marque, Fanny, primary, Régnier, Catherine H., primary, De Pover, Alain, primary, Ryckelynck, Hugues, primary, Bhagwat, Neha, primary, Koppikar, Priya, primary, Goel, Aviva, primary, Wyder, Lorenza, primary, Tavares, Gisele, primary, Baffert, Fabienne, primary, Pissot-Soldermann, Carole, primary, Manley, Paul W., primary, Gaul, Christoph, primary, Voshol, Hans, primary, Levine, Ross L., primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Radimerski, Thomas, primary

Published
2023
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6. Supplementary Figures, Methods, and References from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

Author

Andraos, Rita, primary, Qian, Zhiyan, primary, Bonenfant, Débora, primary, Rubert, Joëlle, primary, Vangrevelinghe, Eric, primary, Scheufler, Clemens, primary, Marque, Fanny, primary, Régnier, Catherine H., primary, De Pover, Alain, primary, Ryckelynck, Hugues, primary, Bhagwat, Neha, primary, Koppikar, Priya, primary, Goel, Aviva, primary, Wyder, Lorenza, primary, Tavares, Gisele, primary, Baffert, Fabienne, primary, Pissot-Soldermann, Carole, primary, Manley, Paul W., primary, Gaul, Christoph, primary, Voshol, Hans, primary, Levine, Ross L., primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Radimerski, Thomas, primary

Published
2023
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7. Supplementary Data from Potent and Selective Inhibition of Polycythemia by the Quinoxaline JAK2 Inhibitor NVP-BSK805

Author

Baffert, Fabienne, primary, Régnier, Catherine H., primary, De Pover, Alain, primary, Pissot-Soldermann, Carole, primary, Tavares, Gisele A., primary, Blasco, Francesca, primary, Brueggen, Josef, primary, Chène, Patrick, primary, Drueckes, Peter, primary, Erdmann, Dirk, primary, Furet, Pascal, primary, Gerspacher, Marc, primary, Lang, Marc, primary, Ledieu, David, primary, Nolan, Lynda, primary, Ruetz, Stephan, primary, Trappe, Joerg, primary, Vangrevelinghe, Eric, primary, Wartmann, Markus, primary, Wyder, Lorenza, primary, Hofmann, Francesco, primary, and Radimerski, Thomas, primary

Published
2023
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9. Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist

Author

Betschart, Claudia, primary, Faller, Michael, additional, Zink, Florence, additional, Hemmig, René, additional, Blank, Jutta, additional, Vangrevelinghe, Eric, additional, Bourrel, Marjorie, additional, Glatthar, Ralf, additional, Behnke, Dirk, additional, Barker, Kerstin, additional, Heizmann, Andreas, additional, Angst, Daniela, additional, Nimsgern, Pierre, additional, Jacquier, Sébastien, additional, Junt, Tobias, additional, Zipfel, Géraldine, additional, Ruzzante, Giulia, additional, Loetscher, Pius, additional, Limonta, Sarah, additional, Hawtin, Stuart, additional, Andre, Cedric Bernard, additional, Boulay, Thomas, additional, Feifel, Roland, additional, and Knoepfel, Thomas, additional

Published
2022
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10. NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitroand in vivo

Author

Namoto, Kenji, Baader, Clara, Orsini, Vanessa, Landshammer, Alexandro, Breuer, Eva, Dinh, Kieu Trinh, Ungricht, Rosemarie, Pikiolek, Monika, Laurent, Stephane, Lu, Bo, Aebi, Alexandra, Schönberger, Katharina, Vangrevelinghe, Eric, Evrova, Olivera, Sun, Tianliang, Annunziato, Stefano, Lachal, Julie, Redmond, Emily, Wang, Louis, Wetzel, Kristie, Capodieci, Paola, Turner, Jonathan, Schutzius, Gabi, Unterreiner, Vincent, Trunzer, Markus, Buschmann, Nicole, Behnke, Dirk, Machauer, Rainer, Scheufler, Clemens, Parker, Christian N., Ferro, Magali, Grevot, Armelle, Beyerbach, Armin, Lu, Wei-Yu, Forbes, Stuart J., Wagner, Jürgen, Bouwmeester, Tewis, Liu, Jun, Sohal, Bindi, Sahambi, Sukhdeep, Greenbaum, Linda E., Lohmann, Felix, Hoppe, Philipp, Cong, Feng, Sailer, Andreas W., Ruffner, Heinz, Glatthar, Ralf, Humar, Bostjan, Clavien, Pierre-Alain, Dill, Michael T., George, Elizabeth, Maibaum, Jürgen, Liberali, Prisca, and Tchorz, Jan S.

Abstract

The YAP/Hippo pathway is an organ growth and size regulation rheostat safeguarding multiple tissue stem cell compartments. LATS kinases phosphorylate and thereby inactivate YAP, thus representing a potential direct drug target for promoting tissue regeneration. Here, we report the identification and characterization of the selective small-molecule LATS kinase inhibitor NIBR-LTSi. NIBR-LTSi activates YAP signaling, shows good oral bioavailability, and expands organoids derived from several mouse and human tissues. In tissue stem cells, NIBR-LTSi promotes proliferation, maintains stemness, and blocks differentiation in vitroand in vivo. NIBR-LTSi accelerates liver regeneration following extended hepatectomy in mice. However, increased proliferation and cell dedifferentiation in multiple organs prevent prolonged systemic LATS inhibition, thus limiting potential therapeutic benefit. Together, we report a selective LATS kinase inhibitor agonizing YAP signaling and promoting tissue regeneration in vitroand in vivo, enabling future research on the regenerative potential of the YAP/Hippo pathway.

Published
2024
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