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Items: 1 to 20 of 99

1.

Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials.

Fritsch C, Huang A, Chatenay-Rivauday C, Schnell C, Reddy A, Liu M, Kauffmann A, Guthy D, Erdmann D, De Pover A, Furet P, Gao H, Ferretti S, Wang Y, Trappe J, Brachmann SM, Maira SM, Wilson C, Boehm M, Garcia-Echeverria C, Chene P, Wiesmann M, Cozens R, Lehar J, Schlegel R, Caravatti G, Hofmann F, Sellers WR.

Mol Cancer Ther. 2014 May;13(5):1117-29. doi: 10.1158/1535-7163.MCT-13-0865. Epub 2014 Mar 7.

2.

Inhibition of PI3K Pathway Reduces Invasiveness and Epithelial-to-Mesenchymal Transition in Squamous Lung Cancer Cell Lines Harboring PIK3CA Gene Alterations.

Bonelli MA, Cavazzoni A, Saccani F, Alfieri RR, Quaini F, La Monica S, Galetti M, Cretella D, Caffarra C, Madeddu D, Frati C, Lagrasta CA, Falco A, Rossetti P, Fumarola C, Tiseo M, Petronini PG, Ardizzoni A.

Mol Cancer Ther. 2015 Aug;14(8):1916-27. doi: 10.1158/1535-7163.MCT-14-0892. Epub 2015 May 26.

3.

Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.

Maira SM, Pecchi S, Huang A, Burger M, Knapp M, Sterker D, Schnell C, Guthy D, Nagel T, Wiesmann M, Brachmann S, Fritsch C, Dorsch M, Chène P, Shoemaker K, De Pover A, Menezes D, Martiny-Baron G, Fabbro D, Wilson CJ, Schlegel R, Hofmann F, García-Echeverría C, Sellers WR, Voliva CF.

Mol Cancer Ther. 2012 Feb;11(2):317-28. doi: 10.1158/1535-7163.MCT-11-0474. Epub 2011 Dec 21.

4.

The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations.

Tanaka H, Yoshida M, Tanimura H, Fujii T, Sakata K, Tachibana Y, Ohwada J, Ebiike H, Kuramoto S, Morita K, Yoshimura Y, Yamazaki T, Ishii N, Kondoh O, Aoki Y.

Clin Cancer Res. 2011 May 15;17(10):3272-81. doi: 10.1158/1078-0432.CCR-10-2882. Epub 2011 May 10.

5.

Genotype-dependent efficacy of a dual PI3K/mTOR inhibitor, NVP-BEZ235, and an mTOR inhibitor, RAD001, in endometrial carcinomas.

Shoji K, Oda K, Kashiyama T, Ikeda Y, Nakagawa S, Sone K, Miyamoto Y, Hiraike H, Tanikawa M, Miyasaka A, Koso T, Matsumoto Y, Wada-Hiraike O, Kawana K, Kuramoto H, McCormick F, Aburatani H, Yano T, Kozuma S, Taketani Y.

PLoS One. 2012;7(5):e37431. doi: 10.1371/journal.pone.0037431. Epub 2012 May 25.

6.

The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells.

Musi E, Ambrosini G, de Stanchina E, Schwartz GK.

Mol Cancer Ther. 2014 May;13(5):1044-53. doi: 10.1158/1535-7163.MCT-13-0550. Epub 2014 Feb 21. Erratum in: Mol Cancer Ther. 2014 Sep;13(9):2250.

7.

Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor.

Juric D, Castel P, Griffith M, Griffith OL, Won HH, Ellis H, Ebbesen SH, Ainscough BJ, Ramu A, Iyer G, Shah RH, Huynh T, Mino-Kenudson M, Sgroi D, Isakoff S, Thabet A, Elamine L, Solit DB, Lowe SW, Quadt C, Peters M, Derti A, Schegel R, Huang A, Mardis ER, Berger MF, Baselga J, Scaltriti M.

Nature. 2015 Feb 12;518(7538):240-4. doi: 10.1038/nature13948. Epub 2014 Nov 17.

8.

Phosphoinositide 3-kinase (PI3K) pathway alterations are associated with histologic subtypes and are predictive of sensitivity to PI3K inhibitors in lung cancer preclinical models.

Spoerke JM, O'Brien C, Huw L, Koeppen H, Fridlyand J, Brachmann RK, Haverty PM, Pandita A, Mohan S, Sampath D, Friedman LS, Ross L, Hampton GM, Amler LC, Shames DS, Lackner MR.

Clin Cancer Res. 2012 Dec 15;18(24):6771-83. doi: 10.1158/1078-0432.CCR-12-2347. Epub 2012 Nov 7.

9.

Dual targeting of phosphoinositide 3-kinase and mammalian target of rapamycin using NVP-BEZ235 as a novel therapeutic approach in human ovarian carcinoma.

Santiskulvong C, Konecny GE, Fekete M, Chen KY, Karam A, Mulholland D, Eng C, Wu H, Song M, Dorigo O.

Clin Cancer Res. 2011 Apr 15;17(8):2373-84. doi: 10.1158/1078-0432.CCR-10-2289. Epub 2011 Mar 3.

10.

Mutations in the phosphatidylinositol-3-kinase pathway predict for antitumor activity of the inhibitor PX-866 whereas oncogenic Ras is a dominant predictor for resistance.

Ihle NT, Lemos R Jr, Wipf P, Yacoub A, Mitchell C, Siwak D, Mills GB, Dent P, Kirkpatrick DL, Powis G.

Cancer Res. 2009 Jan 1;69(1):143-50. doi: 10.1158/0008-5472.CAN-07-6656.

11.

mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer.

Elkabets M, Vora S, Juric D, Morse N, Mino-Kenudson M, Muranen T, Tao J, Campos AB, Rodon J, Ibrahim YH, Serra V, Rodrik-Outmezguine V, Hazra S, Singh S, Kim P, Quadt C, Liu M, Huang A, Rosen N, Engelman JA, Scaltriti M, Baselga J.

Sci Transl Med. 2013 Jul 31;5(196):196ra99. doi: 10.1126/scitranslmed.3005747.

12.

BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models.

Liu N, Rowley BR, Bull CO, Schneider C, Haegebarth A, Schatz CA, Fracasso PR, Wilkie DP, Hentemann M, Wilhelm SM, Scott WJ, Mumberg D, Ziegelbauer K.

Mol Cancer Ther. 2013 Nov;12(11):2319-30. doi: 10.1158/1535-7163.MCT-12-0993-T. Epub 2013 Oct 29.

13.

In vitro anticancer activity of PI3K alpha selective inhibitor BYL719 in head and neck cancer.

Keam B, Kim S, Ahn YO, Kim TM, Lee SH, Kim DW, Heo DS.

Anticancer Res. 2015 Jan;35(1):175-82.

PMID:
25550549
14.

Cell cycle-dependent activity of the novel dual PI3K-MTORC1/2 inhibitor NVP-BGT226 in acute leukemia.

Kampa-Schittenhelm KM, Heinrich MC, Akmut F, Rasp KH, Illing B, Döhner H, Döhner K, Schittenhelm MM.

Mol Cancer. 2013 May 24;12:46. doi: 10.1186/1476-4598-12-46.

15.

Disulfiram treatment facilitates phosphoinositide 3-kinase inhibition in human breast cancer cells in vitro and in vivo.

Zhang H, Chen D, Ringler J, Chen W, Cui QC, Ethier SP, Dou QP, Wu G.

Cancer Res. 2010 May 15;70(10):3996-4004. doi: 10.1158/0008-5472.CAN-09-3752. Epub 2010 Apr 27.

16.

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R, Hamon J, Fabbro D, Caravatti G.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007. Epub 2013 May 14. Erratum in: Bioorg Med Chem Lett. 2013 Aug 15;23(16):4723.

PMID:
23726034
17.

BYL719, a new α-specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for the treatment of osteosarcoma.

Gobin B, Huin MB, Lamoureux F, Ory B, Charrier C, Lanel R, Battaglia S, Redini F, Lezot F, Blanchard F, Heymann D.

Int J Cancer. 2015 Feb 15;136(4):784-96. doi: 10.1002/ijc.29040. Epub 2014 Jun 30.

18.

PI3K inhibition results in enhanced estrogen receptor function and dependence in hormone receptor-positive breast cancer.

Bosch A, Li Z, Bergamaschi A, Ellis H, Toska E, Prat A, Tao JJ, Spratt DE, Viola-Villegas NT, Castel P, Minuesa G, Morse N, Rodón J, Ibrahim Y, Cortes J, Perez-Garcia J, Galvan P, Grueso J, Guzman M, Katzenellenbogen JA, Kharas M, Lewis JS, Dickler M, Serra V, Rosen N, Chandarlapaty S, Scaltriti M, Baselga J.

Sci Transl Med. 2015 Apr 15;7(283):283ra51. doi: 10.1126/scitranslmed.aaa4442.

19.

Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells.

Brachmann SM, Hofmann I, Schnell C, Fritsch C, Wee S, Lane H, Wang S, Garcia-Echeverria C, Maira SM.

Proc Natl Acad Sci U S A. 2009 Dec 29;106(52):22299-304. doi: 10.1073/pnas.0905152106. Epub 2009 Dec 10.

20.

Conditional loss of ErbB3 delays mammary gland hyperplasia induced by mutant PIK3CA without affecting mammary tumor latency, gene expression, or signaling.

Young CD, Pfefferle AD, Owens P, Kuba MG, Rexer BN, Balko JM, Sánchez V, Cheng H, Perou CM, Zhao JJ, Cook RS, Arteaga CL.

Cancer Res. 2013 Jul 1;73(13):4075-85. doi: 10.1158/0008-5472.CAN-12-4579. Epub 2013 Apr 30.

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