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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. 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.
Chemical development of intracellular protein heterodimerizers.
Erhart D, Zimmermann M, Jacques O, Wittwer MB, Ernst B, Constable E, Zvelebil M, Beaufils F, Wymann MP. Erhart D, et al. Among authors: beaufils f. Chem Biol. 2013 Apr 18;20(4):549-57. doi: 10.1016/j.chembiol.2013.03.010. Chem Biol. 2013. PMID: 23601644
Cell-permeant and photocleavable chemical inducer of dimerization.
Zimmermann M, Cal R, Janett E, Hoffmann V, Bochet CG, Constable E, Beaufils F, Wymann MP. Zimmermann M, et al. Among authors: beaufils f. Angew Chem Int Ed Engl. 2014 Apr 25;53(18):4717-20. doi: 10.1002/anie.201310969. Epub 2014 Mar 26. Angew Chem Int Ed Engl. 2014. PMID: 24677313 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: beaufils f. Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683. Nat Commun. 2017. PMID: 28276440 Free PMC article.
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: beaufils f. 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
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. Brandt C, et al. Among authors: beaufils f. Neuropharmacology. 2018 Sep 15;140:107-120. doi: 10.1016/j.neuropharm.2018.08.002. Epub 2018 Aug 3. Neuropharmacology. 2018. PMID: 30081001
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. Rageot D, et al. Among authors: beaufils f. J Med Chem. 2018 Nov 21;61(22):10084-10105. doi: 10.1021/acs.jmedchem.8b01262. Epub 2018 Nov 14. J Med Chem. 2018. PMID: 30359003 Free article.
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: beaufils f. Cancers (Basel). 2019 Jun 4;11(6):775. doi: 10.3390/cancers11060775. Cancers (Basel). 2019. PMID: 31167506 Free PMC article.
(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase.
Rageot D, Bohnacker T, Keles E, McPhail JA, Hoffmann RM, Melone A, Borsari C, Sriramaratnam R, Sele AM, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Burke JE, Wymann MP. Rageot D, et al. Among authors: beaufils f. J Med Chem. 2019 Jul 11;62(13):6241-6261. doi: 10.1021/acs.jmedchem.9b00525. Epub 2019 Jun 20. J Med Chem. 2019. PMID: 31244112 Free article.
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.
Borsari C, Rageot D, Dall'Asen A, Bohnacker T, Melone A, Sele AM, Jackson E, Langlois JB, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Wymann MP. Borsari C, et al. Among authors: beaufils f. J Med Chem. 2019 Sep 26;62(18):8609-8630. doi: 10.1021/acs.jmedchem.9b00972. Epub 2019 Sep 11. J Med Chem. 2019. PMID: 31465220 Free article.
197 results