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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. Tarantelli C, et al. Among authors: cmiljanovic v. Cancers (Basel). 2019 Jun 4;11(6):775. doi: 10.3390/cancers11060775. Cancers (Basel). 2019. PMID: 31167506 Free PMC article.
First-in human, phase 1, dose-escalation pharmacokinetic and pharmacodynamic study of the oral dual PI3K and mTORC1/2 inhibitor PQR309 in patients with advanced solid tumors (SAKK 67/13).
Wicki A, Brown N, Xyrafas A, Bize V, Hawle H, Berardi S, Cmiljanović N, Cmiljanović V, Stumm M, Dimitrijević S, Herrmann R, Prêtre V, Ritschard R, Tzankov A, Hess V, Childs A, Hierro C, Rodon J, Hess D, Joerger M, von Moos R, Sessa C, Kristeleit R. Wicki A, et al. Among authors: cmiljanovic v. Eur J Cancer. 2018 Jun;96:6-16. doi: 10.1016/j.ejca.2018.03.012. Epub 2018 Apr 13. Eur J Cancer. 2018. PMID: 29660598 Clinical Trial.
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. Tarantelli C, et al. Among authors: cmiljanovic v. Clin Cancer Res. 2018 Jan 1;24(1):120-129. doi: 10.1158/1078-0432.CCR-17-1041. Epub 2017 Oct 24. Clin Cancer Res. 2018. PMID: 29066507
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. Beaufils F, et al. Among authors: cmiljanovic v. J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1. J Med Chem. 2017. PMID: 28829592 Free PMC article.
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. Bohnacker T, et al. Among authors: cmiljanovic v. Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683. Nat Commun. 2017. PMID: 28276440 Free PMC article.
Targeting phosphoinositide 3-kinase: moving towards therapy.
Marone R, Cmiljanovic V, Giese B, Wymann MP. Marone R, et al. Among authors: cmiljanovic v. Biochim Biophys Acta. 2008 Jan;1784(1):159-85. doi: 10.1016/j.bbapap.2007.10.003. Epub 2007 Oct 12. Biochim Biophys Acta. 2008. PMID: 17997386 Review.