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Items: 1 to 50 of 97

1.

The Novel TORC1/2 Kinase Inhibitor PQR620 Has Anti-Tumor Activity in Lymphomas as a Single Agent and in Combination with Venetoclax.

Tarantelli C, Gaudio E, Hillmann P, Spriano F, Sartori G, Aresu L, Cascione L, Rageot D, Kwee I, Beaufils F, Zucca E, Stathis A, Wymann MP, Cmiljanovic V, Fabbro D, Bertoni F.

Cancers (Basel). 2019 Jun 4;11(6). pii: E775. doi: 10.3390/cancers11060775.

2.

A class of highly selective inhibitors bind to an active state of PI3Kγ.

Gangadhara G, Dahl G, Bohnacker T, Rae R, Gunnarsson J, Blaho S, Öster L, Lindmark H, Karabelas K, Pemberton N, Tyrchan C, Mogemark M, Wymann MP, Williams RL, Perry MWD, Papavoine T, Petersen J.

Nat Chem Biol. 2019 Apr;15(4):348-357. doi: 10.1038/s41589-018-0215-0. Epub 2019 Feb 4.

PMID:
30718815
3.

New molecular and therapeutic insights into canine diffuse large B-cell lymphoma elucidates the role of the dog as a model for human disease.

Aresu L, Ferraresso S, Marconato L, Cascione L, Napoli S, Gaudio E, Kwee I, Tarantelli C, Testa A, Maniaci C, Ciulli A, Hillmann P, Bohnacker T, Wymann MP, Comazzi S, Milan M, Riondato F, Rovere GD, Giantin M, Giannuzzi D, Bertoni F.

Haematologica. 2019 Jun;104(6):e256-e259. doi: 10.3324/haematol.2018.207027. Epub 2018 Dec 13. No abstract available.

4.

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.

Rageot D, Bohnacker T, Melone A, Langlois JB, Borsari C, Hillmann P, Sele AM, Beaufils F, Zvelebil M, Hebeisen P, Löscher W, Burke J, Fabbro D, Wymann MP.

J Med Chem. 2018 Nov 21;61(22):10084-10105. doi: 10.1021/acs.jmedchem.8b01262. Epub 2018 Nov 14.

PMID:
30359003
5.

The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy.

Brandt C, Hillmann P, Noack A, Römermann K, Öhler LA, Rageot D, Beaufils F, Melone A, Sele AM, Wymann MP, Fabbro D, Löscher W.

Neuropharmacology. 2018 Sep 15;140:107-120. doi: 10.1016/j.neuropharm.2018.08.002. Epub 2018 Aug 3.

PMID:
30081001
6.

PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy.

Tarantelli C, Gaudio E, Arribas AJ, Kwee I, Hillmann P, Rinaldi A, Cascione L, Spriano F, Bernasconi E, Guidetti F, Carrassa L, Pittau RB, Beaufils F, Ritschard R, Rageot D, Sele A, Dossena B, Rossi FM, Zucchetto A, Taborelli M, Gattei V, Rossi D, Stathis A, Stussi G, Broggini M, Wymann MP, Wicki A, Zucca E, Cmiljanovic V, Fabbro D, Bertoni F.

Clin Cancer Res. 2018 Jan 1;24(1):120-129. doi: 10.1158/1078-0432.CCR-17-1041. Epub 2017 Oct 24.

7.

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.

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 RL, Rageot D, Wymann MP.

J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1.

8.

PI3Kγ activity in leukocytes promotes adipose tissue inflammation and early-onset insulin resistance during obesity.

Breasson L, Becattini B, Sardi C, Molinaro A, Zani F, Marone R, Botindari F, Bousquenaud M, Ruegg C, Wymann MP, Solinas G.

Sci Signal. 2017 Jul 18;10(488). pii: eaaf2969. doi: 10.1126/scisignal.aaf2969.

PMID:
28720716
9.

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.

Bohnacker T, Prota AE, Beaufils F, Burke JE, Melone A, Inglis AJ, Rageot D, Sele AM, Cmiljanovic V, Cmiljanovic N, Bargsten K, Aher A, Akhmanova A, Díaz JF, Fabbro D, Zvelebil M, Williams RL, Steinmetz MO, Wymann MP.

Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683.

10.

Targeting PI3Kγ activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response.

Smirnova NF, Gayral S, Pedros C, Loirand G, Vaillant N, Malet N, Kassem S, Calise D, Goudounèche D, Wymann MP, Hirsch E, Gadeau AP, Martinez LO, Saoudi A, Laffargue M.

J Exp Med. 2014 Aug 25;211(9):1779-92. doi: 10.1084/jem.20131276. Epub 2014 Jul 29.

11.

Cell-permeant and photocleavable chemical inducer of dimerization.

Zimmermann M, Cal R, Janett E, Hoffmann V, Bochet CG, Constable E, Beaufils F, Wymann MP.

Angew Chem Int Ed Engl. 2014 Apr 25;53(18):4717-20. doi: 10.1002/anie.201310969. Epub 2014 Mar 26.

12.

Elastin-derived peptides potentiate atherosclerosis through the immune Neu1-PI3Kγ pathway.

Gayral S, Garnotel R, Castaing-Berthou A, Blaise S, Fougerat A, Berge E, Montheil A, Malet N, Wymann MP, Maurice P, Debelle L, Martiny L, Martinez LO, Pshezhetsky AV, Duca L, Laffargue M.

Cardiovasc Res. 2014 Apr 1;102(1):118-27. doi: 10.1093/cvr/cvt336. Epub 2013 Dec 19.

PMID:
24357053
13.

PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control.

Walser R, Burke JE, Gogvadze E, Bohnacker T, Zhang X, Hess D, Küenzi P, Leitges M, Hirsch E, Williams RL, Laffargue M, Wymann MP.

PLoS Biol. 2013;11(6):e1001587. doi: 10.1371/journal.pbio.1001587. Epub 2013 Jun 25.

14.

Transient targeting of phosphoinositide 3-kinase acts as a roadblock in mast cells' route to allergy.

Collmann E, Bohnacker T, Marone R, Dawson J, Rehberg M, Stringer R, Krombach F, Burkhart C, Hirsch E, Hollingworth GJ, Thomas M, Wymann MP.

J Allergy Clin Immunol. 2013 Oct;132(4):959-68. doi: 10.1016/j.jaci.2013.03.008. Epub 2013 May 14.

PMID:
23683463
15.

Membrane dynamics in physiology and disease.

Wymann MP, Simons K.

FEBS J. 2013 Jun;280(12):2729. doi: 10.1111/febs.12322. Epub 2013 Jun 3. No abstract available.

16.

Chemical development of intracellular protein heterodimerizers.

Erhart D, Zimmermann M, Jacques O, Wittwer MB, Ernst B, Constable E, Zvelebil M, Beaufils F, Wymann MP.

Chem Biol. 2013 Apr 18;20(4):549-57. doi: 10.1016/j.chembiol.2013.03.010.

17.

Inhibition of phosphoinositide 3-kinase γ attenuates inflammation, obesity, and cardiovascular risk factors.

Wymann MP, Solinas G.

Ann N Y Acad Sci. 2013 Mar;1280:44-7. doi: 10.1111/nyas.12037.

PMID:
23551103
18.

Fluid-phase pinocytosis of native low density lipoprotein promotes murine M-CSF differentiated macrophage foam cell formation.

Barthwal MK, Anzinger JJ, Xu Q, Bohnacker T, Wymann MP, Kruth HS.

PLoS One. 2013;8(3):e58054. doi: 10.1371/journal.pone.0058054. Epub 2013 Mar 11.

19.

Phosphoinositide 3-kinase γ mediates microglial phagocytosis via lipid kinase-independent control of cAMP.

Schmidt C, Schneble N, Müller JP, Bauer R, Perino A, Marone R, Rybalkin SD, Wymann MP, Hirsch E, Wetzker R.

Neuroscience. 2013 Mar 13;233:44-53. doi: 10.1016/j.neuroscience.2012.12.036. Epub 2012 Dec 29.

PMID:
23276671
20.

The chemical biology of phosphoinositide 3-kinases.

Wymann MP, Schultz C.

Chembiochem. 2012 Sep 24;13(14):2022-35. doi: 10.1002/cbic.201200089. Epub 2012 Sep 10. Review.

PMID:
22965647
21.

Genetic ablation of PI3Kγ results in defective IL-17RA signalling in T lymphocytes and increased IL-17 levels.

Harris SJ, Ciuclan L, Finan PM, Wymann MP, Walker C, Westwick J, Ward SG, Thomas MJ.

Eur J Immunol. 2012 Dec;42(12):3394-404. doi: 10.1002/eji.201242463. Epub 2012 Oct 1.

22.

C-C motif chemokine CCL3 and canonical neutrophil attractants promote neutrophil extravasation through common and distinct mechanisms.

Reichel CA, Puhr-Westerheide D, Zuchtriegel G, Uhl B, Berberich N, Zahler S, Wymann MP, Luckow B, Krombach F.

Blood. 2012 Jul 26;120(4):880-90. doi: 10.1182/blood-2012-01-402164. Epub 2012 Jun 6.

23.

Luminal decoration of blood vessels by activated perivasal mast cells in allergic rhinitis.

Schaefer T, Zajonz A, Lorentz P, Bohnacker T, Wymann MP, Schweighoffer T.

Allergy. 2012 Apr;67(4):510-20. doi: 10.1111/j.1398-9995.2012.02790.x. Epub 2012 Feb 8.

PMID:
22313335
24.

Key role of PI3Kγ in monocyte chemotactic protein-1-mediated amplification of PDGF-induced aortic smooth muscle cell migration.

Fougerat A, Smirnova NF, Gayral S, Malet N, Hirsch E, Wymann MP, Perret B, Martinez LO, Douillon M, Laffargue M.

Br J Pharmacol. 2012 Jul;166(5):1643-53. doi: 10.1111/j.1476-5381.2012.01866.x.

25.

Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL.

Anzinger JJ, Chang J, Xu Q, Barthwal MK, Bohnacker T, Wymann MP, Kruth HS.

J Lipid Res. 2012 Jan;53(1):34-42. doi: 10.1194/jlr.M018887. Epub 2011 Nov 4.

26.

PI3Kγ within a nonhematopoietic cell type negatively regulates diet-induced thermogenesis and promotes obesity and insulin resistance.

Becattini B, Marone R, Zani F, Arsenijevic D, Seydoux J, Montani JP, Dulloo AG, Thorens B, Preitner F, Wymann MP, Solinas G.

Proc Natl Acad Sci U S A. 2011 Oct 18;108(42):E854-63. doi: 10.1073/pnas.1106698108. Epub 2011 Sep 26.

27.

Integrating cardiac PIP3 and cAMP signaling through a PKA anchoring function of p110γ.

Perino A, Ghigo A, Ferrero E, Morello F, Santulli G, Baillie GS, Damilano F, Dunlop AJ, Pawson C, Walser R, Levi R, Altruda F, Silengo L, Langeberg LK, Neubauer G, Heymans S, Lembo G, Wymann MP, Wetzker R, Houslay MD, Iaccarino G, Scott JD, Hirsch E.

Mol Cell. 2011 Apr 8;42(1):84-95. doi: 10.1016/j.molcel.2011.01.030.

28.

Plasmin inhibitors prevent leukocyte accumulation and remodeling events in the postischemic microvasculature.

Reichel CA, Lerchenberger M, Uhl B, Rehberg M, Berberich N, Zahler S, Wymann MP, Krombach F.

PLoS One. 2011 Feb 22;6(2):e17229. doi: 10.1371/journal.pone.0017229.

29.

Neutral not a loss: phosphoinositides beyond the head group.

Wymann MP, Wenk MR.

Nat Methods. 2011 Mar;8(3):219-20. doi: 10.1038/nmeth0311-219. No abstract available.

PMID:
21358625
30.

Targeting PI3K in neuroblastoma.

Spitzenberg V, König C, Ulm S, Marone R, Röpke L, Müller JP, Grün M, Bauer R, Rubio I, Wymann MP, Voigt A, Wetzker R.

J Cancer Res Clin Oncol. 2010 Dec;136(12):1881-90. doi: 10.1007/s00432-010-0847-2. Epub 2010 Mar 12.

PMID:
20224967
31.

Essential role of the p110beta subunit of phosphoinositide 3-OH kinase in male fertility.

Ciraolo E, Morello F, Hobbs RM, Wolf F, Marone R, Iezzi M, Lu X, Mengozzi G, Altruda F, Sorba G, Guan K, Pandolfi PP, Wymann MP, Hirsch E.

Mol Biol Cell. 2010 Mar 1;21(5):704-11. doi: 10.1091/mbc.E09-08-0744. Epub 2010 Jan 6.

32.

Ras is an indispensable coregulator of the class IB phosphoinositide 3-kinase p87/p110gamma.

Kurig B, Shymanets A, Bohnacker T, Prajwal, Brock C, Ahmadian MR, Schaefer M, Gohla A, Harteneck C, Wymann MP, Jeanclos E, Nürnberg B.

Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20312-7. doi: 10.1073/pnas.0905506106. Epub 2009 Nov 11.

33.

Mal connects TLR2 to PI3Kinase activation and phagocyte polarization.

Santos-Sierra S, Deshmukh SD, Kalnitski J, Küenzi P, Wymann MP, Golenbock DT, Henneke P.

EMBO J. 2009 Jul 22;28(14):2018-27. doi: 10.1038/emboj.2009.158. Epub 2009 Jul 2.

34.

PI3Kgamma adaptor subunits define coupling to degranulation and cell motility by distinct PtdIns(3,4,5)P3 pools in mast cells.

Bohnacker T, Marone R, Collmann E, Calvez R, Hirsch E, Wymann MP.

Sci Signal. 2009 Jun 9;2(74):ra27. doi: 10.1126/scisignal.2000259.

35.

Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors.

Marone R, Erhart D, Mertz AC, Bohnacker T, Schnell C, Cmiljanovic V, Stauffer F, Garcia-Echeverria C, Giese B, Maira SM, Wymann MP.

Mol Cancer Res. 2009 Apr;7(4):601-13. doi: 10.1158/1541-7786.MCR-08-0366.

36.

Phosphoinositide 3-kinase p110beta activity: key role in metabolism and mammary gland cancer but not development.

Ciraolo E, Iezzi M, Marone R, Marengo S, Curcio C, Costa C, Azzolino O, Gonella C, Rubinetto C, Wu H, Dastrù W, Martin EL, Silengo L, Altruda F, Turco E, Lanzetti L, Musiani P, Rückle T, Rommel C, Backer JM, Forni G, Wymann MP, Hirsch E.

Sci Signal. 2008 Sep 9;1(36):ra3. doi: 10.1126/scisignal.1161577.

37.

Essential role of phosphoinositide 3-kinase gamma in eosinophil chemotaxis within acute pulmonary inflammation.

Thomas M, Edwards MJ, Sawicka E, Duggan N, Hirsch E, Wymann MP, Owen C, Trifilieff A, Walker C, Westwick J, Finan P.

Immunology. 2009 Mar;126(3):413-22. doi: 10.1111/j.1365-2567.2008.02908.x. Epub 2008 Aug 27.

38.

The forkhead transcription factor FOXO3a increases phosphoinositide-3 kinase/Akt activity in drug-resistant leukemic cells through induction of PIK3CA expression.

Hui RC, Gomes AR, Constantinidou D, Costa JR, Karadedou CT, Fernandez de Mattos S, Wymann MP, Brosens JJ, Schulze A, Lam EW.

Mol Cell Biol. 2008 Oct;28(19):5886-98. doi: 10.1128/MCB.01265-07. Epub 2008 Jul 21.

39.

Genetic and pharmacological targeting of phosphoinositide 3-kinase-gamma reduces atherosclerosis and favors plaque stability by modulating inflammatory processes.

Fougerat A, Gayral S, Gourdy P, Schambourg A, Rückle T, Schwarz MK, Rommel C, Hirsch E, Arnal JF, Salles JP, Perret B, Breton-Douillon M, Wymann MP, Laffargue M.

Circulation. 2008 Mar 11;117(10):1310-7. doi: 10.1161/CIRCULATIONAHA.107.720466. Epub 2008 Feb 11.

PMID:
18268153
40.

Lipid signalling in disease.

Wymann MP, Schneiter R.

Nat Rev Mol Cell Biol. 2008 Feb;9(2):162-76. doi: 10.1038/nrm2335. Review.

PMID:
18216772
41.

Targeting phosphoinositide 3-kinase: moving towards therapy.

Marone R, Cmiljanovic V, Giese B, Wymann MP.

Biochim Biophys Acta. 2008 Jan;1784(1):159-85. Epub 2007 Oct 12. Review.

PMID:
17997386
42.

Inactivation of PI3Kgamma and PI3Kdelta distorts T-cell development and causes multiple organ inflammation.

Ji H, Rintelen F, Waltzinger C, Bertschy Meier D, Bilancio A, Pearce W, Hirsch E, Wymann MP, Rückle T, Camps M, Vanhaesebroeck B, Okkenhaug K, Rommel C.

Blood. 2007 Oct 15;110(8):2940-7. Epub 2007 Jul 12.

43.

A central role for DOCK2 during interstitial lymphocyte motility and sphingosine-1-phosphate-mediated egress.

Nombela-Arrieta C, Mempel TR, Soriano SF, Mazo I, Wymann MP, Hirsch E, Martínez-A C, Fukui Y, von Andrian UH, Stein JV.

J Exp Med. 2007 Mar 19;204(3):497-510. Epub 2007 Feb 26.

44.

GABAA receptor-associated phosphoinositide 3-kinase is required for insulin-induced recruitment of postsynaptic GABAA receptors.

Vetiska SM, Ahmadian G, Ju W, Liu L, Wymann MP, Wang YT.

Neuropharmacology. 2007 Jan;52(1):146-55. Epub 2006 Aug 4.

PMID:
16890252
45.

Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.

Camps M, Rückle T, Ji H, Ardissone V, Rintelen F, Shaw J, Ferrandi C, Chabert C, Gillieron C, Françon B, Martin T, Gretener D, Perrin D, Leroy D, Vitte PA, Hirsch E, Wymann MP, Cirillo R, Schwarz MK, Rommel C.

Nat Med. 2005 Sep;11(9):936-43. Epub 2005 Aug 28.

46.
47.

Susi, a negative regulator of Drosophila PI3-kinase.

Wittwer F, Jaquenoud M, Brogiolo W, Zarske M, Wüstemann P, Fernandez R, Stocker H, Wymann MP, Hafen E.

Dev Cell. 2005 Jun;8(6):817-27.

48.

Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils.

Condliffe AM, Davidson K, Anderson KE, Ellson CD, Crabbe T, Okkenhaug K, Vanhaesebroeck B, Turner M, Webb L, Wymann MP, Hirsch E, Ruckle T, Camps M, Rommel C, Jackson SP, Chilvers ER, Stephens LR, Hawkins PT.

Blood. 2005 Aug 15;106(4):1432-40. Epub 2005 May 5.

49.

Protection from angiotensin II-mediated vasculotoxic and hypertensive response in mice lacking PI3Kgamma.

Vecchione C, Patrucco E, Marino G, Barberis L, Poulet R, Aretini A, Maffei A, Gentile MT, Storto M, Azzolino O, Brancaccio M, Colussi GL, Bettarini U, Altruda F, Silengo L, Tarone G, Wymann MP, Hirsch E, Lembo G.

J Exp Med. 2005 Apr 18;201(8):1217-28. Epub 2005 Apr 11.

50.

Phosphoinositide 3-kinase in disease: timing, location, and scaffolding.

Wymann MP, Marone R.

Curr Opin Cell Biol. 2005 Apr;17(2):141-9. Review.

PMID:
15780590

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