Browse by Basel Contributors ID

2021

Borsari, Chiara and Keles, Erhan and Treyer, Andrea and De Pascale, Martina and Hebeisen, Paul and Hamburger, Matthias and Wymann, Matthias P.. (2021) Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability. RSC Medicinal Chemistry, 12 (4). pp. 579-583.

2017

Breasson, Ludovic and Becattini, Barbara and Sardi, Claudia and Molinaro, Angela and Zani, Fabio and Marone, Romina and Botindari, Fabrizio and Bousquenaud, Melanie and Ruegg, Curzio and Wymann, Matthias P. and Solinas, Giovanni. (2017) PI3K gamma activity in leukocytes promotes adipose tissue inflammation and early-onset insulin resistance during obesity. Science signaling, 10 (488). eaaf2969.

Bohnacker, Thomas and Prota, Andrea E. and Beaufils, Florent and Burke, John E. and Melone, Anna and Inglis, Alison J. and Rageot, Denise and Sele, Alexander M. and Cmiljanovic, Vladimir and Cmiljanovic, Natasa and Bargsten, Katja and Aher, Amol and Akhmanova, Anna and Fernando Diaz, J. and Fabbro, Doriano and Zvelebil, Marketa and Williams, Roger L. and Steinmetz, Michel O. and Wymann, Matthias P.. (2017) Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention. Nature communications, 8. p. 14683.

Beaufils, Florent and Cmiljanovic, Natasa and Cmiljanovic, Vladimir and Bohnacker, Thomas and Melone, Anna and Marone, Romina and Jackson, Eileen and Zhang, Xuxiao and Sele, Alexander and Borsari, Chiara and Mestan, Jurgen and Hebeisen, Paul and Hillmann, Petra and Giese, Bernd and Zvelebil, Marketa and Fabbro, Doriano and Williams, Roger L. and Rageot, Denise and Wymann, Matthias P.. (2017) 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. Journal of Medicinal Chemistry, 60 (17). pp. 7524-7538.

Solinas, G. and Breasson, L. and Becattini, B. and Sardi, C. and Molinaro, A. and Marone, R. and Botindari, F. and Bousquenaud, M. and Ruegg, C. and Wymann, M.. (2017) The role of PI3K gamma signaling within leukocytes in obesity-driven inflammation and insulin resistance. European Journal of Clinical Investigation, 47 (Supplement 1). p. 47.

2016

Beaufils, Florent and Rageot, Denise and Melone, Anna and Sele, Alexander and Lang, Marc and Mestan, Juergen and Ettlin, Robert A. and Hillmann, Petra and Cmiljanovic, Vladimir and Walter, Carolin and Singer, Elisabeth and Nguyen, Hoa H. P. and Hebeisen, Paul and Fabbro, Dorian and Wymann, Matthias P.. (2016) Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620. Cancer Research, 76 (14). 393A.

Beaufils, Florent and Rageot, Denise and Melone, Anna and Lang, Marc and Mestan, Jürgen and Cmiljanovic, Vladimir and Hillmann, Petra and Hebeisen, Paul and Fabbro, Doriano and Wymann, Matthias P.. (2016) Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor. Cancer Research, 76 (14). p. 1336.

Sele, Alexander M. and Rageot, Denise and Bohnacker, Thomas and Beaufils, Florent and Prota, Andrea E. and Steinmetz, Michel O. and Wymann, Matthias P.. (2016) Novel 4-(pyrimidin-2-yl)morpholines targeting the colchicine-binding site of tubulin. Cancer Research, 76 (14). p. 1364.

Lupieri, A. and Smirnova, N. F. and Malet, N. F. and Arnal, J. F. and Martinez, L. O. and Wymann, M. and Hirsch, E. and Gayral, S. and Laffargue, M.. (2016) Absence of PI3Kg leads to increased reendothelialization in mice through modulation of IP-10 secretion. Cardiovascular Research, 111 (Supplement 1). S44.

2015

Cmiljanovic, Vladimir and Ettlin, Robert A. and Beautils, Florent and Dieterle, Walter and Hillmann, Petra and Mestan, Juergen and Melone, Anna and Bohnacker, Thomas and Lang, Marc and Cmiljanovic, Natasa and Giese, Bernd and Hebeisen, Paul and Wymann, Matthias P. and Fabbro, Doriano. (2015) PQR309: A potent, brain-penetrant, dual pan-PI3K/mTOR inhibitor with excellent oral bioavailability and tolerability. Cancer Research, 75 (15). p. 4514.

Tarantelli, Chiara and Gaudio, Eugenio and Kwee, Ivo and Rinaldi, Andrea and Bernasconi, Elena and Cascione, Luciano and Hillmann, Petra and Stathis, Anastasios and Carrassa, Laura and Broggini, Massimo and Stussi, Georg and Fabbro, Doriano and Beaufils, Florent and Melone, Anna and Bohnacker, Thomas and Wymann, Matthias P. and Wicki, Andreas and Zucca, Emanuele and Cmiljanovic, Vladimir and Bertoni, Francesco. (2015) Pre-clinical activity and mechanism of action of the novel dual PI3K/mTOR inhibitor PQR309 in B-cell lymphomas. Cancer Research, 75 (15). p. 2652.

Ettlin, R. and Dieterle, W. and Fabbro, D. and Hebeisen, P. and Beaufils, F. and Hillmann, P. and Stumm, M. and Dimitrijevic, S. and Wymann, M. and Cmiljanovic, N. and Giese, B. and Cmiljanovic, V.. (2015) Early preclinical development of PQR309, a novel balanced dual PI3K/mTOR inhibitor for treatment of various cancer types. Toxicology Letters, 238 (2, Supplement). S337-S338.

Botindari, F. and Wymann, M.. (2015) Dual targeting of PI3K gamma and SHIP1 for a synergistic inhibition of IgE mediated mast cell activation. The FEBS Journal, 282 (1). p. 40.

Bohnacker, Thomas and Beaufils, Florent and Prota, Andrea E. and Burke, John E. and Melone, Anna and Inglis, Alison J. and Fusco, Ludovico and Cmiljanovic, Vladimir and Cmiljanovic, Natasa and Rageot, Denise and Bargsten, Katja and Saez-Calvo, Gonzalo and Pertz, Olivier and Aher, Amol B. and Akhmanova, Anna and Diaz, Fernando J. and Fabbro, Doriano and Zvelebil, Marketa and Williams, Roger L. and Steinmetz, Michel O. and Wymann, Matthias P.. (2015) BKM120-mediated G2 arrest: Structural and functional segregation of off-target action and PI3K inhibition. Cancer Research, 75 (15). p. 671.

Cmiljanovic, Vladimir and Cmiljanovic, Natasa and Marone, Romina and Beaufils, Florent and Zhang, Xuxiao and Zvelebil, Marketa and Hebeisen, Paul and Lang, Marc and Mestan, Juergen and Melone, Anna and Bohnacker, Thomas and Gaudio, Eugenio and Tarantelli, Chiara and Bertoni, Francesco and Ritschard, Reto and Pretre, Vincent and Wicki, Andreas and Fabbro, Doriano and Hillmann, Petra and Williams, Roger and Giese, Bernd and Wymann, Matthias P.. (2015) PQR309: Structure-based design, synthesis and biological evaluation of a novel, selective, dual pan-PI3K/mTOR inhibitor. Cancer Research, 75 (15). p. 2664.

2014

Zimmermann, Mirjam and Cal, Ruben and Janett, Elia and Hoffmann, Viktor and Bochet, Christian G. and Constable, Edwin and Beaufils, Florent and Wymann, Matthias P.. (2014) Cell-Permeant and Photocleavable Chemical Inducer of Dimerization. Angewandte Chemie International Edition, 53 (18). pp. 4717-4720.

Gayral, Stephanie and Garnotel, Roselyne and Castaing-Berthou, Audrey and Blaise, Sebastien and Fougerat, Anne and Berge, Elodie and Montheil, Aurelie and Malet, Nicole and Wymann, Matthias P. and Maurice, Pascal and Debelle, Laurent and Martiny, Laurent and Martinez, Laurent O. and Pshezhetsky, Alexey V. and Duca, Laurent and Laffargue, Muriel. (2014) Elastin-derived peptides potentiate atherosclerosis through the immune Neu1-PI3Kγ pathway. Cardiovascular Research, 102 (1). pp. 118-127.

Smirnova, Natalia F. and Gayral, Stephanie and Pedros, Christophe and Loirand, Gervaise and Vaillant, Nathalie and Malet, Nicole and Kassem, Sahar and Calise, Denis and Goudouneche, Dominique and Wymann, Matthias P. and Hirsch, Emilio and Gadeau, Alain-Pierre and Martinez, Laurent O. and Saoudi, Abdelhadi and Laffargue, Muriel. (2014) Targeting PI3Kgamma activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response. Journal of experimental medicine, 211 (9). pp. 1779-1792.

2013

Erhart, D. and Zimmermann, M. and Jacques, O. and Wittwer, M. B. and Ernst, B. and Constable, E. and Zvelebil, M. and Beaufils, F. and Wymann, M. P.. (2013) Chemical development of intracellular protein heterodimerizers. Chemistry & Biology, 20 (4). pp. 549-557.

Schmidt, C. and Schneble, N. and Muller, J. P. and Bauer, R. and Perino, A. and Marone, R. and Rybalkin, S. D. and Wymann, M. P. and Hirsch, E. and Wetzker, R.. (2013) Phosphoinositide 3-kinase gamma mediates microglial phagocytosis via lipid kinase-independent control of cAMP. Neuroscience, Vol. 233. pp. 44-53.

Barthwal, M. K. and Anzinger, J. J. and Xu, Q. and Bohnacker, T. and Wymann, M. P. and Kruth, H. S.. (2013) Fluid-phase pinocytosis of native low density lipoprotein promotes murine M-CSF differentiated macrophage foam cell formation. PLoS ONE, Vol. 8, H. 3 , e58054.

Collmann, E. and Bohnacker, T. and Marone, R. and Dawson, J. and Rehberg, M. and Stringer, R. and Krombach, F. and Burkhart, C. and Hirsch, E. and Hollingworth, G. J. and Thomas, M. and Wymann, M. P.. (2013) Transient targeting of phosphoinositide 3-kinase acts as a roadblock in mast cells' route to allergy. Journal of allergy and clinical immunology, Vol. 132, H. 4. pp. 959-968.

Walser, R. and Burke, J. E. and Gogvadze, E. and Bohnacker, T. and Zhang, X. and Hess, D. and Kuenzi, P. and Leitges, M. and Hirsch, E. and Williams, R. L. and Laffargue, M. and Wymann, M. P.. (2013) PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control. PLoS Biology, Vol. 11, H. 6 , e1001587.

Wymann, M. P. and Simons, K.. (2013) Membrane dynamics in physiology and disease. The FEBS journal, Vol. 280, H. 12. p. 2729.

Zotes, T. M. and Arias, C. F. and Fuster, J. J. and Spada, R. and Perez-Yague, S. and Hirsch, E. and Wymann, M. and Carrera, A. C. and Andres, V. and Barber, D. F.. (2013) PI3K p110γ deletion attenuates murine atherosclerosis by reducing macrophage proliferation but not polarization or apoptosis in lesions. PLoS ONE, Vol. 8, H. 8 , e72674.

Wymann, M. P. and Solinas, G.. (2013) Inhibition of phosphoinositide 3-kinase γ attenuates inflammation, obesity, and cardiovascular risk factors. Annals of the New York Academy of Sciences, Vol. 1280. pp. 44-47.

2012

Wymann, Matthias. (2012) PI3Ks-drug targets in inflammation and cancer. Subcellular biochemistry, Vol. 58. pp. 111-181.

Anzinger, Joshua J. and Chang, Janet and Xu, Qing and Barthwal, Manoj K. and Bohnacker, Thomas and Wymann, Matthias P. and Kruth, Howard S.. (2012) Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3K?-dependent fluid-phase pinocytosis of native LDL. Journal of Lipid Research, 53 (1). pp. 34-42.

Schaefer, T. and Zajonz, A. and Lorentz, P. and Bohnacker, T. and Wymann, M. P. and Schweighoffer, T.. (2012) Luminal decoration of blood vessels by activated perivasal mast cells in allergic rhinitis. Allergy, Vol. 67, H. 4. pp. 510-520.

Fougerat, A. and Smirnova, N. F. and Gayral, S. and Malet, N. and Hirsch, E. and Wymann, M. P. and Perret, B. and Martinez, L. O. and Douillon, M. and Laffargue, M.. (2012) Key role of PI3Kgamma in monocyte chemotactic protein-1-mediated amplification of PDGF-induced aortic smooth muscle cell migration. British journal of pharmacology, Vol. 166, no. 5. pp. 1643-1653.

Harris, S. J. and Ciuclan, L. and Finan, P. M. and Wymann, M. P. and Walker, C. and Westwick, J. and Ward, S. G. and Thomas, M. J.. (2012) Genetic ablation of PI3Kgamma results in defective IL-17RA signalling in T lymphocytes and increased IL-17 levels. European journal of immunology, Vol. 42, H. 12. pp. 3394-3404.

Reichel, C. A. and Puhr-Westerheide, D. and Zuchtriegel, G. and Uhl, B. and Berberich, N. and Zahler, S. and Wymann, M. P. and Luckow, B. and Krombach, F.. (2012) C-C motif chemokine CCL3 and canonical neutrophil attractants promote neutrophil extravasation through common and distinct mechanisms. Blood, Vol. 120, H. 4. pp. 880-890.

Wymann, M. P. and Schultz, C.. (2012) The chemical biology of phosphoinositide 3-kinases. ChemBioChem, Vol. 13, H. 14. pp. 2022-2035.

2011

Wymann, Matthias P. and Wenk, Markus R.. (2011) Neutral not a loss : phosphoinositides beyond the head group. Nature methods, Vol. 8, H. 3. pp. 219-220.

Becattini, Barbara and Marone, Romina and Zani, Fabio and Arsenijevic, Denis and Seydoux, Josiane and Montani, Jean-Pierre and Dulloo, Abdul G. and Thorens, Bernard and Preitner, Frédéric and Wymann, Matthias P. and Solinas, Giovanni. (2011) PI3Kγ within a nonhematopoietic cell type negatively regulates diet-induced thermogenesis and promotes obesity and insulin resistance. Proceedings of the National Academy of Sciences of the United States of America, Vol. 108, H. 42 , E854-E863.

Perino, A. and Ghigo, A. and Ferrero, E. and Morello, F. and Santulli, G. and Baillie, G. S. and Damilano, F. and Dunlop, A. J. and Pawson, C. and Walser, R. and Levi, R. and Altruda, F. and Silengo, L. and Langeberg, L. K. and Neubauer, G. and Heymans, S. and Lembo, G. and Wymann, M. P. and Wetzker, R. and Houslay, M. D. and Iaccarino, G. and Scott, J. D. and Hirsch, E.. (2011) Integrating cardiac PIP3 and cAMP signaling through a PKA anchoring function of p110γ. Molecular cell, Vol. 42, H. 1. pp. 84-95.

Reichel, C. A. and Lerchenberger, M. and Uhl, B. and Rehberg, M. and Berberich, N. and Zahler, S. and Wymann, M. P. and Krombach, F.. (2011) Plasmin inhibitors prevent leukocyte accumulation and remodeling events in the postischemic microvasculature. PLoS ONE, Vol. 6, H. 2 , e17229.

2010

Ciraolo, Elisa and Morello, Fulvio and Hobbs, Robin M. and Wolf, Frieder and Marone, Romina and Iezzi, Manuela and Lu, Xiaoyun and Mengozzi, Giulio and Altruda, Fiorella and Sorba, Giovanni and Guan, Kaomei and Pandolfi, Pier Paolo and Wymann, Matthias P. and Hirsch, Emilio. (2010) Essential role of the p110beta subunit of phosphoinositide 3-OH kinase in male fertility. Molecular Biology of the Cell, 21 (5). pp. 704-711.

Spitzenberg, Volker and König, Christian and Ulm, Susanne and Marone, Romina and Röpke, Luise and Müller, Jörg P. and Grün, Michael and Bauer, Reinhard and Rubio, Ignacio and Wymann, Matthias Paul and Voigt, Astrid and Wetzker, Reinhard. (2010) Targeting PI3K in neuroblastoma. Journal of cancer research and clinical oncology, Vol. 136, H. 12. pp. 1881-1890.

2009

Marone, Romina and Erhart, Dominik and Mertz, Ann C. and Bohnacker, Thomas and Schnell, Christian and Cmiljanovic, Vladimir and Stauffer, Frédéric and Garcia-Echeverria, Carlos and Giese, Bernd and Maira, Sauveur-Michel and Wymann, Matthias P.. (2009) Targeting melanoma with dual phosphoinosite 3-kinase/mammalian target of rapamycin inhibitors. Molecular Cancer Research, Vol. 7. pp. 601-613.

Barberis, Laura and Pasquali, Christian and Bertschy-Meier, Dominique and Cuccurullo, Alessandra and Costa, Carlotta and Ambrogio, Chiara and Vilbois, Francis and Chiarle, Roberto and Wymann, Matthias and Altruda, Fiorella and Rommel, Christian and Hirsch, Emilio. (2009) Leukocyte transmigration is modulated by chemokine-mediated PI3Kgamma-dependent phosphorylation of vimentin. European journal of immunology, Vol. 39. pp. 1136-1146.

Kurig, Barbara and Shymanets, Aliaksei and Bohnacker, Thomas and Prajwal, and Brock, Carsten and Ahmadian, Mohammad Reza and Schaefer, Michael and Gohla, Antje and Harteneck, Christian and Wymann, Matthias P. and Jeanclos, Elisabeth and Nürnberg, Bernd. (2009) Ras is an indispensable coregulator of the class IB phosphoinositide 3-kinase p87/p110gamma. Proceedings of the National Academy of Sciences of the United States of America, Vol. 106. pp. 20312-20317.

Bohnacker, Thomas and Marone, Romina and Collmann, Emilie and Calvez, Ronan and Hirsch, Emilio and Wymann, Matthias P.. (2009) PI3Kgamma adaptor subunits define coupling to degranulation and cell motility by distinct PtdIns(3,4,5)P3 pools in mast cells. Science signaling : the signal transduction knowledge environment, Vol. 2 , ra27.

Santos-Sierra, Sandra and Deshmukh, Sachin D. and Kalnitski, Julia and Küenzi, Peter and Wymann, Matthias P. and Golenbock, Douglas T. and Henneke, Philipp. (2009) Mal connects TLR2 to PI3Kinase activation and phagocyte polarization. The EMBO journal, Vol. 28. pp. 2018-2027.

Thomas, Matthew and Edwards, Matthew J. and Sawicka, Elzbieta and Duggan, Nicholas and Hirsch, Emilio and Wymann, Matthias P. and Owen, Charles and Trifilieff, Alexandre and Walker, Christoph and Westwick, John and Finan, Peter. (2009) Essential role of phosphoinositide 3-kinase gamma in eosinophil chemotaxis within acute pulmonary inflammation. Immunology : an official journal of the British Society for Immunology, Vol. 126. pp. 413-422.

2008

Fougerat, A. and Gayral, S. and Gourdy, P. and Schambourg, A. and Rückle, T. and Schwarz, M. K. and Rommel, C. and Hirsch, E. and Arnal, J. F. and Salles, J. P. and Perret, B. and Breton-Douillon, M. and Wymann, M. P. and Laffargue, M.. (2008) Genetic and pharmacological targeting of phosphoinositide 3-kinase-gamma reduces atherosclerosis and favors plaque stability by modulating inflammatory processes. Circulation, Vol. 117, H. 10. pp. 1310-1317.

Marone, R. and Cmiljanovic, V. and Giese, B. and Wymann, M. P.. (2008) Targeting phosphoinositide 3-kinase-Moving towards therapy. Biochimica et biophysica acta, Vol. 1784, H. 1. pp. 159-185.

Ciraolo, E. and Iezzi, M. and Marone, R. and Marengo, S. and Curcio, C. and Costa, C. and Azzolino, O. and Gonella, C. and Rubinetto, C. and Wu, H. and Dastrù, W. and Martin, E. L. and Silengo, L. and Altruda, F. and Turco, E. and Lanzetti, L. and Musiani, P. and Rückle, T. and Rommel, C. and Backer, J. M. and Forni, G. and Wymann, M. P. and Hirsch, E.. (2008) Phosphoinositide 3-kinase p110beta activity : key role in metabolism and mammary gland cancer but not development. Science signaling, Vol. 1, H. 36 , ra3.

Wymann, M. P. and Schneiter, R.. (2008) Lipid signalling in disease. Nature reviews. Molecular cell biology, Vol. 9, H. 2. pp. 162-176.

Hui, Rosaline C.-Y. and Gomes, Ana R. and Constantinidou, Demetra and Costa, Joana R. and Karadedou, Christina T. and Fernandez de Mattos, Silvia and Wymann, Matthias P. and Brosens, Jan J. and Schulze, Almut and Lam, Eric W.-F.. (2008) The forkhead transcription factor FOXO3a increases phosphoinositide-3 kinase/Akt activity in drug-resistant leukemic cells through induction of PIK3CA expression. Molecular and Cellular Biology, 28 (19). pp. 5886-5898.