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Volumn 13, Issue 5, 2014, Pages 1021-1031

Picking the point of inhibition: A comparative review of PI3K/AKT/mTOR pathway inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMITOTIC AGENT; ANTINEOPLASTIC AGENT; B RAF KINASE; K RAS PROTEIN; MAMMALIAN TARGET OF RAPAMYCIN; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; P110ALPHA INHIBITOR; P110BETA INHIBITOR; P110DELTA INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PROTEIN; PROTEIN KINASE B; PROTEIN KINASE B INHIBITOR; PROTEIN KINASE LKB1; TUBERIN; TUBEROUS SCLEROSIS COMPLEX 1; UNCLASSIFIED DRUG; ISOENZYME; PROTEIN KINASE INHIBITOR; TARGET OF RAPAMYCIN KINASE;

EID: 84899850988     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-13-0639     Document Type: Review
Times cited : (382)

References (86)
  • 1
    • 84875554160 scopus 로고    scopus 로고
    • Genomic determinants of PI3K pathway inhibitor response in cancer
    • Weigelt B, Downward J. Genomic determinants of PI3K pathway inhibitor response in cancer. Front Oncol 2012;2:109.
    • (2012) Front Oncol , vol.2 , pp. 109
    • Weigelt, B.1    Downward, J.2
  • 2
    • 33746257209 scopus 로고    scopus 로고
    • The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism
    • Engelman JA, Luo J, Cantley LC. The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev Genet 2006;7:606-19.
    • (2006) Nat Rev Genet , vol.7 , pp. 606-619
    • Engelman, J.A.1    Luo, J.2    Cantley, L.C.3
  • 3
    • 51849111524 scopus 로고    scopus 로고
    • NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations
    • Serra V, Markman B, Scaltriti M, Eichhorn PJ, Valero V, Guzman M, et al. NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations. Cancer Res 2008;68:8022-30.
    • (2008) Cancer Res , vol.68 , pp. 8022-8030
    • Serra, V.1    Markman, B.2    Scaltriti, M.3    Eichhorn, P.J.4    Valero, V.5    Guzman, M.6
  • 4
    • 83355163329 scopus 로고    scopus 로고
    • GDC-0980 is a novel class i PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway
    • Wallin JJ, Edgar KA, Guan J, Berry M, PriorWW,Lee L, et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther 2011; 10:2426-36.
    • (2011) Mol Cancer Ther , vol.10 , pp. 2426-2436
    • Wallin, J.J.1    Edgar, K.A.2    Guan, J.3    Berry, M.4    Prior, W.W.5    Lee, L.6
  • 5
    • 79960605738 scopus 로고    scopus 로고
    • Targeting phosphatidylinositol 3 kinase (PI3K)-Akt beyond rapalogs
    • Ogita S, Lorusso P. Targeting phosphatidylinositol 3 kinase (PI3K)-Akt beyond rapalogs. Target Oncol 2011;6:103-17.
    • (2011) Target Oncol , vol.6 , pp. 103-117
    • Ogita, S.1    Lorusso, P.2
  • 6
    • 84856826293 scopus 로고    scopus 로고
    • 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, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther 2012;11: 317-28.
    • (2012) Mol Cancer Ther , vol.11 , pp. 317-328
    • Maira, S.M.1    Pecchi, S.2    Huang, A.3    Burger, M.4    Knapp, M.5    Sterker, D.6
  • 7
    • 77954755623 scopus 로고    scopus 로고
    • Predictive biomarkers of sensitivity to the phosphatidylinositol 30 kinase inhibitor GDC-0941 in breast cancer preclinical models
    • O'Brien C, Wallin JJ, Sampath D, GuhaThakurta D, Savage H, Punnoose EA, et al. Predictive biomarkers of sensitivity to the phosphatidylinositol 30 kinase inhibitor GDC-0941 in breast cancer preclinical models. Clin Cancer Res 2010;16:3670-83.
    • (2010) Clin Cancer Res , vol.16 , pp. 3670-3683
    • O'Brien, C.1    Wallin, J.J.2    Sampath, D.3    Guhathakurta, D.4    Savage, H.5    Punnoose, E.A.6
  • 8
    • 84856071447 scopus 로고    scopus 로고
    • Phase I, dose-escalation study of BKM120, an oral pan-Class i PI3K inhibitor, in patients with advanced solid tumors
    • Bendell JC, Rodon J, Burris HA, de Jonge M, Verweij J, Birle D, et al. Phase I, dose-escalation study of BKM120, an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors. J Clin Oncol 2012; 30:282-90.
    • (2012) J Clin Oncol , vol.30 , pp. 282-290
    • Bendell, J.C.1    Rodon, J.2    Burris, H.A.3    De Jonge, M.4    Verweij, J.5    Birle, D.6
  • 9
    • 84861963385 scopus 로고    scopus 로고
    • A phase i dose-escalation study to evaluate GDC-0941, a pan-PI3K inhibitor, administered QD or BID in patients with advanced or metastatic solid tumors
    • Von Hoff DD, LoRusso P, Demetri GD, Weiss GJ, Shapiro G, Ramanathan RK, et al. A phase I dose-escalation study to evaluate GDC-0941, a pan-PI3K inhibitor, administered QD or BID in patients with advanced or metastatic solid tumors. J Clin Oncol 2011;29: 15s.
    • (2011) J Clin Oncol , vol.29
    • Von Hoff, D.D.1    Lorusso, P.2    Demetri, G.D.3    Weiss, G.J.4    Shapiro, G.5    Ramanathan, R.K.6
  • 10
    • 84899819057 scopus 로고    scopus 로고
    • Phase i dose-escalation study of the oral dual mTOR/PI3K inhibitor BEZ235, solid dispersion system (SDS) sachet formulation, in patients with advanced solid tumors
    • Rodon J, Burris HA, Schellens JHM, Schuler M, Goodman O, Britten C, et al. Phase I dose-escalation study of the oral dual mTOR/PI3K inhibitor BEZ235, solid dispersion system (SDS) sachet formulation, in patients with advanced solid tumors. Eur J Cancer 2012;48:112.
    • (2012) Eur J Cancer , vol.48 , pp. 112
    • Rodon, J.1    Burris, H.A.2    Schellens, J.H.M.3    Schuler, M.4    Goodman, O.5    Britten, C.6
  • 11
    • 84892988581 scopus 로고    scopus 로고
    • A pilot study of sirolimus (S) in subjects with Cowden syndrome (CS) with germ-line mutations in PTEN
    • (suppl; abstr 2532)
    • Komiya T, Blumenthal G, Ballas M, Dechowdhury R, Manu M, Fioravanti S, et al. A pilot study of sirolimus (S) in subjects with Cowden syndrome (CS) with germ-line mutations in PTEN. J Clin Oncol 31, 2013 (suppl; abstr 2532).
    • (2013) J Clin Oncol , vol.31
    • Komiya, T.1    Blumenthal, G.2    Ballas, M.3    Dechowdhury, R.4    Manu, M.5    Fioravanti, S.6
  • 12
    • 34447272449 scopus 로고    scopus 로고
    • Tuberous sclerosis complex: Advances in diagnosis, genetics, and management
    • Schwartz RA, Fernandez G, Kotulska K, Jozwiak S. Tuberous sclerosis complex: advances in diagnosis, genetics, and management. J Am Acad Dermatol 2007;57:189-202.
    • (2007) J Am Acad Dermatol , vol.57 , pp. 189-202
    • Schwartz, R.A.1    Fernandez, G.2    Kotulska, K.3    Jozwiak, S.4
  • 13
    • 80052313178 scopus 로고    scopus 로고
    • Everolimus: An mTOR inhibitor for the treatment of tuberous sclerosis
    • Franz DN. Everolimus: an mTOR inhibitor for the treatment of tuberous sclerosis. Expert Rev Anticancer Ther 2011;11:1181-92.
    • (2011) Expert Rev Anticancer Ther , vol.11 , pp. 1181-1192
    • Franz, D.N.1
  • 14
    • 45749119969 scopus 로고    scopus 로고
    • Bladder tumour-derived somatic TSC1 missense mutations cause loss of function via distinct mechanisms
    • Pymar LS, Platt FM, Askham JM, Morrison EE, Knowles MA. Bladder tumour-derived somatic TSC1 missense mutations cause loss of function via distinct mechanisms. Hum Mol Genet 2008;17:2006-17.
    • (2008) Hum Mol Genet , vol.17 , pp. 2006-2017
    • Pymar, L.S.1    Platt, F.M.2    Askham, J.M.3    Morrison, E.E.4    Knowles, M.A.5
  • 18
    • 58749097239 scopus 로고    scopus 로고
    • LKB1/KRAS mutant lung cancers constitute a genetic subset of NSCLC with increased sensitivity to MAPK and mTOR signalling inhibition
    • Mahoney CL, Choudhury B, Davies H, Edkins S, Greenman C, Haaften G, et al. LKB1/KRAS mutant lung cancers constitute a genetic subset of NSCLC with increased sensitivity to MAPK and mTOR signalling inhibition. Br J Cancer 2009;100:370-5.
    • (2009) Br J Cancer , vol.100 , pp. 370-375
    • Mahoney, C.L.1    Choudhury, B.2    Davies, H.3    Edkins, S.4    Greenman, C.5    Haaften, G.6
  • 19
    • 44449103256 scopus 로고    scopus 로고
    • Important role of the LKB1-AMPK pathway in suppressing tumorigenesis in PTEN-deficient mice
    • Huang X, Wullschleger S, Shpiro N, McGuire VA, Sakamoto K, Woods YL, et al. Important role of the LKB1-AMPK pathway in suppressing tumorigenesis in PTEN-deficient mice. Biochem J 2008;412:211-21.
    • (2008) Biochem J , vol.412 , pp. 211-221
    • Huang, X.1    Wullschleger, S.2    Shpiro, N.3    McGuire, V.A.4    Sakamoto, K.5    Woods, Y.L.6
  • 20
    • 79953216329 scopus 로고    scopus 로고
    • Effect of PI3K- and mTOR-specific inhibitors on spontaneous B-cell follicular lymphomas in PTEN/LKB1-deficient mice
    • Garcia-Martinez JM, Wullschleger S, Preston G, Guichard S, Fleming S, Alessi DR, et al. Effect of PI3K- and mTOR-specific inhibitors on spontaneous B-cell follicular lymphomas in PTEN/LKB1-deficient mice. Br J Cancer 2011;104:1116-25.
    • (2011) Br J Cancer , vol.104 , pp. 1116-1125
    • Garcia-Martinez, J.M.1    Wullschleger, S.2    Preston, G.3    Guichard, S.4    Fleming, S.5    Alessi, D.R.6
  • 21
    • 84856988295 scopus 로고    scopus 로고
    • A dose-escalation study with the novel formulation of the oral pan-class i PI3K inhibitor BEZ235, solid dispersion system (SDS) sachet, in patients with advanced solid tumors
    • (suppl; abstr 3066)
    • Peyton JD, Rodon Ahnert J, Burris H, Britten C, Chen LC, Tabernero J, et al. A dose-escalation study with the novel formulation of the oral pan-class I PI3K inhibitor BEZ235, solid dispersion system (SDS) sachet, in patients with advanced solid tumors. J Clin Oncol 29: 2011 (suppl; abstr 3066).
    • (2011) J Clin Oncol , vol.29
    • Peyton, J.D.1    Rodon Ahnert, J.2    Burris, H.3    Britten, C.4    Chen, L.C.5    Tabernero, J.6
  • 22
    • 80054740282 scopus 로고    scopus 로고
    • A first-in-human phase i study to evaluate GDC-0980, an oral PI3K/mTOR inhibitor, administered QDin patients with advanced solid tumors
    • (suppl; abstr 3020)
    • Wagner AJ, Bendell JC, Dolly S, Morgan JA, Ware JA, Fredrickson J, et al. A first-in-human phase I study to evaluate GDC-0980, an oral PI3K/mTOR inhibitor, administered QDin patients with advanced solid tumors. J Clin Oncol 2011;29:15s, (suppl; abstr 3020).
    • (2011) J Clin Oncol , vol.29
    • Wagner, A.J.1    Bendell, J.C.2    Dolly, S.3    Morgan, J.A.4    Ware, J.A.5    Fredrickson, J.6
  • 23
    • 84899798609 scopus 로고    scopus 로고
    • Everolimus with paclitaxel plus bevacizumab as first-line therapy for HER2-negative metastatic breast cancer (MBC): A randomized, double-blind, placebo-controlled phase II trial of the Sarah Cannon Research Institute (SCRI)
    • (suppl; abstr 1018)
    • Yardley D, Linda D, Bosserman L, Walker-Peacock N, Favret A, Morgan S, Priego V, et al. Everolimus with paclitaxel plus bevacizumab as first-line therapy for HER2-negative metastatic breast cancer (MBC): A randomized, double-blind, placebo-controlled phase II trial of the Sarah Cannon Research Institute (SCRI). J Clin Oncol 30, 2012 (suppl; abstr 1018).
    • (2012) J Clin Oncol , vol.30
    • Yardley, D.1    Linda, D.2    Bosserman, L.3    Walker-Peacock, N.4    Favret, A.5    Morgan, S.6    Priego, V.7
  • 24
    • 84899851966 scopus 로고    scopus 로고
    • Phase Ib dose-escalation study of BEZ235 or BKM120 in combination with paclitaxel (Ptx) in patients with advanced solid tumors
    • (abstr 454P)
    • Dirix L, Schuler M, Machiels J, Hess D, Awada A, Steeghs N, et al. Phase Ib dose-escalation study of BEZ235 or BKM120 in combination with paclitaxel (Ptx) in patients with advanced solid tumors. Ann Oncol 2012;23:ix157-ix158 (abstr 454P).
    • (2012) Ann Oncol , vol.23
    • Dirix, L.1    Schuler, M.2    Machiels, J.3    Hess, D.4    Awada, A.5    Steeghs, N.6
  • 25
    • 84863925300 scopus 로고    scopus 로고
    • GDC- 0941, a novel class i selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo
    • Wallin JJ, Guan J, Prior WW, Lee LB, Berry L, Belmont LD, et al. GDC- 0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo. Clin Cancer Res 2012;18:3901-11.
    • (2012) Clin Cancer Res , vol.18 , pp. 3901-3911
    • Wallin, J.J.1    Guan, J.2    Prior, W.W.3    Lee, L.B.4    Berry, L.5    Belmont, L.D.6
  • 26
    • 63749106157 scopus 로고    scopus 로고
    • Should individual PI3 kinase isoforms be targeted in cancer?
    • Jia S, Roberts TM, Zhao JJ. Should individual PI3 kinase isoforms be targeted in cancer? Curr Opin Cell Biol 2009;21:199-208.
    • (2009) Curr Opin Cell Biol , vol.21 , pp. 199-208
    • Jia, S.1    Roberts, T.M.2    Zhao, J.J.3
  • 27
    • 84869024543 scopus 로고    scopus 로고
    • The complexity of prostate cancer: Genomic alterations and heterogeneity
    • Boyd LK, Mao X, Lu YJ. The complexity of prostate cancer: genomic alterations and heterogeneity. Nat Rev Urol 2012;9:652-64.
    • (2012) Nat Rev Urol , vol.9 , pp. 652-664
    • Boyd, L.K.1    Mao, X.2    Lu, Y.J.3
  • 28
    • 84875752240 scopus 로고    scopus 로고
    • Emerging targeted agents in metastatic breast cancer
    • Zardavas D, Baselga J, Piccart M. Emerging targeted agents in metastatic breast cancer. Nat Rev Clin Oncol 2013;10:191-210.
    • (2013) Nat Rev Clin Oncol , vol.10 , pp. 191-210
    • Zardavas, D.1    Baselga, J.2    Piccart, M.3
  • 29
    • 80054778946 scopus 로고    scopus 로고
    • High frequency of PIK3R1 and PIK3R2 mutations in endometrial cancer elucidates a novel mechanism for regulation of PTEN protein stability
    • Cheung LW, Hennessy BT, Li J, Yu S, Myers AP, Djordjevic B, et al. High frequency of PIK3R1 and PIK3R2 mutations in endometrial cancer elucidates a novel mechanism for regulation of PTEN protein stability. Cancer Discov 2011;1:170-85.
    • (2011) Cancer Discov , vol.1 , pp. 170-185
    • Cheung, L.W.1    Hennessy, B.T.2    Li, J.3    Yu, S.4    Myers, A.P.5    Djordjevic, B.6
  • 30
    • 84886720477 scopus 로고    scopus 로고
    • Single agent activity of PIK3CA inhibitor BYL719 in a broad cancer cell line panel
    • Huang A, Fritsch C, Wilson C, Reddy A, Liu M, Lehar J, et al. Single agent activity of PIK3CA inhibitor BYL719 in a broad cancer cell line panel. Cancer Res 2012;72:3749.
    • (2012) Cancer Res , vol.72 , pp. 3749
    • Huang, A.1    Fritsch, C.2    Wilson, C.3    Reddy, A.4    Liu, M.5    Lehar, J.6
  • 31
    • 84899831498 scopus 로고    scopus 로고
    • P110 a-specific inhibitor is more suitable in PIK3CA mutated breast cancer model but ineffective in PTEN loss of function breast cancer model
    • Sun Y, Dey P, Wu H, Leyland-Jones B. P110 a-specific inhibitor is more suitable in PIK3CA mutated breast cancer model but ineffective in PTEN loss of function breast cancer model. Cancer Res 2012;72:2227.
    • (2012) Cancer Res , vol.72 , pp. 2227
    • Sun, Y.1    Dey, P.2    Wu, H.3    Leyland-Jones, B.4
  • 32
    • 84885431490 scopus 로고    scopus 로고
    • Safety, pharmacokinetics, and preliminary activity of the a-specific PI3K inhibitor BYL719: Results from the first-in-human study
    • (suppl; abstr 2531)
    • Gonzalez-Angulo A, Juric D, Argiles G, Schellens J, Burris H, Berlin J, et al. Safety, pharmacokinetics, and preliminary activity of the a-specific PI3K inhibitor BYL719: Results from the first-in-human study. J Clin Oncol 31: 2013 (suppl; abstr 2531).
    • (2013) J Clin Oncol , vol.31
    • Gonzalez-Angulo, A.1    Juric, D.2    Argiles, G.3    Schellens, J.4    Burris, H.5    Berlin, J.6
  • 33
    • 84899881210 scopus 로고    scopus 로고
    • GDC- 0032, a beta isoform-sparing PI3K inhibitor: Results of a first-in-human phase Ia dose escalation study
    • Juric D, Krop I,Ramanathan R, Xiao J, Sanabria S, Wilson T, et al. GDC- 0032, a beta isoform-sparing PI3K inhibitor: results of a first-in-human phase Ia dose escalation study. Cancer Res 2013;73:LB-64.
    • (2013) Cancer Res , vol.73
    • Juric, D.1    Krop, I.2    Ramanathan, R.3    Xiao, J.4    Sanabria, S.5    Wilson, T.6
  • 34
    • 84894885323 scopus 로고    scopus 로고
    • AZD8186: A potent selective inhibitor of PI3Kb targeting PTEN-deficient tumours dependent on dysregulated PI3Kb signalling
    • Hancox U, Cosulich S, Dry H, Hanson L, Crafter C, Barlaam B, et al. AZD8186: a potent selective inhibitor of PI3Kb targeting PTEN-deficient tumours dependent on dysregulated PI3Kb signalling. Cancer Res 2013;73:3264.
    • (2013) Cancer Res , vol.73 , pp. 3264
    • Hancox, U.1    Cosulich, S.2    Dry, H.3    Hanson, L.4    Crafter, C.5    Barlaam, B.6
  • 35
    • 84863833204 scopus 로고    scopus 로고
    • Functional characterization of an isoform-selective inhibitor of PI3K-p110beta as a potential anticancer agent
    • Ni J, Liu Q, Xie S, Carlson C, Von T, Vogel K, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110beta as a potential anticancer agent. Cancer Discov 2012;2:425-33.
    • (2012) Cancer Discov , vol.2 , pp. 425-433
    • Ni, J.1    Liu, Q.2    Xie, S.3    Carlson, C.4    Von, T.5    Vogel, K.6
  • 36
    • 76249092302 scopus 로고    scopus 로고
    • Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors
    • Edgar KA, Wallin JJ, Berry M, Lee LB, Prior WW, Sampath D, et al. Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors. Cancer Res 2010;70:1164-72.
    • (2010) Cancer Res , vol.70 , pp. 1164-1172
    • Edgar, K.A.1    Wallin, J.J.2    Berry, M.3    Lee, L.B.4    Prior, W.W.5    Sampath, D.6
  • 38
    • 84879843662 scopus 로고    scopus 로고
    • Proliferation of PTEN-deficient haematopoietic tumour cells is not affected by isoform- selective inhibition of p110 PI3-kinase and requires blockade of all class 1 PI3K activity
    • Stengel C, Jenner E, Meja K, Mayekar S, Khwaja A. Proliferation of PTEN-deficient haematopoietic tumour cells is not affected by isoform- selective inhibition of p110 PI3-kinase and requires blockade of all class 1 PI3K activity. Br J Haematol 2013;162:285-9.
    • (2013) Br J Haematol , vol.162 , pp. 285-289
    • Stengel, C.1    Jenner, E.2    Meja, K.3    Mayekar, S.4    Khwaja, A.5
  • 39
    • 84875143933 scopus 로고    scopus 로고
    • Identification of GSK2636771, a potent and selective, orally bioavailable inhibitor of phosphatidylinositol 3-kinasebeta (PI3Kb) for the treatment of PTEN deficient tumors
    • Rivero RA, Hardwicke MA. Identification of GSK2636771, a potent and selective, orally bioavailable inhibitor of phosphatidylinositol 3-kinasebeta (PI3Kb) for the treatment of PTEN deficient tumors. Cancer Res 2012;72:2913.
    • (2012) Cancer Res , vol.72 , pp. 2913
    • Rivero, R.A.1    Hardwicke, M.A.2
  • 40
    • 84873650548 scopus 로고    scopus 로고
    • Temsirolimus in the treatment of mantle cell lymphoma: Frequency and management of adverse effects
    • Bouabdallah K, Ribrag V, Terriou L, Soria JC, Delarue R. Temsirolimus in the treatment of mantle cell lymphoma: frequency and management of adverse effects. Curr Opin Oncol 2013;25:S1-12.
    • (2013) Curr Opin Oncol , vol.25
    • Bouabdallah, K.1    Ribrag, V.2    Terriou, L.3    Soria, J.C.4    Delarue, R.5
  • 41
    • 77957203544 scopus 로고    scopus 로고
    • Interim results from a phase i study of CAL-101, a selective oral inhibitor of phosphatidylinositol 3-kinase p110d isoform, in patients with relapsed or refractory hematologic malignancies
    • (suppl; abstr 3032)
    • Furman RR, Byrd JC, Flinn IW, Coutre SE, Benson DM, Brown JR, et al. Interim results from a phase I study of CAL-101, a selective oral inhibitor of phosphatidylinositol 3-kinase p110d isoform, in patients with relapsed or refractory hematologic malignancies. J Clin Oncol 28:15s, 2010 (suppl; abstr 3032).
    • (2010) J Clin Oncol , vol.28
    • Furman, R.R.1    Byrd, J.C.2    Flinn, I.W.3    Coutre, S.E.4    Benson, D.M.5    Brown, J.R.6
  • 42
    • 84889100379 scopus 로고    scopus 로고
    • Final results of a phase i study of idelalisib (GS-1101) a selective inhibitor of PI3Kd, in patients with relapsed or refractory CLL
    • (suppl; abstr 7003)
    • Brown J, Furman R, Flinn I, Coutre S, Wagner-Johnston N, Kahl B, et al. Final results of a phase I study of idelalisib (GS-1101) a selective inhibitor of PI3Kd, in patients with relapsed or refractory CLL. J Clin Oncol 73: 2013 (suppl; abstr 7003).
    • (2013) J Clin Oncol , vol.73
    • Brown, J.1    Furman, R.2    Flinn, I.3    Coutre, S.4    Wagner-Johnston, N.5    Kahl, B.6
  • 43
    • 84877930029 scopus 로고    scopus 로고
    • P110alpha mediated constitutive PI3K signaling limits the efficacy of p110delta-selective inhibition in mantle cell lymphoma, particularly with multiple relapse
    • Iyengar S, Clear A, Bodor C, Maharaj L, Lee A, Calaminici M, et al. P110alpha mediated constitutive PI3K signaling limits the efficacy of p110delta-selective inhibition in mantle cell lymphoma, particularly with multiple relapse. Blood 2013;121:2274-84.
    • (2013) Blood , vol.121 , pp. 2274-2284
    • Iyengar, S.1    Clear, A.2    Bodor, C.3    Maharaj, L.4    Lee, A.5    Calaminici, M.6
  • 45
    • 84876669684 scopus 로고    scopus 로고
    • The phosphatidylinositol- 3 kinase i inhibitor BKM120 induces cell death in Bchronic lymphocytic leukemia cells in vitro
    • Amrein L, Shawi M, Grenier J, Aloyz R, Panasci L. The phosphatidylinositol- 3 kinase I inhibitor BKM120 induces cell death in Bchronic lymphocytic leukemia cells in vitro. Int J Cancer 2013; 133:247-52.
    • (2013) Int J Cancer , vol.133 , pp. 247-252
    • Amrein, L.1    Shawi, M.2    Grenier, J.3    Aloyz, R.4    Panasci, L.5
  • 46
    • 84857844598 scopus 로고    scopus 로고
    • PI3Kdelta inhibitors in cancer: Rationale and serendipity merge in the clinic
    • Fruman DA, Rommel C. PI3Kdelta inhibitors in cancer: rationale and serendipity merge in the clinic. Cancer Discov 2011;1:562-72.
    • (2011) Cancer Discov , vol.1 , pp. 562-572
    • Fruman, D.A.1    Rommel, C.2
  • 47
    • 84868268199 scopus 로고    scopus 로고
    • A phase i dose expansion cohort study of the safety, pharmacokinetics and pharmacodynamics of SAR245409 (S09), an orally administered PI3K/mTOR inhibitor, in patients with lymphoma
    • Papadopoulos K, Abrisqueta P, Chambers G, Rasco D, Patnaik A, Tabernero J, et al. A phase I dose expansion cohort study of the safety, pharmacokinetics and pharmacodynamics of SAR245409 (S09), an orally administered PI3K/mTOR inhibitor, in patients with lymphoma. Blood 2011;118:1608.
    • (2011) Blood , vol.118 , pp. 1608
    • Papadopoulos, K.1    Abrisqueta, P.2    Chambers, G.3    Rasco, D.4    Patnaik, A.5    Tabernero, J.6
  • 48
    • 84867234045 scopus 로고    scopus 로고
    • Phase i trial of SAR245408 (S08), a pan-phosphatidylinositol 3 kinase (PI3K) inhibitor, in patients with Chronic Lymphocytic Leukemia (CLL) and lymphoma
    • Brown J, Davids M, Rodon J, Abrisqueta P, DeCillis A, Rockich K, et al. Phase I trial of SAR245408 (S08), a pan-phosphatidylinositol 3 kinase (PI3K) inhibitor, in patients with Chronic Lymphocytic Leukemia (CLL) and lymphoma. Blood 2011;118:2683.
    • (2011) Blood , vol.118 , pp. 2683
    • Brown, J.1    Davids, M.2    Rodon, J.3    Abrisqueta, P.4    Decillis, A.5    Rockich, K.6
  • 49
    • 0037047590 scopus 로고    scopus 로고
    • Impaired B and T cell antigen receptor signaling in p110delta PI 3- kinase mutant mice
    • Okkenhaug K, Bilancio A, Farjot G, Priddle H, Sancho S, Peskett E, et al. Impaired B and T cell antigen receptor signaling in p110delta PI 3- kinase mutant mice. Science 2002;297:1031-4.
    • (2002) Science , vol.297 , pp. 1031-1034
    • Okkenhaug, K.1    Bilancio, A.2    Farjot, G.3    Priddle, H.4    Sancho, S.5    Peskett, E.6
  • 50
    • 80053079880 scopus 로고    scopus 로고
    • Phase i study of CAL-101, an isoform-selective inhibitor of phosphatidylinositol 3-kinase P110d, in patients with previously treated chronic lymphocytic leukemia
    • (suppl; abstr 6631)
    • Coutre SE, Byrd JC, Furman RR, Brown JR, Benson DM, Wagner- Johnston ND, et al. Phase I study of CAL-101, an isoform-selective inhibitor of phosphatidylinositol 3-kinase P110d, in patients with previously treated chronic lymphocytic leukemia. J Clin Oncol 2011;29:15s, (suppl; abstr 6631).
    • (2011) J Clin Oncol , vol.29
    • Coutre, S.E.1    Byrd, J.C.2    Furman, R.R.3    Brown, J.R.4    Benson, D.M.5    Wagner-Johnston, N.D.6
  • 51
    • 84875950102 scopus 로고    scopus 로고
    • BYL719, a next generation PI3K alpha specific inhibitor: Preliminary safety, PK, and efficacy results from the first-in-human study
    • Juric D, Rodon J, Gonzalez-Angulo AM, Burris HA, Bendell J, Berlin JD, et al. BYL719, a next generation PI3K alpha specific inhibitor: Preliminary safety, PK, and efficacy results from the first-in-human study. Cancer Res 2012;72: Suppl 1:CT-01.
    • (2012) Cancer Res , vol.72 , Issue.SUPPL. 1
    • Juric, D.1    Rodon, J.2    Gonzalez-Angulo, A.M.3    Burris, H.A.4    Bendell, J.5    Berlin, J.D.6
  • 52
    • 33744990592 scopus 로고    scopus 로고
    • Critical role for the p110alpha phosphoinositide-3-OHkinase in growth and metabolic regulation
    • Foukas LC, Claret M, Pearce W, Okkenhaug K, Meek S, Peskett E, et al. Critical role for the p110alpha phosphoinositide-3-OHkinase in growth and metabolic regulation. Nature 2006;441:366-70.
    • (2006) Nature , vol.441 , pp. 366-370
    • Foukas, L.C.1    Claret, M.2    Pearce, W.3    Okkenhaug, K.4    Meek, S.5    Peskett, E.6
  • 53
    • 84863080820 scopus 로고    scopus 로고
    • Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo
    • Smith GC, Ong WK, Rewcastle GW, Kendall JD, Han W, Shepherd PR. Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo. Biochem J 2012;442:161-9.
    • (2012) Biochem J , vol.442 , pp. 161-169
    • Smith, G.C.1    Ong, W.K.2    Rewcastle, G.W.3    Kendall, J.D.4    Han, W.5    Shepherd, P.R.6
  • 54
    • 83255162603 scopus 로고    scopus 로고
    • First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors
    • Yap TA, Yan L, Patnaik A, Fearen I, Olmos D, Papadopoulos K, et al. First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors. J Clin Oncol 2011;29:4688-95.
    • (2011) J Clin Oncol , vol.29 , pp. 4688-4695
    • Yap, T.A.1    Yan, L.2    Patnaik, A.3    Fearen, I.4    Olmos, D.5    Papadopoulos, K.6
  • 55
    • 84874650433 scopus 로고    scopus 로고
    • A first-in-human trial of GDC-0068: A novel, oral, ATP-competitive Akt inhibitor, demonstrates robust suppression of the Akt pathway in surrogate and tumor tissues
    • Yan Y, Wagle M, Punnoose E, Musib L, Budha N, Nannini M, et al. A first-in-human trial of GDC-0068: A novel, oral, ATP-competitive Akt inhibitor, demonstrates robust suppression of the Akt pathway in surrogate and tumor tissues. Mol Cancer Ther 2011;10:B154.
    • (2011) Mol Cancer Ther , vol.10
    • Yan, Y.1    Wagle, M.2    Punnoose, E.3    Musib, L.4    Budha, N.5    Nannini, M.6
  • 56
    • 84874648382 scopus 로고    scopus 로고
    • A phase Ib study of the Akt inhibitor GDC-0068 with docetaxel (D) or mFOLFOX-6 (F) in patients (pts) with advanced solid tumors
    • (suppl; abstr 3021)
    • Saura C, Jones S, Mateo J, Hollebecque A, Cleary JM, Roda Perez D, et al. A phase Ib study of the Akt inhibitor GDC-0068 with docetaxel (D) or mFOLFOX-6 (F) in patients (pts) with advanced solid tumors. J Clin Oncol 30:2012 (suppl; abstr 3021).
    • (2012) J Clin Oncol , vol.30
    • Saura, C.1    Jones, S.2    Mateo, J.3    Hollebecque, A.4    Cleary, J.M.5    Roda Perez, D.6
  • 57
    • 52449092107 scopus 로고    scopus 로고
    • Breast tumor cells with PI3K mutation or HER2 amplification are selectively addicted to Akt signaling
    • She QB, Chandarlapaty S, Ye Q, Lobo J, Haskell KM, Leander KR, et al. Breast tumor cells with PI3K mutation or HER2 amplification are selectively addicted to Akt signaling. PLoS ONE 2008;3:e3065.
    • (2008) PLoS ONE , vol.3
    • She, Q.B.1    Chandarlapaty, S.2    Ye, Q.3    Lobo, J.4    Haskell, K.M.5    Leander, K.R.6
  • 60
  • 61
    • 84862738897 scopus 로고    scopus 로고
    • Preclinical pharmacology of AZD5363, an inhibitor of AKT: Pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background
    • Davies BR, Greenwood H, Dudley P, Crafter C, Yu DH, Zhang J, et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther 2012;11:873-87.
    • (2012) Mol Cancer Ther , vol.11 , pp. 873-887
    • Davies, B.R.1    Greenwood, H.2    Dudley, P.3    Crafter, C.4    Yu, D.H.5    Zhang, J.6
  • 62
    • 84875804031 scopus 로고    scopus 로고
    • Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models
    • Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res 2013; 19:1760-72.
    • (2013) Clin Cancer Res , vol.19 , pp. 1760-1772
    • Lin, J.1    Sampath, D.2    Nannini, M.A.3    Lee, B.B.4    Degtyarev, M.5    Oeh, J.6
  • 63
    • 84899879337 scopus 로고    scopus 로고
    • Results of two phase i multicenter trials of AZD5363, an inhibitor of AKT1, 2 and 3: Biomarker and early clinical evaluation in Western and Japanese patients with advanced solid tumors
    • Banerji U, Ranson M, Schellens J, Esaki T, Dean E, Zivi A, et al. Results of two phase I multicenter trials of AZD5363, an inhibitor of AKT1, 2 and 3: Biomarker and early clinical evaluation in Western and Japanese patients with advanced solid tumors. Cancer Res 2013;73:LB-66.
    • (2013) Cancer Res , vol.73
    • Banerji, U.1    Ranson, M.2    Schellens, J.3    Esaki, T.4    Dean, E.5    Zivi, A.6
  • 64
    • 84862777192 scopus 로고    scopus 로고
    • The translational landscape of mTOR signalling steers cancer initiation and metastasis
    • Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature 2012;485:55-61.
    • (2012) Nature , vol.485 , pp. 55-61
    • Hsieh, A.C.1    Liu, Y.2    Edlind, M.P.3    Ingolia, N.T.4    Janes, M.R.5    Sher, A.6
  • 65
    • 80051590039 scopus 로고    scopus 로고
    • Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: Distinct from rapamycin
    • Bhagwat SV, Gokhale PC, Crew AP, Cooke A, Yao Y, Mantis C, et al. Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin. Mol Cancer Ther 2011;10:1394-406.
    • (2011) Mol Cancer Ther , vol.10 , pp. 1394-1406
    • Bhagwat, S.V.1    Gokhale, P.C.2    Crew, A.P.3    Cooke, A.4    Yao, Y.5    Mantis, C.6
  • 67
    • 84877918260 scopus 로고    scopus 로고
    • Equivalent benefit of rapamycin and a potent mTOR ATP-competitive inhibitor, MLN0128 (INK128), in a mouse model of tuberous sclerosis
    • Guo Y, Kwiatkowski DJ. Equivalent benefit of rapamycin and a potent mTOR ATP-competitive inhibitor, MLN0128 (INK128), in a mouse model of tuberous sclerosis. Mol Cancer Res 2013;11:467-73.
    • (2013) Mol Cancer Res , vol.11 , pp. 467-473
    • Guo, Y.1    Kwiatkowski, D.J.2
  • 68
    • 84876276597 scopus 로고    scopus 로고
    • First-in-human phase i trial of the dual mTORC1 and mTORC2 inhibitor AZD2014 in solid tumors
    • (suppl; abstr 3004)
    • Banerji U, Dean EJ, Gonzalez M, Greystoke AP, Basu B, Krebs M, et al. First-in-human phase I trial of the dual mTORC1 and mTORC2 inhibitor AZD2014 in solid tumors. J Clin Oncol 30:2012 (suppl; abstr 3004).
    • (2012) J Clin Oncol , vol.30
    • Banerji, U.1    Dean, E.J.2    Gonzalez, M.3    Greystoke, A.P.4    Basu, B.5    Krebs, M.6
  • 69
    • 84885658197 scopus 로고    scopus 로고
    • Phase i expansion trial of an oral TORC1/TORC2 inhibitor (CC-223) in advanced solid tumors
    • (suppl; abstr 2606)
    • Varga A, Mita M, Wu J, Nemunaitis J, Cloughesy T, Mischel P, et al. Phase I expansion trial of an oral TORC1/TORC2 inhibitor (CC-223) in advanced solid tumors. J Clin Oncol 31:2013 (suppl; abstr 2606).
    • (2013) J Clin Oncol , vol.31
    • Varga, A.1    Mita, M.2    Wu, J.3    Nemunaitis, J.4    Cloughesy, T.5    Mischel, P.6
  • 70
    • 84874656719 scopus 로고    scopus 로고
    • Phase i trial of an oral TORC1/TORC2 inhibitor (CC-223) in advanced solid and hematologic cancers
    • (suppl; abstr 3006)
    • Shih KC, Bendell JC, Reinert A, Jones S, Kelley RK, Infante JR, et al. Phase I trial of an oral TORC1/TORC2 inhibitor (CC-223) in advanced solid and hematologic cancers. J Clin Oncol 30:2012 (suppl; abstr 3006).
    • (2012) J Clin Oncol , vol.30
    • Shih, K.C.1    Bendell, J.C.2    Reinert, A.3    Jones, S.4    Kelley, R.K.5    Infante, J.R.6
  • 71
    • 84988641494 scopus 로고    scopus 로고
    • Phase i expansion trial of an oral TORC1/TORC2 inhibitor (CC-223) in diffuse large B-cell lymphoma (DLBCL) and multiple myeloma (MM)
    • (suppl; abstr 8522)
    • Goy A, Ribrag V, Varga A, Witzig T, Ocio E, Paz-Ares L, et al. Phase I expansion trial of an oral TORC1/TORC2 inhibitor (CC-223) in diffuse large B-cell lymphoma (DLBCL) and multiple myeloma (MM). J Clin Oncol 31:2013 (suppl; abstr 8522).
    • (2013) J Clin Oncol , vol.31
    • Goy, A.1    Ribrag, V.2    Varga, A.3    Witzig, T.4    Ocio, E.5    Paz-Ares, L.6
  • 72
    • 84878831559 scopus 로고    scopus 로고
    • Overcoming acquired resistance to anticancer therapy: Focus on the PI3K/AKT/mTOR pathway
    • Burris HA III. Overcoming acquired resistance to anticancer therapy: focus on the PI3K/AKT/mTOR pathway. Cancer Chemother Pharmacol 2013;71:829-42.
    • (2013) Cancer Chemother Pharmacol , vol.71 , pp. 829-842
    • Burris III, H.A.1
  • 73
    • 84889654398 scopus 로고    scopus 로고
    • Everolimus plus exemestane in postmenopausal patients withHR breast cancer: BOLERO-2 final progression-free survival analysis
    • Yardley DA, Noguchi S, Pritchard KI, Burris HA III, Baselga J, Gnant M, et al. Everolimus plus exemestane in postmenopausal patients withHR breast cancer: BOLERO-2 final progression-free survival analysis. Adv Ther 2013;30:870-84.
    • (2013) Adv Ther , vol.30 , pp. 870-884
    • Yardley, D.A.1    Noguchi, S.2    Pritchard, K.I.3    Burris III, H.A.4    Baselga, J.5    Gnant, M.6
  • 74
    • 84885420714 scopus 로고    scopus 로고
    • Phase III, randomized, double-blind, placebo-controlled multicenter trial of daily everolimus plus weekly trastuzumab and vinorelbine in trastuzumab-resistant, advanced breast cancer (BOLERO-3)
    • (suppl; abstr 505)
    • O'Regan R, Ozguroglu M, Andre F, Toi M, Heinrich G, Jerusalem M, et al. Phase III, randomized, double-blind, placebo-controlled multicenter trial of daily everolimus plus weekly trastuzumab and vinorelbine in trastuzumab- resistant, advanced breast cancer (BOLERO-3). J Clin Oncol 31:2013 (suppl; abstr 505).
    • (2013) J Clin Oncol , vol.31
    • O'Regan, R.1    Ozguroglu, M.2    Andre, F.3    Toi, M.4    Heinrich, G.5    Jerusalem, M.6
  • 75
    • 84863338519 scopus 로고    scopus 로고
    • PI3K/AKT/mTOR inhibitors in patients with breast and gynecologic malignancies harboring PIK3CA mutations
    • Janku F, Wheler JJ, Westin SN, Moulder SL, Naing A, Tsimberidou AM, et al. PI3K/AKT/mTOR inhibitors in patients with breast and gynecologic malignancies harboring PIK3CA mutations. J Clin Oncol 2012;30:777-82.
    • (2012) J Clin Oncol , vol.30 , pp. 777-782
    • Janku, F.1    Wheler, J.J.2    Westin, S.N.3    Moulder, S.L.4    Naing, A.5    Tsimberidou, A.M.6
  • 76
    • 84871968444 scopus 로고    scopus 로고
    • PIK3CA mutation H1047R is associated with response to PI3K/ AKT/mTOR signaling pathway inhibitors in early-phase clinical trials
    • Janku F, Wheler JJ, Naing A, Falchook GS, Hong DS, Stepanek VM, et al. PIK3CA mutation H1047R is associated with response to PI3K/ AKT/mTOR signaling pathway inhibitors in early-phase clinical trials. Cancer Res 2013;73:276-84.
    • (2013) Cancer Res , vol.73 , pp. 276-284
    • Janku, F.1    Wheler, J.J.2    Naing, A.3    Falchook, G.S.4    Hong, D.S.5    Stepanek, V.M.6
  • 77
    • 84889040481 scopus 로고    scopus 로고
    • Technologies for detection of circulating tumor cells: Facts and vision
    • Alix-Panabieres C, Pantel K. Technologies for detection of circulating tumor cells: facts and vision. Lab Chip 2014;14:57-62.
    • (2014) Lab Chip , vol.14 , pp. 57-62
    • Alix-Panabieres, C.1    Pantel, K.2
  • 78
    • 51049109033 scopus 로고    scopus 로고
    • 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
    • Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, 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 2008;7:1851-63.
    • (2008) Mol Cancer Ther , vol.7 , pp. 1851-1863
    • Maira, S.M.1    Stauffer, F.2    Brueggen, J.3    Furet, P.4    Schnell, C.5    Fritsch, C.6
  • 81
    • 77957104533 scopus 로고    scopus 로고
    • A phase i dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics of XL765 (SAR245409), a PI3K/TORC1/ TORC2 inhibitor administered orally to patients (pts) with advanced malignancies
    • (suppl; abstr 3030)
    • Brana I, LoRusso P, Baselga J, Heath EI, Patnaik A, Gendreau S, et al. A phase I dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics of XL765 (SAR245409), a PI3K/TORC1/ TORC2 inhibitor administered orally to patients (pts) with advanced malignancies. J Clin Oncol 28:15s, 2010 (suppl; abstr 3030).
    • (2010) J Clin Oncol , vol.28
    • Brana, I.1    Lorusso, P.2    Baselga, J.3    Heath, E.I.4    Patnaik, A.5    Gendreau, S.6
  • 82
    • 77956602070 scopus 로고    scopus 로고
    • A first-in-human phase i study of BKM120, an oral pan-class i PI3K inhibitor, in patients (pts) with advanced solid tumors
    • suppl abstr 3003
    • Baselga J, De Jonge MJ, Rodon J, Burris HA, Birle DC, De Buck SS, et al. A first-in-human phase I study of BKM120, an oral pan-class I PI3K inhibitor, in patients (pts) with advanced solid tumors. J Clin Oncol 28:15s, 2010 (suppl; abstr 3003).
    • (2010) J Clin Oncol , vol.28
    • Baselga, J.1    De Jonge, M.J.2    Rodon, J.3    Burris, H.A.4    Birle, D.C.5    De Buck, S.S.6
  • 83
    • 77956566979 scopus 로고    scopus 로고
    • A phase i dose-escalation study of XL147 (SAR245408), a PI3K inhibitor administered orally to patients (pts) with advanced malignancies
    • suppl abstr 3004
    • Edelman G, Bedell C, Shapiro G, Pandya SS, Kwak EL, Scheffold C, et al. A phase I dose-escalation study of XL147 (SAR245408), a PI3K inhibitor administered orally to patients (pts) with advanced malignancies. J Clin Oncol 28:15s, 2010 (suppl; abstr 3004).
    • (2010) J Clin Oncol , vol.28
    • Edelman, G.1    Bedell, C.2    Shapiro, G.3    Pandya, S.S.4    Kwak, E.L.5    Scheffold, C.6
  • 84
    • 52449106253 scopus 로고    scopus 로고
    • The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin- 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
    • Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin- 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 2008;51: 5522-32.
    • (2008) J Med Chem , vol.51 , pp. 5522-5532
    • Folkes, A.J.1    Ahmadi, K.2    Alderton, W.K.3    Alix, S.4    Baker, S.J.5    Box, G.6
  • 85
    • 84899823533 scopus 로고    scopus 로고
    • The evolution of PI3 kinase inhibitors: Results of a firstin human phase i study of BAY 80-6946 in patients with advanced solid tumors
    • 2
    • Patnaik A, Ramanathan R, Dubowy R, Tolcher A, Papadopoulos K, Beeram M, et al. The evolution of PI3 kinase inhibitors: results of a firstin human phase I study of BAY 80-6946 in patients with advanced solid tumors. Ann Oncol 2012;23:L2. 2.
    • (2012) Ann Oncol , vol.23
    • Patnaik, A.1    Ramanathan, R.2    Dubowy, R.3    Tolcher, A.4    Papadopoulos, K.5    Beeram, M.6


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