Publications

Solinas, G., Breasson, L., Becattini, B., Sardi, C., Molinaro, A., Marone, R., Botindari, F., Bousquenaud, M., 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. WILEY.   
Breasson, L., Becattini, B., Sardi, C., Molinaro, A., Zani, F., Marone, R., Botindari, F., Bousquenaud, M., Ruegg, C., Wymann, M. P. and Solinas, G. (2017) ‘PI3K gamma activity in leukocytes promotes adipose tissue inflammation and early-onset insulin resistance during obesity’, SCIENCE SIGNALING. AMER ASSOC ADVANCEMENT SCIENCE, 10(488). doi: 10.1126/scisignal.aaf2969.   
Beaufils, F., Cmiljanovic, N., Cmiljanovic, V., Bohnacker, T., Melone, A., Marone, R., Jackson, E., Zhang, X., Sele, A., Borsari, C., Mestan, J., Hebeisen, P., Hillmann, P., Giese, B., Zvelebil, M., Fabbro, D., Williams, R. L., Rageot, D. and Wymann, M. 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. AMER CHEMICAL SOC, 60(17), pp. 7524-7538. doi: 10.1021/acs.jmedchem.7b00930.   
Bohnacker, T., Prota, A. E., Beaufils, F., Burke, J. E., Melone, A., Inglis, A. J., Rageot, D., Sele, A. M., Cmiljanovic, V., Cmiljanovic, N., Bargsten, K., Aher, A., Akhmanova, A., Fernando Diaz, J., Fabbro, D., Zvelebil, M., Williams, R. L., Steinmetz, M. O. and Wymann, M. P. (2017) ‘Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention’, NATURE COMMUNICATIONS. NATURE PUBLISHING GROUP, 8. doi: 10.1038/ncomms14683.   
Beaufils, F., Cmiljanovic, N., Cmiljanovic, V., Bohnacker, T., Melone, A., Marone, R., Jackson, E., Zhang, X., Sele, A., Borsari, C., Mestan, J., Hebeisen, P., Hillmann, P., Giese, B., Zvelebil, M., Fabbro, D., Williams, R. L., Rageot, D. and Wymann, M. 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’, Figshare. doi: 10.1021/acs.jmedchem.7b00930.s001.   
Beaufils, F., Rageot, D., Melone, A., Lang, M., Mestan, J., Cmiljanovic, V., Hillmann, P., Hebeisen, P., Fabbro, D. and Wymann, M. P. (2016) ‘Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor’, CANCER RESEARCH. AMER ASSOC CANCER RESEARCH. doi: 10.1158/1538-7445.AM2016-1336.   
Sele, A. M., Rageot, D., Bohnacker, T., Beaufils, F., Prota, A. E., Steinmetz, M. O. and Wymann, M. P. (2016) ‘Novel 4-(pyrimidin-2-yl)morpholines targeting the colchicine-binding site of tubulin’, CANCER RESEARCH. AMER ASSOC CANCER RESEARCH. doi: 10.1158/1538-7445.AM2016-1364.   
Lupieri, A., Smirnova, N. F., Malet, N. F., Arnal, J. F., Martinez, L. O., Wymann, M., Hirsch, E., Gayral, S. and Laffargue, M. (2016) ‘Absence of PI3Kg leads to increased reendothelialization in mice through modulation of IP-10 secretion’, CARDIOVASCULAR RESEARCH. OXFORD UNIV PRESS. doi: 10.1093/cvr/cvw137.   
Beaufils, F., Rageot, D., Melone, A., Sele, A., Lang, M., Mestan, J., Ettlin, R. A., Hillmann, P., Cmiljanovic, V., Walter, C., Singer, E., Nguyen, H. H. P., Hebeisen, P., Fabbro, D. and Wymann, M. P. (2016) ‘Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620’, CANCER RESEARCH. AMER ASSOC CANCER RESEARCH. doi: 10.1158/1538-7445.AM2016-393A.   
Botindari, F. and Wymann, M. (2015) ‘Dual targeting of PI3K gamma and SHIP1 for a synergistic inhibition of IgE mediated mast cell activation’, FEBS JOURNAL. WILEY-BLACKWELL.   
Tarantelli, C., Gaudio, E., Kwee, I., Rinaldi, A., Bernasconi, E., Cascione, L., Hillmann, P., Stathis, A., Carrassa, L., Broggini, M., Stussi, G., Fabbro, D., Beaufils, F., Melone, A., Bohnacker, T., Wymann, M. P., Wicki, A., Zucca, E., Cmiljanovic, V. and Bertoni, F. (2015) ‘Pre-clinical activity and mechanism of action of the novel dual PI3K/mTOR inhibitor PQR309 in B-cell lymphomas’, CANCER RESEARCH. AMER ASSOC CANCER RESEARCH. doi: 10.1158/1538-7445.AM2015-2652.   
Cmiljanovic, V., Cmiljanovic, N., Marone, R., Beaufils, F., Zhang, X., Zvelebil, M., Hebeisen, P., Lang, M., Mestan, J., Melone, A., Bohnacker, T., Gaudio, E., Tarantelli, C., Bertoni, F., Ritschard, R., Pretre, V., Wicki, A., Fabbro, D., Hillmann, P., Williams, R., Giese, B. and Wymann, M. P. (2015) ‘PQR309: Structure-based design, synthesis and biological evaluation of a novel, selective, dual pan-PI3K/mTOR inhibitor’, CANCER RESEARCH. AMER ASSOC CANCER RESEARCH. doi: 10.1158/1538-7445.AM2015-2664.   
Bohnacker, T., Beaufils, F., Prota, A. E., Burke, J. E., Melone, A., Inglis, A. J., Fusco, L., Cmiljanovic, V., Cmiljanovic, N., Rageot, D., Bargsten, K., Saez-Calvo, G., Pertz, O., Aher, A. B., Akhmanova, A., Diaz, F. J., Fabbro, D., Zvelebil, M., Williams, R. L., Steinmetz, M. O. and Wymann, M. P. (2015) ‘BKM120-mediated G2 arrest: Structural and functional segregation of off-target action and PI3K inhibition’, CANCER RESEARCH. AMER ASSOC CANCER RESEARCH. doi: 10.1158/1538-7445.AM2015-671.   
Ettlin, R., Dieterle, W., Fabbro, D., Hebeisen, P., Beaufils, F., Hillmann, P., Stumm, M., Dimitrijevic, S., Wymann, M., Cmiljanovic, N., 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. ELSEVIER IRELAND LTD. doi: 10.1016/j.toxlet.2015.08.963.   
Cmiljanovic, V., Ettlin, R. A., Beautils, F., Dieterle, W., Hillmann, P., Mestan, J., Melone, A., Bohnacker, T., Lang, M., Cmiljanovic, N., Giese, B., Hebeisen, P., Wymann, M. P. and Fabbro, D. (2015) ‘PQR309: A potent, brain-penetrant, dual pan-PI3K/mTOR inhibitor with excellent oral bioavailability and tolerability’, CANCER RESEARCH. AMER ASSOC CANCER RESEARCH. doi: 10.1158/1538-7445.AM2015-4514.   
Zimmermann, M., Cal, R., Janett, E., Hoffmann, V., Bochet, C. G., Constable, E., Beaufils, F. and Wymann, M. P. (2014) ‘Cell-Permeant and Photocleavable Chemical Inducer of Dimerization’, Angewandte Chemie International Edition. Wiley, 53(18), pp. 4717-4720. doi: 10.1002/anie.201310969.   edoc
Gayral, S., Garnotel, R., Castaing-Berthou, A., Blaise, S., Fougerat, A., Berge, E., Montheil, A., Malet, N., Wymann, M. P., Maurice, P., Debelle, L., Martiny, L., Martinez, L. O., Pshezhetsky, A. V., Duca, L. and Laffargue, M. (2014) ‘Elastin-derived peptides potentiate atherosclerosis through the immune Neu1-PI3Kγ pathway’, Cardiovascular research, 102(1), pp. 118-127. doi: 10.1093/cvr/cvt336.   
Smirnova, N. F., Gayral, S., Pedros, C., Loirand, G., Vaillant, N., Malet, N., Kassem, S., Calise, D., Goudouneche, D., Wymann, M. P., Hirsch, E., Gadeau, A. P., Martinez, L. O., Saoudi, A. and Laffargue, M. (2014) ‘Targeting PI3Kgamma activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response’, J Exp Med, 211(9), pp. 1779-1792. doi: 10.1084/jem.20131276.   
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. Blackwell Publishing, Vol. 1280, pp. 44-47. doi: 10.1111/nyas.12037.   edoc
Zotes, T. M., Arias, C. F., Fuster, J. J., Spada, R., Perez-Yague, S., Hirsch, E., Wymann, M., Carrera, A. C., 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. Public Library of Science, Vol. 8, H. 8 , e72674. doi: 10.1371/journal.pone.0072674.   edoc
Barthwal, M. K., Anzinger, J. J., Xu, Q., Bohnacker, T., 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. Public Library of Science, 8(3), p. e58054. doi: 10.1371/journal.pone.0058054.   edoc
Wymann, M. P. and Simons, K. (2013) ‘Membrane dynamics in physiology and disease’, The FEBS journal. Blackwell, 280(12), p. 2729. doi: 10.1111/febs.12322.   edoc
Walser, R., Burke, J. E., Gogvadze, E., Bohnacker, T., Zhang, X., Hess, D., Kuenzi, P., Leitges, M., Hirsch, E., Williams, R. L., Laffargue, M. and Wymann, M. P. (2013) ‘PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control’, PLoS Biology. Public Library of Science, 11(6), p. e1001587. doi: 10.1371/journal.pbio.1001587.   edoc
Schmidt, C., Schneble, N., Muller, J. P., Bauer, R., Perino, A., Marone, R., Rybalkin, S. D., Wymann, M. P., Hirsch, E. and Wetzker, R. (2013) ‘Phosphoinositide 3-kinase gamma mediates microglial phagocytosis via lipid kinase-independent control of cAMP’, Neuroscience. Elsevier, Vol. 233, pp. 44-53. doi: 10.1016/j.neuroscience.2012.12.036.   edoc
Collmann, E., Bohnacker, T., Marone, R., Dawson, J., Rehberg, M., Stringer, R., Krombach, F., Burkhart, C., Hirsch, E., Hollingworth, G. J., 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. Mosby, 132(4), pp. 959-968. doi: 10.1016/j.jaci.2013.03.008.   edoc
Erhart, D., Zimmermann, M., Jacques, O., Wittwer, M. B., Ernst, B., Constable, E., Zvelebil, M., Beaufils, F. and Wymann, M. P. (2013) ‘Chemical development of intracellular protein heterodimerizers’, Chemistry & Biology. Cell Press, 20(4), pp. 549-557. doi: 10.1016/j.chembiol.2013.03.010.   edoc
Wymann, M. P. and Schultz, C. (2012) ‘The chemical biology of phosphoinositide 3-kinases’, ChemBioChem. Wiley-VCH, 13(14), pp. 2022-2035. doi: 10.1002/cbic.201200089.   edoc
Fougerat, A., Smirnova, N. F., Gayral, S., Malet, N., Hirsch, E., Wymann, M. P., Perret, B., Martinez, L. O., 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. Nature Publishing Group, 166(5), pp. 1643-1653. doi: 10.1111/j.1476-5381.2012.01866.x.   edoc
Reichel, C. A., Puhr-Westerheide, D., Zuchtriegel, G., Uhl, B., Berberich, N., Zahler, S., Wymann, M. P., Luckow, B. and Krombach, F. (2012) ‘C-C motif chemokine CCL3 and canonical neutrophil attractants promote neutrophil extravasation through common and distinct mechanisms’, Blood. American Society of Hematology, 120(4), pp. 880-890. doi: 10.1182/blood-2012-01-402164.   edoc
Harris, S. J., Ciuclan, L., Finan, P. M., Wymann, M. P., Walker, C., Westwick, J., 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. Verl. Chemie, 42(12), pp. 3394-3404. doi: 10.1002/eji.201242463.   edoc