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Volumn 9, Issue 3, 2014, Pages

Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use

Author keywords

[No Author keywords available]

Indexed keywords

ABL1 INHIBITOR; AFATINIB; AXITINIB; B RAF KINASE INHIBITOR; BORTEZOMIB; BOSUTINIB; CABOZANTINIB; CRIZOTINIB; DABRAFENIB; DASATINIB; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; EVEROLIMUS; FASUDIL; GEFITINIB; IMATINIB; LAPATINIB; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; NILOTINIB; PAZOPANIB; PHOSPHOTRANSFERASE INHIBITOR; PONATINIB; REGORAFENIB; RUXOLITINIB; SORAFENIB; SUNITINIB; TEMSIROLIMUS; TOFACITINIB; TRAMETINIB; UNCLASSIFIED DRUG; VANDETANIB; VEMURAFENIB; GENETIC MARKER; PROTEIN KINASE INHIBITOR; PROTEOME;

EID: 84901281392     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0092146     Document Type: Article
Times cited : (85)

References (55)
  • 1
  • 2
    • 84877278637 scopus 로고    scopus 로고
    • Implementing personalized cancer genomics in clinical trials
    • Simon R, Roychowdbury S (2013) Implementing personalized cancer genomics in clinical trials. Nature Rev Drug Disc 12: 358-369.
    • (2013) Nature Rev Drug Disc , vol.12 , pp. 358-369
    • Simon, R.1    Roychowdbury, S.2
  • 3
    • 79952284127 scopus 로고    scopus 로고
    • Hallmarks of cancer: The next generation
    • Hanahan D,Weinberg RA (2011) Hallmarks of cancer: the next generation. Cell 144: 646-674.
    • (2011) Cell , vol.144 , pp. 646-674
    • Hanahan, D.1    Weinberg, R.A.2
  • 4
    • 84859187259 scopus 로고    scopus 로고
    • Systematic identification of genomic markers of drug sensitivity in cancer cells
    • Garnett MJ, Edelman EJ, Heidorn SJ, Greenman CD, Dastur A, et al. (2012) Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature 483: 570-575.
    • (2012) Nature , vol.483 , pp. 570-575
    • Garnett, M.J.1    Edelman, E.J.2    Heidorn, S.J.3    Greenman, C.D.4    Dastur, A.5
  • 5
    • 84859169877 scopus 로고    scopus 로고
    • The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity
    • Barretina J, Caponigro G, Stransky N, Venkatesan K, Margolin AA, et al. (2013) The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity. Nature 483: 603-607.
    • (2013) Nature , vol.483 , pp. 603-607
    • Barretina, J.1    Caponigro, G.2    Stransky, N.3    Venkatesan, K.4    Margolin, A.A.5
  • 6
    • 77951717316 scopus 로고    scopus 로고
    • Molecular target class is predictive of in vitro response profile
    • Greshock J, Bachman KE, Degenhardt YY, Jing J, Wen YH, et al. (2010) Molecular target class is predictive of in vitro response profile. Cancer Res 70: 3677-3686.
    • (2010) Cancer Res , vol.70 , pp. 3677-3686
    • Greshock, J.1    Bachman, K.E.2    Degenhardt, Y.Y.3    Jing, J.4    Wen, Y.H.5
  • 7
    • 38049097938 scopus 로고    scopus 로고
    • Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling
    • McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, et al. (2007) Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci USA 104: 19936-19941.
    • (2007) Proc Natl Acad Sci USA , vol.104 , pp. 19936-19941
    • McDermott, U.1    Sharma, S.V.2    Dowell, L.3    Greninger, P.4    Montagut, C.5
  • 8
    • 77949957365 scopus 로고    scopus 로고
    • Cell line-based platforms to evaluate the therapeutic efficacy of candidate anticancer agents
    • Sharma SV, Haber DA, Settleman J (2010) Cell line-based platforms to evaluate the therapeutic efficacy of candidate anticancer agents. Nature Rev Cancer 10: 241-253.
    • (2010) Nature Rev Cancer , vol.10 , pp. 241-253
    • Sharma, S.V.1    Haber, D.A.2    Settleman, J.3
  • 9
    • 33749011163 scopus 로고    scopus 로고
    • The NCI human tumour cell line anticancer screen
    • Shoemaker RH (2006) The NCI human tumour cell line anticancer screen. Nature Rev Cancer 6: 813-823.
    • (2006) Nature Rev Cancer , vol.6 , pp. 813-823
    • Shoemaker, R.H.1
  • 11
    • 84873056956 scopus 로고    scopus 로고
    • Activity-based kinase profiling of approved tyrosine kinase inhibitors
    • Kitagawa D, Yokota K, Gouda M, Narumi Y, Ohmoto H, et al. (2013) Activity-based kinase profiling of approved tyrosine kinase inhibitors. Genes to cells 18: 110-122.
    • (2013) Genes to Cells , vol.18 , pp. 110-122
    • Kitagawa, D.1    Yokota, K.2    Gouda, M.3    Narumi, Y.4    Ohmoto, H.5
  • 14
    • 84860851057 scopus 로고    scopus 로고
    • A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets
    • Uitdehaag JCM, Verkaar FA, Alwan H, de Man J, Buijsman RC, et al. (2012) A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets. Br J Pharmacol 166: 858-876.
    • (2012) Br J Pharmacol , vol.166 , pp. 858-876
    • Uitdehaag, J.C.M.1    Verkaar, F.A.2    Alwan, H.3    De Man, J.4    Buijsman, R.C.5
  • 15
    • 83355166909 scopus 로고    scopus 로고
    • Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth
    • Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, et al. (2011) Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther 10: 2298-2308.
    • (2011) Mol Cancer Ther , vol.10 , pp. 2298-2308
    • Yakes, F.M.1    Chen, J.2    Tan, J.3    Yamaguchi, K.4    Shi, Y.5
  • 16
    • 84879754813 scopus 로고    scopus 로고
    • Dabrafenib, preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions
    • King AJ, Arnone MR, Bleam MR, Moss KG, Yang J, et al. (2013) Dabrafenib, preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions. PLOS One 8, e67583.
    • (2013) PLOS One , vol.8
    • King, A.J.1    Arnone, M.R.2    Bleam, M.R.3    Moss, K.G.4    Yang, J.5
  • 17
    • 70350507997 scopus 로고    scopus 로고
    • AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance
    • 2009
    • O'Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, et al. (2009) AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 16: 401-412 (2009).
    • (2009) Cancer Cell , vol.16 , pp. 401-412
    • O'Hare, T.1    Shakespeare, W.C.2    Zhu, X.3    Eide, C.A.4    Rivera, V.M.5
  • 18
    • 79954499886 scopus 로고    scopus 로고
    • Regorafenib (BAY 73-4506): A new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
    • Wilhelm SM, Dumas J, Adnane L, Lynch M, Carter CA, et al. (2011) Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer 129: 245-255.
    • (2011) Int J Cancer , vol.129 , pp. 245-255
    • Wilhelm, S.M.1    Dumas, J.2    Adnane, L.3    Lynch, M.4    Carter, C.A.5
  • 19
    • 84874736379 scopus 로고    scopus 로고
    • Identification and characterization of a novel chemotype MEK inhibitor able to alter the phosphorylation state of MEK1/2
    • Yoshida T, Kakegawa J, Yamaguchi T, Hantani Y, Okajima N, et al. (2012) Identification and characterization of a novel chemotype MEK inhibitor able to alter the phosphorylation state of MEK1/2. Oncotarget 3: 1533-1545.
    • (2012) Oncotarget , vol.3 , pp. 1533-1545
    • Yoshida, T.1    Kakegawa, J.2    Yamaguchi, T.3    Hantani, Y.4    Okajima, N.5
  • 20
    • 77957089182 scopus 로고    scopus 로고
    • The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner
    • Joseph EW, Pratilas CA, Poulikakos PI, Tadi M, Wang W, et al. (2010) The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci USA 107: 14903-14908.
    • (2010) Proc Natl Acad Sci USA , vol.107 , pp. 14903-14908
    • Joseph, E.W.1    Pratilas, C.A.2    Poulikakos, P.I.3    Tadi, M.4    Wang, W.5
  • 25
    • 0028983849 scopus 로고
    • DLD-1 and HCT-15 cell lines derived separately from colorectal carcinomas have totally different chromosome changes but the same genetic origin
    • Chen TR, Dorotinsky CS, McGuire LJ, Macy ML, Hay RJ (1995) DLD-1 and HCT-15 cell lines derived separately from colorectal carcinomas have totally different chromosome changes but the same genetic origin. Cancer Genet Cytogenet 81: 103-108.
    • (1995) Cancer Genet Cytogenet , vol.81 , pp. 103-108
    • Chen, T.R.1    Dorotinsky, C.S.2    McGuire, L.J.3    Macy, M.L.4    Hay, R.J.5
  • 26
    • 15744380263 scopus 로고    scopus 로고
    • Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
    • Ohren JF, Chen H, Pavlovsky A, Whitehead C, Zhang E, et al. (2004) Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nature Struct Mol Biol 11: 1192-1197.
    • (2004) Nature Struct Mol Biol , vol.11 , pp. 1192-1197
    • Ohren, J.F.1    Chen, H.2    Pavlovsky, A.3    Whitehead, C.4    Zhang, E.5
  • 27
    • 84885173677 scopus 로고    scopus 로고
    • Regorafenib as second-line therapy for intermediate or advanced hepatocellular carcinoma: Multicentre, open-label, phase II safety study
    • Bruix J, Tak WY, Gasbarrini A, Santoro A, Colombo M, et al. (2013) Regorafenib as second-line therapy for intermediate or advanced hepatocellular carcinoma: multicentre, open-label, phase II safety study. Eur J Cancer 49: 3412-3419.
    • (2013) Eur J Cancer , vol.49 , pp. 3412-3419
    • Bruix, J.1    Tak, W.Y.2    Gasbarrini, A.3    Santoro, A.4    Colombo, M.5
  • 28
    • 84885638118 scopus 로고    scopus 로고
    • In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET and VEGFR2, in a model of medullary thyroid cancer
    • 2013 Sep 17 [epub ahead of print]
    • Bentzien F, Zuzow M, Heald N, Gibson A, Shi Y, et al. (2013) In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET and VEGFR2, in a model of medullary thyroid cancer Thyroid. 2013 Sep 17 [epub ahead of print].
    • (2013) Thyroid
    • Bentzien, F.1    Zuzow, M.2    Heald, N.3    Gibson, A.4    Shi, Y.5
  • 30
    • 36549040859 scopus 로고    scopus 로고
    • The selectivity of protein kinase inhibitors: A further update
    • Bain J, Plater L, Elliott M, Shapiro N, Hastie CJ, et al. (2007) The selectivity of protein kinase inhibitors: a further update. Biochem J 408: 297-315.
    • (2007) Biochem J , vol.408 , pp. 297-315
    • Bain, J.1    Plater, L.2    Elliott, M.3    Shapiro, N.4    Hastie, C.J.5
  • 31
    • 84867928657 scopus 로고    scopus 로고
    • System-based drug discovery within the human kinome
    • Bamborough P (2012) System-based drug discovery within the human kinome. Expert Opin Drug Discovery 7: 1053-1070.
    • (2012) Expert Opin Drug Discovery , vol.7 , pp. 1053-1070
    • Bamborough, P.1
  • 33
    • 79953837902 scopus 로고    scopus 로고
    • A theoretical entropy score as a single value to express inhibitor selectivity
    • Uitdehaag JCM, Zaman GJ (2011) A theoretical entropy score as a single value to express inhibitor selectivity. BMC Bioinformatics 12: 94.
    • (2011) BMC Bioinformatics , vol.12 , pp. 94
    • Uitdehaag, J.C.M.1    Zaman, G.J.2
  • 34
    • 65049090992 scopus 로고    scopus 로고
    • Ephrin A5 acts as a tumor suppressor in glioma by negative regulation of epidermal growth factor receptor
    • Li JJ, Liu DP, Liu GT, Xie D (2009) Ephrin A5 acts as a tumor suppressor in glioma by negative regulation of epidermal growth factor receptor. Oncogene 28: 1759-1768.
    • (2009) Oncogene , vol.28 , pp. 1759-1768
    • Li, J.J.1    Liu, D.P.2    Liu, G.T.3    Xie, D.4
  • 35
    • 0036401105 scopus 로고    scopus 로고
    • BAY 43-9006: Preclinical data
    • DOI 10.2174/1381612023393026
    • Wilhelm S, Chien DS (2002) BAY 43-9006: preclinical data. Curr Pharm Design 8: 2255-2257. (Pubitemid 35189898)
    • (2002) Current Pharmaceutical Design , vol.8 , Issue.25 , pp. 2255-2257
    • Wilhelm, S.1    Chien, D.-S.2
  • 36
    • 57749188299 scopus 로고    scopus 로고
    • Targeting cancer with small molecule kinase inhibitors
    • Zhang J, Yang PL, Gray NS (2009) Targeting cancer with small molecule kinase inhibitors Nature Rev Cancer 9: 28-39.
    • (2009) Nature Rev Cancer , vol.9 , pp. 28-39
    • Zhang, J.1    Yang, P.L.2    Gray, N.S.3
  • 37
    • 84863230465 scopus 로고    scopus 로고
    • Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR
    • Prahallad A, Sun C, Huang S, Nicolantonio F, Salazar R, et al. (2012) Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature 483: 100-103.
    • (2012) Nature , vol.483 , pp. 100-103
    • Prahallad, A.1    Sun, C.2    Huang, S.3    Nicolantonio, F.4    Salazar, R.5
  • 38
    • 75149130051 scopus 로고    scopus 로고
    • Targeting the cancer kinome through polypharmacology
    • Knight ZA, Lin H, Shokat KM (2010) Targeting the cancer kinome through polypharmacology. Nature Rev Cancer 10: 130-137.
    • (2010) Nature Rev Cancer , vol.10 , pp. 130-137
    • Knight, Z.A.1    Lin, H.2    Shokat, K.M.3
  • 39
    • 77649204688 scopus 로고    scopus 로고
    • Selectively nonselective kinase inhibition: Striking the right balance
    • Morphy R (2010) Selectively nonselective kinase inhibition: striking the right balance. J Med Chem 53: 1413-1437.
    • (2010) J Med Chem , vol.53 , pp. 1413-1437
    • Morphy, R.1
  • 41
    • 84859713534 scopus 로고    scopus 로고
    • Ras stabilization through aberrant activation of Wnt/β-catenin signaling promotes intestinal tumorigenesis
    • Jeong W-J, Yoon J, Park JC, Lee SH, Kaduwal S, et al. (2012) Ras stabilization through aberrant activation of Wnt/β-catenin signaling promotes intestinal tumorigenesis. Science Signaling 5: ra30.
    • (2012) Science Signaling , vol.5
    • Jeong, W.-J.1    Yoon, J.2    Park, J.C.3    Lee, S.H.4    Kaduwal, S.5
  • 42
    • 77952316612 scopus 로고    scopus 로고
    • De novo stabilization of β-catenin via H-Ras and MEK regulates airway smooth muscle growth
    • Gosens R, Baarsma HA, Heijink IH, Oenema TA, Halayko AJ, et al. (2010) De novo stabilization of β-catenin via H-Ras and MEK regulates airway smooth muscle growth. The FASEB J 24: 757-768.
    • (2010) The FASEB J , vol.24 , pp. 757-768
    • Gosens, R.1    Baarsma, H.A.2    Heijink, I.H.3    Oenema, T.A.4    Halayko, A.J.5
  • 43
    • 77956642350 scopus 로고    scopus 로고
    • Expression of oncogenic K-ras and loss of Smad4 cooperate to induce the expression of EGFR and to promote invasion of immortalized human pancreas ductal cells
    • Zhao S, Wang Y, Cao L, Ouellette MM, Freeman JW (2010) Expression of oncogenic K-ras and loss of Smad4 cooperate to induce the expression of EGFR and to promote invasion of immortalized human pancreas ductal cells. Int J Cancer 127: 2076-2086.
    • (2010) Int J Cancer , vol.127 , pp. 2076-2086
    • Zhao, S.1    Wang, Y.2    Cao, L.3    Ouellette, M.M.4    Freeman, J.W.5
  • 44
    • 19944427126 scopus 로고    scopus 로고
    • Coexpression of matrix metalloproteinase-7 (MMP-7) and epidermal growth factor (EGF) receptor in colorectal cancer: An EGF receptor tyrosine kinase inhibitor is effective against MMP-7 - Expressing cancer cells
    • DOI 10.1158/1078-0432.CCR-04-0849
    • Mimori K, Yamashita K, Ohta M, Yoshinaga K, Ishikawa K, et al. (2004) Coexpression of matrix metalloproteinase-7 (MMP-7) and epidermal growth factor (EGF) receptor in colorectal cancer: an EGF receptor tyrosine kinase inhibitor is effective against MMP-7 expressing cancer cells. Clin Cancer Res 10, 8243-8249. (Pubitemid 40053384)
    • (2004) Clinical Cancer Research , vol.10 , Issue.24 , pp. 8243-8249
    • Mimori, K.1    Yamashita, K.2    Ohta, M.3    Yoshinaga, K.4    Ishikawa, K.5    Ishii, H.6    Utsunomiya, T.7    Barnard, G.F.8    Inoue, H.9    Mori, M.10
  • 46
    • 77956920417 scopus 로고    scopus 로고
    • ABL tyrosine kinases: Evolution of function, regulation and specificity
    • Colicelli J (2010) ABL tyrosine kinases: evolution of function, regulation and specificity. Sci Signal 3: (139) re6.
    • (2010) Sci Signal , vol.3 , Issue.139
    • Colicelli, J.1
  • 47
    • 84859610210 scopus 로고    scopus 로고
    • c-Abl and Arg are activated in human primary melanomas, promote melanoma cell invasion via distinct pathways, and drive metastatic progression
    • Ganguly SS, Fiore LS, Sims JT, Friend JW, Srinivasan D (2012) c-Abl and Arg are activated in human primary melanomas, promote melanoma cell invasion via distinct pathways, and drive metastatic progression. Oncogene 31: 1804-1816.
    • (2012) Oncogene , vol.31 , pp. 1804-1816
    • Ganguly, S.S.1    Fiore, L.S.2    Sims, J.T.3    Friend, J.W.4    Srinivasan, D.5
  • 48
    • 84863304598 scopus 로고    scopus 로고
    • R development core team R Foundation for statistical computing, Vienna, Austria
    • R development core team (2008) R: a language and environment for statistical computing. R Foundation for statistical computing, Vienna, Austria.
    • (2008) R: A Language and Environment for Statistical Computing
  • 49
    • 84944178665 scopus 로고
    • Hierarchical grouping to optimize an objective function
    • Ward JH Jr (1963) Hierarchical grouping to optimize an objective function. J Am Stat Assoc 58: 236-244.
    • (1963) J Am Stat Assoc , vol.58 , pp. 236-244
    • Ward Jr., J.H.1
  • 51
    • 78249279676 scopus 로고    scopus 로고
    • The tyrosine kinase c-Abl promotes proliferation and is expressed in atypical tertoid and malignant rhabdoid tumors
    • Koos B, Jeibmann A, Lünenbürger H, Mertsch S, Nupponen NN (2010) The tyrosine kinase c-Abl promotes proliferation and is expressed in atypical tertoid and malignant rhabdoid tumors. Cancer 116: 5075-5081.
    • (2010) Cancer , vol.116 , pp. 5075-5081
    • Koos, B.1    Jeibmann, A.2    Lünenbürger, H.3    Mertsch, S.4    Nupponen, N.N.5
  • 53
    • 0001677717 scopus 로고
    • Controlling the false discovery rate: A practical and powerful approach to multiple testing
    • Benjamini Y, Hochberg Y (1995) Controlling the false discovery rate: a practical and powerful approach to multiple testing. J Royal Statistic Soc B 57: 289-300.
    • (1995) J Royal Statistic Soc B , vol.57 , pp. 289-300
    • Benjamini, Y.1    Hochberg, Y.2
  • 54
    • 84871604633 scopus 로고    scopus 로고
    • Theoretical and experimental relationships between percent inhibition and IC50 data observed in high-throughput screening
    • Gubler H, Schopfer U, Jacoby E (2013) Theoretical and experimental relationships between percent inhibition and IC50 data observed in high-throughput screening. J Biomol Screen 18: 1-13.
    • (2013) J Biomol Screen , vol.18 , pp. 1-13
    • Gubler, H.1    Schopfer, U.2    Jacoby, E.3
  • 55
    • 0031657020 scopus 로고    scopus 로고
    • Chemical modification of rapamycin: The discovery of SDZ RAD
    • DOI 10.1016/S0041-1345(98)00587-9, PII S0041134598005879
    • Sedrani R, Cottens S, Kallen J, Schuler W (1998) Chemical modification of rapamycin: the discovery of SDZ RAD. Transplantation proceedings 30: 2192-2194. (Pubitemid 28399473)
    • (1998) Transplantation Proceedings , vol.30 , Issue.5 , pp. 2192-2194
    • Sedrani, R.1    Cottens, S.2    Kallen, J.3    Schuler, W.4


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