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Volumn 12, Issue 2, 2010, Pages 87-94

Development of phosphoinositide-3 kinase pathway inhibitors for advanced cancer

Author keywords

Drug development; Phosphoinositide 3 kinase; Targeted therapy

Indexed keywords

1 (1 CYANO 1 METHYLETHYL) 3 METHYL 8 (3 QUINOLINYL)IMIDAZO[4,5 C]QUINOLIN 2(1H,3H) ONE; 17 HYDROXYWORTMANNIN; 2 (1H INDAZOL 4 YL) 6 (4 METHANESULFONYL 1 PIPERAZINYLMETHYL) 4 MORPHOLINOTHIENO[3,2 D]PYRIMIDINE; 2 (4 HYDROXYPHENYL) 4 MORPHOLINOPYRIDO[3',2':4,5]FURO[3,2 D]PYRIMIDINE; 2 MORPHOLINO 8 PHENYLCHROMONE; 4 DIALLYLAMINOMETHYLENE 1,3,4,7,10,11,12,13,14,15,16,17 DODECAHYDRO 6 HYDROXY 1 METHOXYMETHYL 10,13 DIMETHYL 3,7,17 TRIOXO 2 OXACYCLOPENTA[A]PHENANTHREN 11 YL ACETATE; 5 (4 BROMO 2 CHLOROANILINO) 4 FLUORO 1 METHYL 1H BENZIMIDAZOLE 6 CARBOHYDROXAMIC ACID 2 HYDROXYETHYL ESTER; [1 (4 OXO 8 PHENYL 4H 1 BENZOPYRAN 2 YL)MORPHOLINIO]METHOXYSUCCINYLARGINYLGLYCYLASPARTYLSERINE ACETATE; CAL 101; CARBOPLATIN; CISPLATIN; ERLOTINIB; GDC 0980; GEFITINIB; GEMCITABINE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MK 2206; PACLITAXEL; PERIFOSINE; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHOTRANSFERASE INHIBITOR; PROTEIN KINASE B INHIBITOR; PWT 458; UNCLASSIFIED DRUG; WORTMANNIN; XL 147; XL 765;

EID: 77952243758     PISSN: 15233790     EISSN: None     Source Type: Journal    
DOI: 10.1007/s11912-010-0091-6     Document Type: Review
Times cited : (53)

References (54)
  • 1
    • 33746257209 scopus 로고    scopus 로고
    • The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism
    • DOI 10.1038/nrg1879, PII NRG1879
    • JA Engelman L Ji LC Cantley 2006 The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism Nat Rev Genet 7 606 619 10.1038/nrg1879 1:CAS:528:DC%2BD28XmvFCnu7Y%3D 16847462 (Pubitemid 44100518)
    • (2006) Nature Reviews Genetics , vol.7 , Issue.8 , pp. 606-619
    • Engelman, J.A.1    Luo, J.2    Cantley, L.C.3
  • 2
    • 73349138892 scopus 로고    scopus 로고
    • Regulation of tissue growth through nutrient sensing
    • 10.1146/annurev-genet-102108-134815 1:CAS:528:DC%2BD1MXhsF2qtrnF 19694515
    • V Hietakangas SM Cohen 2009 Regulation of tissue growth through nutrient sensing Annu Rev Genet 43 389 410 10.1146/annurev-genet-102108-134815 1:CAS:528:DC%2BD1MXhsF2qtrnF 19694515
    • (2009) Annu Rev Genet , vol.43 , pp. 389-410
    • Hietakangas, V.1    Cohen, S.M.2
  • 3
    • 68249093818 scopus 로고    scopus 로고
    • Targeting the phosphoinositide 3-kinase pathway in cancer
    • 10.1038/nrd2926 1:CAS:528:DC%2BD1MXpt1Wgtb4%3D 19644473 This article provides an extremely informative review on the role of PI3K in cancer. It also reviews therapeutic approaches of targeting the PI3K pathway.
    • P Liu H Cheng TM Roberts JJ Zhao 2009 Targeting the phosphoinositide 3-kinase pathway in cancer Nat Rev Drug Discov 8 627 644 10.1038/nrd2926 1:CAS:528:DC%2BD1MXpt1Wgtb4%3D 19644473 This article provides an extremely informative review on the role of PI3K in cancer. It also reviews therapeutic approaches of targeting the PI3K pathway.
    • (2009) Nat Rev Drug Discov , vol.8 , pp. 627-644
    • Liu, P.1    Cheng, H.2    Roberts, T.M.3    Zhao, J.J.4
  • 4
    • 38149120449 scopus 로고    scopus 로고
    • Targeting phosphoinositide 3-kinase: Moving towards therapy
    • 1:CAS:528:DC%2BD1cXptlerug%3D%3D 17997386 This excellent review thoroughly details the development of PI3K inhibitors.
    • R Marone V Cmiljanovic B Giese MP Wymann 2008 Targeting phosphoinositide 3-kinase: moving towards therapy Biochim Biophys Acta 1784 159 185 1:CAS:528:DC%2BD1cXptlerug%3D%3D 17997386 This excellent review thoroughly details the development of PI3K inhibitors.
    • (2008) Biochim Biophys Acta , vol.1784 , pp. 159-185
    • Marone, R.1    Cmiljanovic, V.2    Giese, B.3    Wymann, M.P.4
  • 5
    • 34249026448 scopus 로고    scopus 로고
    • Binding of Ras to Phosphoinositide 3-Kinase p110α Is Required for Ras- Driven Tumorigenesis in Mice
    • DOI 10.1016/j.cell.2007.03.051, PII S009286740700520X
    • S Gupta AR Ramjaun P Haiko Y Wang, et al. 2007 Binding of ras to phosphoinositide 3-kinase p110alpha is required for ras-driven tumorigenesis in mice Cell 129 957 968 10.1016/j.cell.2007.03.051 1:CAS:528:DC%2BD2sXmsl2qsLc%3D 17540175 (Pubitemid 46802703)
    • (2007) Cell , vol.129 , Issue.5 , pp. 957-968
    • Gupta, S.1    Ramjaun, A.R.2    Haiko, P.3    Wang, Y.4    Warne, P.H.5    Nicke, B.6    Nye, E.7    Stamp, G.8    Alitalo, K.9    Downward, J.10
  • 6
    • 61849126233 scopus 로고    scopus 로고
    • Fine tuning the immune response with PI3K
    • 10.1111/j.1600-065X.2008.00750.x 1:CAS:528:DC%2BD1MXhsFGls7vI 19290933
    • DA Fruman G Bismuth 2009 Fine tuning the immune response with PI3K Immunol Rev 228 253 272 10.1111/j.1600-065X.2008.00750.x 1:CAS:528: DC%2BD1MXhsFGls7vI 19290933
    • (2009) Immunol Rev , vol.228 , pp. 253-272
    • Fruman, D.A.1    Bismuth, G.2
  • 7
    • 54949109808 scopus 로고    scopus 로고
    • PI3K/Akt: Getting it right matters
    • 10.1038/onc.2008.313 1:CAS:528:DC%2BD1cXht12ltLvN 18955974
    • TF Franke 2008 PI3K/Akt: getting it right matters Oncogene 27 6473 6488 10.1038/onc.2008.313 1:CAS:528:DC%2BD1cXht12ltLvN 18955974
    • (2008) Oncogene , vol.27 , pp. 6473-6488
    • Franke, T.F.1
  • 8
    • 26444448463 scopus 로고    scopus 로고
    • The survival kinases Akt and Pim as potential pharmacological targets
    • DOI 10.1172/JCI26273
    • R Amaravadi CB Thompson 2005 The survival kinases Akt and Pim as potential pharmacological targets J Clin Invest 115 2618 2624 10.1172/JCI26273 1:CAS:528:DC%2BD2MXhtVygt7vL 16200194 (Pubitemid 41434384)
    • (2005) Journal of Clinical Investigation , vol.115 , Issue.10 , pp. 2618-2624
    • Amaravadi, R.1    Thompson, C.B.2
  • 9
    • 34347220473 scopus 로고    scopus 로고
    • Defining the Role of mTOR in Cancer
    • DOI 10.1016/j.ccr.2007.05.008, PII S1535610807001511
    • DA Guertin DM Sabatini 2007 Defining the role of mTOR in cancer Cancer Cell 12 9 22 10.1016/j.ccr.2007.05.008 1:CAS:528:DC%2BD2sXotVyqsr0%3D 17613433 (Pubitemid 47001784)
    • (2007) Cancer Cell , vol.12 , Issue.1 , pp. 9-22
    • Guertin, D.A.1    Sabatini, D.M.2
  • 10
    • 51849084360 scopus 로고    scopus 로고
    • The PTEN-PI3K pathway: Of feedbacks and cross-talks
    • 10.1038/onc.2008.247 1:CAS:528:DC%2BD1cXhtFWiurzF 18794886
    • A Carracedo PP Pandolfi 2008 The PTEN-PI3K pathway: of feedbacks and cross-talks Oncogene 27 5527 5541 10.1038/onc.2008.247 1:CAS:528: DC%2BD1cXhtFWiurzF 18794886
    • (2008) Oncogene , vol.27 , pp. 5527-5541
    • Carracedo, A.1    Pandolfi, P.P.2
  • 12
    • 67749122122 scopus 로고    scopus 로고
    • Targeting PI3K signalling in cancer: Opportunities, challenges and limitations
    • 10.1038/nrc2664 1:CAS:528:DC%2BD1MXovFylsrg%3D 19629070
    • JA Engelman 2009 Targeting PI3K signalling in cancer: opportunities, challenges and limitations Nat Rev Cancer 9 550 562 10.1038/nrc2664 1:CAS:528:DC%2BD1MXovFylsrg%3D 19629070
    • (2009) Nat Rev Cancer , vol.9 , pp. 550-562
    • Engelman, J.A.1
  • 13
    • 70749115641 scopus 로고    scopus 로고
    • PI3K regulatory subunits lose control in cancer
    • 10.1016/j.ccr.2009.11.017 1:CAS:528:DC%2BC3cXht1eqsLc%3D 19962660
    • I Martin-Berenjeno B Vanhaesebroeck 2009 PI3K regulatory subunits lose control in cancer Cancer Cell 16 449 450 10.1016/j.ccr.2009.11.017 1:CAS:528:DC%2BC3cXht1eqsLc%3D 19962660
    • (2009) Cancer Cell , vol.16 , pp. 449-450
    • Martin-Berenjeno, I.1    Vanhaesebroeck, B.2
  • 15
    • 51849128358 scopus 로고    scopus 로고
    • Class i PI3K in oncogenic cellular transformation
    • 10.1038/onc.2008.244 1:CAS:528:DC%2BD1cXhtFWiur%2FP 18794883
    • L Zhao PK Vogt 2008 Class I PI3K in oncogenic cellular transformation Oncogene 27 5486 5496 10.1038/onc.2008.244 1:CAS:528:DC%2BD1cXhtFWiur%2FP 18794883
    • (2008) Oncogene , vol.27 , pp. 5486-5496
    • Zhao, L.1    Vogt, P.K.2
  • 16
    • 70749140937 scopus 로고    scopus 로고
    • Somatic mutations in p85alpha promote tumorigenesis through class IA PI3K activation
    • 10.1016/j.ccr.2009.10.016 1:CAS:528:DC%2BC3cXht1eqsbo%3D 19962665
    • BS Jaiswal V Janakiraman NM Kljavin, et al. 2009 Somatic mutations in p85alpha promote tumorigenesis through class IA PI3K activation Cancer Cell 16 463 474 10.1016/j.ccr.2009.10.016 1:CAS:528:DC%2BC3cXht1eqsbo%3D 19962665
    • (2009) Cancer Cell , vol.16 , pp. 463-474
    • Jaiswal, B.S.1    Janakiraman, V.2    Kljavin, N.M.3
  • 18
    • 73349129405 scopus 로고    scopus 로고
    • Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition
    • 10.1073/pnas.0905056106 1:CAS:528:DC%2BD1MXhsFGitrzJ 19850869 This paper demonstrates that combination therapy with PI3K and MEK inhibitors can be effective in EGFR-addicted cancers.
    • AC Faber D Li Y Song, et al. 2009 Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition Proc Natl Acad Sci U S A 106 19503 19508 10.1073/pnas.0905056106 1:CAS:528:DC%2BD1MXhsFGitrzJ 19850869 This paper demonstrates that combination therapy with PI3K and MEK inhibitors can be effective in EGFR-addicted cancers.
    • (2009) Proc Natl Acad Sci U S A , vol.106 , pp. 19503-19508
    • Faber, A.C.1    Li, D.2    Song, Y.3
  • 24
    • 0028170210 scopus 로고
    • A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002)
    • 1:CAS:528:DyaK2cXjtFGit78%3D 8106507
    • CJ Vlahos WF Matter KY Hui RF Brown 1994 A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002) J Biol Chem 269 5241 5248 1:CAS:528:DyaK2cXjtFGit78%3D 8106507
    • (1994) J Biol Chem , vol.269 , pp. 5241-5248
    • Vlahos, C.J.1    Matter, W.F.2    Hui, K.Y.3    Brown, R.F.4
  • 26
    • 33644685228 scopus 로고    scopus 로고
    • The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts
    • 10.1158/1535-7163.MCT-05-0149 1:CAS:528:DC%2BD2MXhtVKnt7nN 16170026
    • NT Ihle G Paine-Murrieta MI Berggren, et al. 2005 The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts Mol Cancer Ther 4 1349 1357 10.1158/1535-7163.MCT- 05-0149 1:CAS:528:DC%2BD2MXhtVKnt7nN 16170026
    • (2005) Mol Cancer Ther , vol.4 , pp. 1349-1357
    • Ihle, N.T.1    Paine-Murrieta, G.2    Berggren, M.I.3
  • 27
    • 76749151758 scopus 로고    scopus 로고
    • Phase i trial of PX-866, a novel phosphoinositide-3-kinase (PI-3K) inhibitor
    • A Jimeno DS Hong S Hecker, et al. 2009 Phase I trial of PX-866, a novel phosphoinositide-3-kinase (PI-3K) inhibitor J Clin Oncol (Meeting Abstracts) 27 3542
    • (2009) J Clin Oncol (Meeting Abstracts) , vol.27 , pp. 3542
    • Jimeno, A.1    Hong, D.S.2    Hecker, S.3
  • 28
    • 23644451118 scopus 로고    scopus 로고
    • PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors
    • 1:CAS:528:DC%2BD28Xitl2rurw%3D 15846106
    • K Yu J Lucas T Zhu, et al. 2005 PWT-458, a novel pegylated-17- hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors Cancer Biol Ther 4 538 545 1:CAS:528:DC%2BD28Xitl2rurw%3D 15846106
    • (2005) Cancer Biol Ther , vol.4 , pp. 538-545
    • Yu, K.1    Lucas, J.2    Zhu, T.3
  • 29
    • 77952243392 scopus 로고    scopus 로고
    • Phase i evaluation of SF1126, a vascular targeted PI3K inhibitor, administered twice weekly IV in patients with refractory solid tumors
    • EG Chiorean D Mahadevan WB Harris, et al. 2009 Phase I evaluation of SF1126, a vascular targeted PI3K inhibitor, administered twice weekly IV in patients with refractory solid tumors J Clin Oncol (Meeting Abstracts) 27 2558
    • (2009) J Clin Oncol (Meeting Abstracts) , vol.27 , pp. 2558
    • Chiorean, E.G.1    Mahadevan, D.2    Harris, W.B.3
  • 30
    • 52449106253 scopus 로고    scopus 로고
    • The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin- 1-ylmethyl)-4-morpholin-4-yl-t hieno[3, 2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class i PI3 kinase for the treatment of cancer
    • 10.1021/jm800295d 1:CAS:528:DC%2BD1cXhtVCmsr7E 18754654
    • AJ Folkes K Ahmadi WK Alderton, et al. 2008 The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl) -4-morpholin-4-yl-t hieno[3, 2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer J Med Chem 51 5522 5532 10.1021/jm800295d 1:CAS:528:DC%2BD1cXhtVCmsr7E 18754654
    • (2008) J Med Chem , vol.51 , pp. 5522-5532
    • Folkes, A.J.1    Ahmadi, K.2    Alderton, W.K.3
  • 31
    • 76749136608 scopus 로고    scopus 로고
    • A first-in-human phase i study to evaluate the pan-PI3K inhibitor GDC-0941 administered QD or BID in patients with advanced solid tumors
    • AJ Wagner DH Von Hoff PM LoRusso, et al. 2009 A first-in-human phase I study to evaluate the pan-PI3K inhibitor GDC-0941 administered QD or BID in patients with advanced solid tumors J Clin Oncol (Meeting Abstracts) 27 3501
    • (2009) J Clin Oncol (Meeting Abstracts) , vol.27 , pp. 3501
    • Wagner, A.J.1    Von Hoff, D.H.2    Lorusso, P.M.3
  • 32
    • 70350155874 scopus 로고    scopus 로고
    • A phase i study evaluating the pharmacokinetics (PK) and pharmacodynamics (PD) of the oral pan-phosphoinositide-3 kinase (PI3K) inhibitor GDC-0941
    • D Sarker R Kristeleit KE Mazina, et al. 2009 A phase I study evaluating the pharmacokinetics (PK) and pharmacodynamics (PD) of the oral pan-phosphoinositide-3 kinase (PI3K) inhibitor GDC-0941 J Clin Oncol (Meeting Abstracts) 27 3538
    • (2009) J Clin Oncol (Meeting Abstracts) , vol.27 , pp. 3538
    • Sarker, D.1    Kristeleit, R.2    Mazina, K.E.3
  • 33
    • 77952238072 scopus 로고    scopus 로고
    • Potentiating the antitumor effects of chemotherapy with the selective PI3K inhibitor XL147
    • P Foster 2007 Potentiating the antitumor effects of chemotherapy with the selective PI3K inhibitor XL147 AACR Meeting Abstracts 2007 C199
    • (2007) AACR Meeting Abstracts , vol.2007 , pp. 199
    • Foster, P.1
  • 34
    • 76749171098 scopus 로고    scopus 로고
    • Phase i dose-escalation study of XL147, a PI3K inhibitor administered orally to patients with solid tumors
    • G Shapiro E Kwak J Baselga, et al. 2009 Phase I dose-escalation study of XL147, a PI3K inhibitor administered orally to patients with solid tumors J Clin Oncol (Meeting Abstracts) 27 3500
    • (2009) J Clin Oncol (Meeting Abstracts) , vol.27 , pp. 3500
    • Shapiro, G.1    Kwak, E.2    Baselga, J.3
  • 35
    • 77952239122 scopus 로고    scopus 로고
    • A phase 1 safety and pharmacokinetic (PK) study of the PI3K inhibitor XL147 (SAR245408) in combination with erlotinib in patients with advanced solid tumors
    • N Faulkner PM LoRusso T Guthrie, et al. 2009 A phase 1 safety and pharmacokinetic (PK) study of the PI3K inhibitor XL147 (SAR245408) in combination with erlotinib in patients with advanced solid tumors Mol Cancer Ther 8 C197
    • (2009) Mol Cancer Ther , vol.8 , pp. 197
    • Faulkner, N.1    Lorusso, P.M.2    Guthrie, T.3
  • 37
    • 70350176755 scopus 로고    scopus 로고
    • A phase i dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics of XL765, a PI3K/TORC1/TORC2 inhibitor administered orally to patients (pts) with advanced solid tumors
    • P LoRusso B Markman J Tabernero, et al. 2009 A phase I dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics of XL765, a PI3K/TORC1/TORC2 inhibitor administered orally to patients (pts) with advanced solid tumors J Clin Oncol (Meeting Abstracts) 27 3502
    • (2009) J Clin Oncol (Meeting Abstracts) , vol.27 , pp. 3502
    • Lorusso, P.1    Markman, B.2    Tabernero, J.3
  • 38
    • 51049109033 scopus 로고    scopus 로고
    • Brueggen J, et al.: Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
    • 10.1158/1535-7163.MCT-08-0017 1:CAS:528:DC%2BD1cXoslCgtb4%3D 18606717
    • S-M Maira 2008 Brueggen J, et al.: Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity Mol Cancer Ther 7 1851 1863 10.1158/1535-7163.MCT-08-0017 1:CAS:528:DC%2BD1cXoslCgtb4%3D 18606717
    • (2008) Mol Cancer Ther , vol.7 , pp. 1851-1863
    • Maira, S.-M.1
  • 39
    • 56449111358 scopus 로고    scopus 로고
    • Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235
    • 10.1158/0008-5472.CAN-08-1740 1:CAS:528:DC%2BD1cXhtlOmt73F 19010894
    • PJ Eichhorn M Gili M Scaltriti, et al. 2008 Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235 Cancer Res 68 9221 9230 10.1158/0008-5472.CAN-08-1740 1:CAS:528:DC%2BD1cXhtlOmt73F 19010894
    • (2008) Cancer Res , vol.68 , pp. 9221-9230
    • Eichhorn, P.J.1    Gili, M.2    Scaltriti, M.3
  • 40
    • 50049105906 scopus 로고    scopus 로고
    • PI3K enters beta-testing
    • 10.1016/j.cmet.2008.08.011 1:CAS:528:DC%2BD1cXhtFejurfF 18762017
    • AJ Shaywitz KD Courtney A Patnaik LC Cantley 2008 PI3K enters beta-testing Cell Metabolism 8 179 181 10.1016/j.cmet.2008.08.011 1:CAS:528:DC%2BD1cXhtFejurfF 18762017
    • (2008) Cell Metabolism , vol.8 , pp. 179-181
    • Shaywitz, A.J.1    Courtney, K.D.2    Patnaik, A.3    Cantley, L.C.4
  • 41
    • 33750459743 scopus 로고    scopus 로고
    • A selective inhibitor of the p110δ isoform of PI 3-kinase inhibits AML cell proliferation and survival and increases the cytotoxic effects of VP16
    • DOI 10.1038/sj.onc.1209670, PII 1209670
    • C Billottet VL Grandage RE Gale, et al. 2006 A selective inhibitor of the p110delta isoform of PI 3-kinase inhibits AML cell proliferation and survival and increases the cytotoxic effects of VP16 Oncogene 25 6648 6659 10.1038/sj.onc.1209670 1:CAS:528:DC%2BD28XhtFaks7%2FN 16702948 (Pubitemid 44646192)
    • (2006) Oncogene , vol.25 , Issue.50 , pp. 6648-6659
    • Billottet, C.1    Grandage, V.L.2    Gale, R.E.3    Quattropani, A.4    Rommel, C.5    Vanhaesebroeck, B.6    Khwaja, A.7
  • 43
    • 84870019546 scopus 로고    scopus 로고
    • Evidence of clinical activity in a phase 1 study of CAL-101, an oral P110δ isoform-selective inhibitor of phosphatidylinositol 3-kinase, in patients with relapsed or refractory B-Cell malignancies
    • New Orleans, LA: December 5-8, 2009:922. This abstract describes preliminary results showing that single agent CAL-101 has produced several partial responses in B cell malignancies
    • •• Flinn IW, Byrd JC, Furman RR, et al.: Evidence of clinical activity in a phase 1 study of CAL-101, an oral P110δ isoform-selective inhibitor of phosphatidylinositol 3-kinase, in patients with relapsed or refractory B-Cell malignancies. Presented at the 51st American Society of Hematology Annual Meeting. New Orleans, LA: December 5-8, 2009:922. This abstract describes preliminary results showing that single agent CAL-101 has produced several partial responses in B cell malignancies.
    • Presented at the 51st American Society of Hematology Annual Meeting
    • Flinn, I.W.1    Byrd, J.C.2    Furman, R.R.3
  • 44
    • 60349088457 scopus 로고    scopus 로고
    • Perifosine: Update on a novel Akt inhibitor
    • 10.1007/s11912-009-0016-4 1:CAS:528:DC%2BD1MXltVSlurs%3D 19216841
    • JJ Gills PA Dennis 2009 Perifosine: update on a novel Akt inhibitor Curr Oncol Rep 11 102 110 10.1007/s11912-009-0016-4 1:CAS:528:DC%2BD1MXltVSlurs%3D 19216841
    • (2009) Curr Oncol Rep , vol.11 , pp. 102-110
    • Gills, J.J.1    Dennis, P.A.2
  • 45
    • 68049132168 scopus 로고    scopus 로고
    • A phase i study of MK-2206, an oral potent allosteric Akt inhibitor (Akti), in patients (pts) with advanced solid tumor (ST)
    • AW Tolcher TA Yap I Fearen, et al. 2009 A phase I study of MK-2206, an oral potent allosteric Akt inhibitor (Akti), in patients (pts) with advanced solid tumor (ST) ASCO Meeting Abstracts 27 3503
    • (2009) ASCO Meeting Abstracts , vol.27 , pp. 3503
    • Tolcher, A.W.1    Yap, T.A.2    Fearen, I.3
  • 46
    • 76049123027 scopus 로고    scopus 로고
    • Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells
    • 10.1073/pnas.0905152106 1:CAS:528:DC%2BC3cXmtlagug%3D%3D 20007781 This paper demonstrates that NVP-BEZ235 is effective in HER2 amplified and PIK3CA mutant breast cancer cells. Importantly, it also shows that breast cancer cells with loss of PTEN function are resistant to NVP-BEZ235.
    • SM Brachmann I Hofmann C Schnell, et al. 2009 Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells Proc Natl Acad Sci U S A 106 22299 22304 10.1073/pnas.0905152106 1:CAS:528:DC%2BC3cXmtlagug%3D%3D 20007781 This paper demonstrates that NVP-BEZ235 is effective in HER2 amplified and PIK3CA mutant breast cancer cells. Importantly, it also shows that breast cancer cells with loss of PTEN function are resistant to NVP-BEZ235.
    • (2009) Proc Natl Acad Sci U S A , vol.106 , pp. 22299-22304
    • Brachmann, S.M.1    Hofmann, I.2    Schnell, C.3
  • 47
    • 70449995469 scopus 로고    scopus 로고
    • Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer
    • 10.1073/pnas.0907325106 1:CAS:528:DC%2BD1MXhsVWrsbvJ 19805051
    • ML Sos S Fischer R Ullrich M Peifer JM Heuckmann M Koker, et al. 2009 Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer Proc Natl Acad Sci U S A. 106 18351 6 10.1073/pnas.0907325106 1:CAS:528:DC%2BD1MXhsVWrsbvJ 19805051
    • (2009) Proc Natl Acad Sci U S A. , vol.106 , pp. 18351-6
    • Sos, M.L.1    Fischer, S.2    Ullrich, R.3    Peifer, M.4    Heuckmann, J.M.5    Koker, M.6
  • 48
    • 77649193334 scopus 로고    scopus 로고
    • In vitro evaluation of pan-PI3-kinase inhibitor SF1126 in trastuzumab-sensitive and trastuzumab-resistant HER2-over-expressing breast cancer cells
    • Jul 28 (Epub ahead of print)
    • Ozbay T, Durden DL, Liu T, et al.: In vitro evaluation of pan-PI3-kinase inhibitor SF1126 in trastuzumab-sensitive and trastuzumab-resistant HER2-over-expressing breast cancer cells. Cancer Chemother Pharmacol 2009 Jul 28 (Epub ahead of print).
    • (2009) Cancer Chemother Pharmacol
    • Ozbay, T.1    Durden, D.L.2    Liu, T.3
  • 49
    • 65349101151 scopus 로고    scopus 로고
    • Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941
    • 10.1016/j.ccr.2009.03.020 1:CAS:528:DC%2BD1MXmvVGitrg%3D 19411071
    • TT Junttila RW Akita K Parsons, et al. 2009 Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941 Cancer Cell 15 429 440 10.1016/j.ccr.2009.03.020 1:CAS:528:DC%2BD1MXmvVGitrg%3D 19411071
    • (2009) Cancer Cell , vol.15 , pp. 429-440
    • Junttila, T.T.1    Akita, R.W.2    Parsons, K.3
  • 50
    • 57349194139 scopus 로고    scopus 로고
    • Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers
    • 10.1038/nm.1890 1:CAS:528:DC%2BD1cXhsVWhu7rI 19029981 This paper shows that combined PI3K and MEK inhibition is effective in a RAS mutated model of murine lung cancer.
    • JA Engelman L Chen X Tan, et al. 2008 Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers Nat Med 14 1351 1356 10.1038/nm.1890 1:CAS:528:DC%2BD1cXhsVWhu7rI 19029981 This paper shows that combined PI3K and MEK inhibition is effective in a RAS mutated model of murine lung cancer.
    • (2008) Nat Med , vol.14 , pp. 1351-1356
    • Engelman, J.A.1    Chen, L.2    Tan, X.3
  • 51
    • 52649115891 scopus 로고    scopus 로고
    • The forkhead transcription factor FOXO3a increases phosphoinositide-3 kinase/Akt activity in drug-resistant leukemic cells through induction of PIK3CA expression
    • 10.1128/MCB.01265-07 1:CAS:528:DC%2BD1cXhtF2gt73E 18644865
    • RC Hui AR Gomes D Constantinidou, et al. 2008 The forkhead transcription factor FOXO3a increases phosphoinositide-3 kinase/Akt activity in drug-resistant leukemic cells through induction of PIK3CA expression Mol Cell Biol 28 5886 5898 10.1128/MCB.01265-07 1:CAS:528:DC%2BD1cXhtF2gt73E 18644865
    • (2008) Mol Cell Biol , vol.28 , pp. 5886-5898
    • Hui, R.C.1    Gomes, A.R.2    Constantinidou, D.3
  • 52
    • 0034307305 scopus 로고    scopus 로고
    • Inhibition of phosphatidylinositide 3-kinase enhances gemcitabine-induced apoptosis in human pancreatic cancer cells
    • 1:CAS:528:DC%2BD3cXns1ehtrw%3D 11034087
    • SSW Ng MS Tsao S Chow DW Hedley 2000 Inhibition of phosphatidylinositide 3-kinase enhances gemcitabine-induced apoptosis in human pancreatic cancer cells Cancer Res 60 5451 5455 1:CAS:528:DC%2BD3cXns1ehtrw%3D 11034087
    • (2000) Cancer Res , vol.60 , pp. 5451-5455
    • Ng, S.S.W.1    Tsao, M.S.2    Chow, S.3    Hedley, D.W.4
  • 53
    • 67649382929 scopus 로고    scopus 로고
    • AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer
    • 10.1016/j.ccr.2009.04.012 1:CAS:528:DC%2BD1MXhtVWnsL7M 19573809
    • KM Vasudevan DA Barbie MA Davies, et al. 2009 AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer Cancer Cell 16 21 32 10.1016/j.ccr.2009.04.012 1:CAS:528:DC%2BD1MXhtVWnsL7M 19573809
    • (2009) Cancer Cell , vol.16 , pp. 21-32
    • Vasudevan, K.M.1    Barbie, D.A.2    Davies, M.A.3
  • 54
    • 19344375090 scopus 로고    scopus 로고
    • Characterization of the cloned full-length and a truncated human target of rapamycin: Activity, specificity, and enzyme inhibition as studied by a high capacity assay
    • DOI 10.1016/j.bbrc.2005.04.117, PII S0006291X05008776
    • L Toral-Barza WG Zhang C Lamison, et al. 2005 Characterization of the cloned full-length and a truncated human target of rapamycin: activity, specificity, and enzyme inhibition as studied by a high capacity assay Biochem Biophys Res Commun 332 304 310 10.1016/j.bbrc.2005.04.117 1:CAS:528: DC%2BD2MXkt1OjtL4%3D 15896331 (Pubitemid 40719487)
    • (2005) Biochemical and Biophysical Research Communications , vol.332 , Issue.1 , pp. 304-310
    • Toral-Barza, L.1    Zhang, W.-G.2    Lamison, C.3    LaRocque, J.4    Gibbons, J.5    Yu, K.6


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