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Page 1
Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Abecassis PY, Lejeune P, Vincent L, Bonnevaux H, Nicolas JP, Bertrand T, Marquette JP, Michot N, Benard T, Below P, Vade I, Chatreaux F, Lebourg G, Pilorge F, Angouillant-Boniface O, Louboutin A, Lengauer C, Schio L. Certal V, et al. Among authors: lengauer c. J Med Chem. 2012 May 24;55(10):4788-805. doi: 10.1021/jm300241b. Epub 2012 May 2. J Med Chem. 2012. PMID: 22524426
Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L. Certal V, et al. Among authors: lengauer c. J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24387221
Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors.
Certal V, Halley F, Virone-Oddos A, Filoche-Rommé B, Carry JC, Gruss-Leleu F, Bertin L, Guizani H, Pilorge F, Richepin P, Karlsson A, Charrier V, Abecassis PY, Vincent L, Nicolas JP, Lengauer C, Garcia-Echeverria C, Schio L. Certal V, et al. Among authors: lengauer c. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1506-10. doi: 10.1016/j.bmcl.2014.02.004. Epub 2014 Feb 8. Bioorg Med Chem Lett. 2014. PMID: 24560540
Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor.
Bonnevaux H, Lemaitre O, Vincent L, Levit MN, Windenberger F, Halley F, Delorme C, Lengauer C, Garcia-Echeverria C, Virone-Oddos A. Bonnevaux H, et al. Among authors: lengauer c. Mol Cancer Ther. 2016 Jul;15(7):1460-71. doi: 10.1158/1535-7163.MCT-15-0496. Epub 2016 May 12. Mol Cancer Ther. 2016. PMID: 27196754
Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kβ inhibitors.
Certal V, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Delorme C, Karlsson A, Abecassis PY, Vincent L, Bonnevaux H, Nicolas JP, Morales R, Michot N, Vade I, Louboutin A, Perron S, Doerflinger G, Tric B, Monget S, Lengauer C, Schio L. Certal V, et al. Among authors: lengauer c. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6381-4. doi: 10.1016/j.bmcl.2012.08.072. Epub 2012 Aug 25. Bioorg Med Chem Lett. 2012. PMID: 22981333
Combination of PIM and JAK2 inhibitors synergistically suppresses MPN cell proliferation and overcomes drug resistance.
Huang SM, Wang A, Greco R, Li Z, Barberis C, Tabart M, Patel V, Schio L, Hurley R, Chen B, Cheng H, Lengauer C, Pollard J, Watters J, Garcia-Echeverria C, Wiederschain D, Adrian F, Zhang J. Huang SM, et al. Among authors: lengauer c. Oncotarget. 2014 May 30;5(10):3362-74. doi: 10.18632/oncotarget.1951. Oncotarget. 2014. PMID: 24830942 Free PMC article.
PIM inhibitors target CD25-positive AML cells through concomitant suppression of STAT5 activation and degradation of MYC oncogene.
Guo Z, Wang A, Zhang W, Levit M, Gao Q, Barberis C, Tabart M, Zhang J, Hoffmann D, Wiederschain D, Rocnik J, Sun F, Murtie J, Lengauer C, Gross S, Zhang B, Cheng H, Patel V, Schio L, Adrian F, Dorsch M, Garcia-Echeverria C, Huang SM. Guo Z, et al. Among authors: lengauer c. Blood. 2014 Sep 11;124(11):1777-89. doi: 10.1182/blood-2014-01-551234. Epub 2014 Jul 8. Blood. 2014. PMID: 25006129 Free article. Clinical Trial.
Evaluation of cancer dependence and druggability of PRP4 kinase using cellular, biochemical, and structural approaches.
Gao Q, Mechin I, Kothari N, Guo Z, Deng G, Haas K, McManus J, Hoffmann D, Wang A, Wiederschain D, Rocnik J, Czechtizky W, Chen X, McLean L, Arlt H, Harper D, Liu F, Majid T, Patel V, Lengauer C, Garcia-Echeverria C, Zhang B, Cheng H, Dorsch M, Huang SA. Gao Q, et al. Among authors: lengauer c. J Biol Chem. 2013 Oct 18;288(42):30125-30138. doi: 10.1074/jbc.M113.473348. Epub 2013 Sep 3. J Biol Chem. 2013. PMID: 24003220 Free PMC article.
PTEN-deficient cancers depend on PIK3CB.
Wee S, Wiederschain D, Maira SM, Loo A, Miller C, deBeaumont R, Stegmeier F, Yao YM, Lengauer C. Wee S, et al. Among authors: lengauer c. Proc Natl Acad Sci U S A. 2008 Sep 2;105(35):13057-62. doi: 10.1073/pnas.0802655105. Epub 2008 Aug 28. Proc Natl Acad Sci U S A. 2008. PMID: 18755892 Free PMC article.
PI3Kα inhibitors that inhibit metastasis.
Schmidt-Kittler O, Zhu J, Yang J, Liu G, Hendricks W, Lengauer C, Gabelli SB, Kinzler KW, Vogelstein B, Huso DL, Zhou S. Schmidt-Kittler O, et al. Among authors: lengauer c. Oncotarget. 2010 Sep;1(5):339-48. doi: 10.18632/oncotarget.166. Oncotarget. 2010. PMID: 21179398 Free PMC article.
143 results