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Items: 14

1.

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
2.

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.

3.

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
4.

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.

5.

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.

6.

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.

7.

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
8.

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.

9.

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
10.

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.

11.

Activation of the PI3K pathway increases TLR-induced TNF-α and IL-6 but reduces IL-1β production in mast cells.

Hochdörfer T, Kuhny M, Zorn CN, Hendriks RW, Vanhaesebroeck B, Bohnacker T, Krystal G, Huber M.

Cell Signal. 2011 May;23(5):866-75. doi: 10.1016/j.cellsig.2011.01.012. Epub 2011 Jan 22.

PMID:
21262348
12.

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.

13.

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.

14.

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.

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