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Volumn , Issue , 2009, Pages 41-56

Tykerb Discovery: A Dual EGFR and ERBB2 Tyrosine Kinase Inhibitor

Author keywords

Drug candidate selection; Inhibiting erbB2 and EGFR tyrosine kinase activity; Tykerb discovery dual EGFR and erbB2 tyrosine kinase inhibitor

Indexed keywords


EID: 84889805263     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1002/9780470524961.ch2     Document Type: Chapter
Times cited : (1)

References (36)
  • 1
    • 0030795612 scopus 로고    scopus 로고
    • The erbB signaling network in embryogenesis and oncogenesis: signal diversification through combinatorial ligand-receptor interactions
    • Alroy, I., and Yarden, Y. (1997). The erbB signaling network in embryogenesis and oncogenesis: signal diversification through combinatorial ligand-receptor interactions . FEBS Lett. 410, 83-86.
    • (1997) FEBS Lett. , vol.410 , pp. 83-86
    • Alroy, I.1    Yarden, Y.2
  • 2
    • 0033763084 scopus 로고    scopus 로고
    • ZD1839 (" Iressa ") as an anticancer agent
    • Baselga, J., and Averbuch, S. G. (2000). ZD1839 (" Iressa ") as an anticancer agent. Drugs. 60 (Suppl. 1), 33-40.
    • (2000) Drugs. , vol.60 , Issue.1 SUPPL , pp. 33-40
    • Baselga, J.1    Averbuch, S.G.2
  • 3
    • 20844437246 scopus 로고    scopus 로고
    • Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR -ErbB-2 inhibitor, in healthy subjects
    • Bence, A. K., Anderson, E. B., Halepota, M. A., et al. (2005). Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR -ErbB-2 inhibitor, in healthy subjects. Invest New Drugs. 23 (1), 39-49.
    • (2005) Invest New Drugs. , vol.23 , Issue.1 , pp. 39-49
    • Bence, A.K.1    Anderson, E.B.2    Halepota, M.A.3
  • 4
    • 0029005367 scopus 로고
    • Prognostic relevance of aberrations in the erbB oncogenes from breast, ovarian, oral and lung cancers: double-differential polymerase chain reaction (ddPCR) for clinical diagnosis
    • Brandt, B., Vogt, U., Sclotter, C. M., et al. (1995). Prognostic relevance of aberrations in the erbB oncogenes from breast, ovarian, oral and lung cancers: double-differential polymerase chain reaction (ddPCR) for clinical diagnosis. Gene. 159, 35-42.
    • (1995) Gene. , vol.159 , pp. 35-42
    • Brandt, B.1    Vogt, U.2    Sclotter, C.M.3
  • 5
    • 0037059757 scopus 로고    scopus 로고
    • Comparison of the biochemical and kinetic properties of the type 1 receptor tyrosine kinase intracellular domains:demonstration of differential sensitivity to kinase inhibitors
    • Brignola, P. S., Lackey, K., Kadwell, S. H., et al. (2002). Comparison of the biochemical and kinetic properties of the type 1 receptor tyrosine kinase intracellular domains:demonstration of differential sensitivity to kinase inhibitors. J Biol Chem. 277 (2), 1576-1585.
    • (2002) J Biol Chem. , vol.277 , Issue.2 , pp. 1576-1585
    • Brignola, P.S.1    Lackey, K.2    Kadwell, S.H.3
  • 6
    • 0035806197 scopus 로고    scopus 로고
    • Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and c-erbB-2
    • Cockerill, G. S., Stubberfield, C., Stables, J., et al. (2001). Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and c-erbB-2. Bioorg Med Chem Lett. 11 (11), 1401-1405.
    • (2001) Bioorg Med Chem Lett. , vol.11 , Issue.11 , pp. 1401-1405
    • Cockerill, G.S.1    Stubberfield, C.2    Stables, J.3
  • 7
    • 0036214044 scopus 로고    scopus 로고
    • The ErbB receptor family: a therapeutic target for cancer
    • de Bono, J. S., and Rowinsky, E. K. (2002). The ErbB receptor family: a therapeutic target for cancer. Trends Mol Med. 8 (4), S19-S26.
    • (2002) Trends Mol Med. , vol.8 , Issue.4
    • de Bono, J.S.1    Rowinsky, E.K.2
  • 8
    • 0021281324 scopus 로고
    • Close similarity of epidermal growth factor receptor and v-erbB oncogene protein sequences
    • Downward, J., Yarden, Y., Mayes, E., et al. (1984). Close similarity of epidermal growth factor receptor and v-erbB oncogene protein sequences. Nature. 307, 521-527.
    • (1984) Nature. , vol.307 , pp. 521-527
    • Downward, J.1    Yarden, Y.2    Mayes, E.3
  • 9
    • 19744365702 scopus 로고    scopus 로고
    • A small molecule-kinase interaction map for clinical kinase inhibitors
    • Fabian, M. A., Biggs, W. H., Treiber, D. K., et al. (2005). A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol. 23 (3), 329-336.
    • (2005) Nat Biotechnol. , vol.23 , Issue.3 , pp. 329-336
    • Fabian, M.A.1    Biggs, W.H.2    Treiber, D.K.3
  • 10
    • 0028142387 scopus 로고
    • A specific inhibitor of the epidermal growth factor receptor tyrosine kinase
    • Fry, D. W., Kraker, A. J., McMichael, A., et al. (1994). A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 265 (5175), 1093-1095.
    • (1994) Science. , vol.265 , Issue.5175 , pp. 1093-1095
    • Fry, D.W.1    Kraker, A.J.2    McMichael, A.3
  • 11
    • 0032933182 scopus 로고    scopus 로고
    • New model of erbB-2 over-expression in human mammary luminal epithelial cells
    • Harris, R. A., Eichholtz, T. J., Hiles, I. D., et al. (1999). New model of erbB-2 over-expression in human mammary luminal epithelial cells. Int J Cancer. 80 (3), 477-484.
    • (1999) Int J Cancer. , vol.80 , Issue.3 , pp. 477-484
    • Harris, R.A.1    Eichholtz, T.J.2    Hiles, I.D.3
  • 12
    • 1942453243 scopus 로고    scopus 로고
    • Ligand efficiency: a useful metric for lead selection
    • Hopkins, A. L., Groom, C. R., and Alex, A. (2004). Ligand efficiency: a useful metric for lead selection. Drug Discov Today. 9 (10), 430-431.
    • (2004) Drug Discov Today. , vol.9 , Issue.10 , pp. 430-431
    • Hopkins, A.L.1    Groom, C.R.2    Alex, A.3
  • 13
    • 38049018155 scopus 로고    scopus 로고
    • A quantitative analysis of kinase inhibitor selectivity
    • Karaman, M. W., Herrgard, S., Treiber, D. K., et al. (2008). A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 26 (1), 127-132.
    • (2008) Nat Biotechnol. , vol.26 , Issue.1 , pp. 127-132
    • Karaman, M.W.1    Herrgard, S.2    Treiber, D.K.3
  • 14
    • 0242529140 scopus 로고    scopus 로고
    • Anti-tumor activity of GW2016 in the erbB-2 positive human breast cancer xenograft, BT474
    • Proceedings of the American Association of Cancer Research 92nd Annual Meeting.
    • Keith, B. R., Allen, P. P., Alligood, K. J., et al. (2001). Anti-tumor activity of GW2016 in the erbB-2 positive human breast cancer xenograft, BT474. Proceedings of the American Association of Cancer Research 92nd Annual Meeting.
    • (2001)
    • Keith, B.R.1    Allen, P.P.2    Alligood, K.J.3
  • 15
    • 0033992633 scopus 로고    scopus 로고
    • Biochemical and clinical implications of the erbB/HER signaling network of growth factor receptors
    • Klapper, L. N., Kirschbaum, M. H., Sela, M., and Yarden, Y. (2000). Biochemical and clinical implications of the erbB/HER signaling network of growth factor receptors. Adv Cancer Res. 77 : 25-79.
    • (2000) Adv Cancer Res. , vol.77 , pp. 25-79
    • Klapper, L.N.1    Kirschbaum, M.H.2    Sela, M.3    Yarden, Y.4
  • 16
    • 33646125891 scopus 로고    scopus 로고
    • Lessons from the drug discovery of lapatinib, a dual ErbB1/2 tyrosine kinase inhibitor
    • Lackey, K. E. (2006). Lessons from the drug discovery of lapatinib, a dual ErbB1/2 tyrosine kinase inhibitor. Curr Topics Med Chem. 6 (5), 435-460.
    • (2006) Curr Topics Med Chem. , vol.6 , Issue.5 , pp. 435-460
    • Lackey, K.E.1
  • 17
    • 0035423120 scopus 로고    scopus 로고
    • Signaling-inactive epidermal growth factor receptor/ligand complexes in intact carcinoma cells by quinazoline tyrosine kinase inhibitors
    • Lichtner, R. B., Menrad, A., Sommer, A., et al. (2001). Signaling-inactive epidermal growth factor receptor/ligand complexes in intact carcinoma cells by quinazoline tyrosine kinase inhibitors. Cancer Res. 61, 5790-5795.
    • (2001) Cancer Res. , vol.61 , pp. 5790-5795
    • Lichtner, R.B.1    Menrad, A.2    Sommer, A.3
  • 18
    • 0031024171 scopus 로고    scopus 로고
    • Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    • Lipinski, C. A., Lombardo, F., Dominy, B. W., and Feeney, P. J. (1997). Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Delivery Rev. 23 (1-3), 3-25.
    • (1997) Adv Drug Delivery Rev. , vol.23 , Issue.1-3 , pp. 3-25
    • Lipinski, C.A.1    Lombardo, F.2    Dominy, B.W.3    Feeney, P.J.4
  • 19
    • 0031817827 scopus 로고    scopus 로고
    • EGFR blockade by tyrosine kinase inhibitor or monoclonal antibody inhibits growth, directs terminal differentiation and induces apoptosis in the human squamous cell carcinoma HN5
    • Modjtahedi, H., Affleck, K., Stubberfield, C., and Dean, C. (1998). EGFR blockade by tyrosine kinase inhibitor or monoclonal antibody inhibits growth, directs terminal differentiation and induces apoptosis in the human squamous cell carcinoma HN5. Int J Oncol. 13, 335-342.
    • (1998) Int J Oncol. , vol.13 , pp. 335-342
    • Modjtahedi, H.1    Affleck, K.2    Stubberfield, C.3    Dean, C.4
  • 20
    • 0032939325 scopus 로고    scopus 로고
    • Multiple positive and negative regulators of signaling by the EGF-receptor
    • Moghal, N., and Sternberg, P. W. (1999). Multiple positive and negative regulators of signaling by the EGF-receptor. Curr Opin Cell Biol. 11 (2), 190-196.
    • (1999) Curr Opin Cell Biol. , vol.11 , Issue.2 , pp. 190-196
    • Moghal, N.1    Sternberg, P.W.2
  • 21
    • 33646137744 scopus 로고    scopus 로고
    • Discovery and profile of GW572016, a dual reversible EGFR/ErbB-2 tyrosine kinase inhibitor
    • Abstracts of Papers, 226th ACS National Meeting, New York.
    • Mullin, R. J. (2003). Discovery and profile of GW572016, a dual reversible EGFR/ErbB-2 tyrosine kinase inhibitor. Abstracts of Papers, 226th ACS National Meeting, New York.
    • (2003)
    • Mullin, R.J.1
  • 22
    • 0027450792 scopus 로고
    • Expression of the c-erbB-2 gene in the BT474 human mammary tumor cell line: measurement of c-erbB-2 mRNA half-life
    • Pasleau, F., Grooteclaes, M., and Gol-Winkler, R. (1993). Expression of the c-erbB-2 gene in the BT474 human mammary tumor cell line: measurement of c-erbB-2 mRNA half-life. Oncogene. 8, 849-854.
    • (1993) Oncogene. , vol.8 , pp. 849-854
    • Pasleau, F.1    Grooteclaes, M.2    Gol-Winkler, R.3
  • 23
    • 10644235453 scopus 로고    scopus 로고
    • Targeting protein kinases in cancer therapy: a success?
    • Pearson, M. A., and Fabbro, D. (2004). Targeting protein kinases in cancer therapy: a success? Exp Rev Anticancer Ther. 4 (6), 1113-1124.
    • (2004) Exp Rev Anticancer Ther. , vol.4 , Issue.6 , pp. 1113-1124
    • Pearson, M.A.1    Fabbro, D.2
  • 24
    • 3042782959 scopus 로고    scopus 로고
    • Epidermal growth factor receptor tyrosine kinase inhibitors
    • Ranson, M. (2004). Epidermal growth factor receptor tyrosine kinase inhibitors. Br J Cancer. 90 (12), 2250-2255.
    • (2004) Br J Cancer. , vol.90 , Issue.12 , pp. 2250-2255
    • Ranson, M.1
  • 25
    • 0031936410 scopus 로고    scopus 로고
    • Specificity within the EGF family/ErbB receptor family signaling network
    • Riese, D. J., and Stern, D. F. (1998). Specificity within the EGF family/ErbB receptor family signaling network. BioEssays. 20 (1), 41-48.
    • (1998) BioEssays. , vol.20 , Issue.1 , pp. 41-48
    • Riese, D.J.1    Stern, D.F.2
  • 26
    • 0035476866 scopus 로고    scopus 로고
    • The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer
    • Rusnak, D. W., Affleck, K., Cockerill, S. G., et al. (2001a). The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer. Cancer Res. 61 (19), 7196-7203.
    • (2001) Cancer Res. , vol.61 , Issue.19 , pp. 7196-7203
    • Rusnak, D.W.1    Affleck, K.2    Cockerill, S.G.3
  • 27
    • 0035553174 scopus 로고    scopus 로고
    • The effects of the novel, reversible EGFR/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo
    • Rusnak, D. W., Lackey, K., Affleck, K., et al. (2001b). The effects of the novel, reversible EGFR/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 1 (2), 85-94.
    • (2001) Mol Cancer Ther. , vol.1 , Issue.2 , pp. 85-94
    • Rusnak, D.W.1    Lackey, K.2    Affleck, K.3
  • 28
    • 0023279839 scopus 로고
    • Epidermal-growth-factor receptor status as predictor of early recurrence of and death from breast cancer
    • Sainsbury, J. R., Farndon, J. R., Needham, G. K., et al. (1987). Epidermal-growth-factor receptor status as predictor of early recurrence of and death from breast cancer. Lancet. 1398-1402.
    • (1987) Lancet. , pp. 1398-1402
    • Sainsbury, J.R.1    Farndon, J.R.2    Needham, G.K.3
  • 29
    • 0010066582 scopus 로고
    • A v-erbB-related protooncogene, c-erbB-2, is distinct from the c-erbB-1/epidermal growth factor-receptor gene and is amplified in a human salivary gland adenocarcinoma
    • Semba, K., Kamata, N., Toyoshima, K., and Yamamoto, T. (1985). A v-erbB-related protooncogene, c-erbB-2, is distinct from the c-erbB-1/epidermal growth factor-receptor gene and is amplified in a human salivary gland adenocarcinoma. Proc Natl Acad Sci USA. 82, 6497-6501.
    • (1985) Proc Natl Acad Sci USA. , vol.82 , pp. 6497-6501
    • Semba, K.1    Kamata, N.2    Toyoshima, K.3    Yamamoto, T.4
  • 30
    • 0033008412 scopus 로고    scopus 로고
    • Use of " N-in-one " dosing to create an in vivo pharmacokinetics database for use in developing structure-pharmacokinetic relationships
    • Shaffer, J. E., Adkison, K. K., Halm, K., et al. (1999). Use of " N-in-one " dosing to create an in vivo pharmacokinetics database for use in developing structure-pharmacokinetic relationships. J Pharm Sci. 88 (3), 313-318.
    • (1999) J Pharm Sci. , vol.88 , Issue.3 , pp. 313-318
    • Shaffer, J.E.1    Adkison, K.K.2    Halm, K.3
  • 31
    • 20244388653 scopus 로고    scopus 로고
    • Study of the biologic effects of lapatinib, a reversible inhibitor of ErbB1 and ErbB-2 tyrosine kinases, on tumor growth and survival pathways in patients with advanced malignancies
    • Spector, N. L., Xia, W., Burris, H., et al. (2005). Study of the biologic effects of lapatinib, a reversible inhibitor of ErbB1 and ErbB-2 tyrosine kinases, on tumor growth and survival pathways in patients with advanced malignancies. J Clin Oncol. 23 (11), 2502-2512.
    • (2005) J Clin Oncol. , vol.23 , Issue.11 , pp. 2502-2512
    • Spector, N.L.1    Xia, W.2    Burris, H.3
  • 32
    • 0141599428 scopus 로고    scopus 로고
    • Structure of the EGF receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor
    • Stamos, J., Sliwkowski, M. X., and Eigenbrot, C. (2002). Structure of the EGF receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J Biol Chem. 277, 46265-46272.
    • (2002) J Biol Chem. , vol.277 , pp. 46265-46272
    • Stamos, J.1    Sliwkowski, M.X.2    Eigenbrot, C.3
  • 33
    • 1642442499 scopus 로고    scopus 로고
    • Epidermal growth factor receptor inhibitors: a new prospective in the treatment of lung cancer
    • Tiseo, M., Loprevite, M., and Ardizzoni, A. (2004). Epidermal growth factor receptor inhibitors: a new prospective in the treatment of lung cancer. Curr Med Chem Anticancer Agents. 4 (2), 139-148.
    • (2004) Curr Med Chem Anticancer Agents. , vol.4 , Issue.2 , pp. 139-148
    • Tiseo, M.1    Loprevite, M.2    Ardizzoni, A.3
  • 34
    • 4644289313 scopus 로고    scopus 로고
    • Unique structure for epidermal growth factor receptor bound to GW572016 (lapatinib): relationship between protein conformation, inhibitor off-rate, and receptor activity in tumor cells
    • Wood, E. R., Truesdale, A. T., McDonald, O. B., et al. (2004). Unique structure for epidermal growth factor receptor bound to GW572016 (lapatinib): relationship between protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res. 64 (18), 6652-6659.
    • (2004) Cancer Res. , vol.64 , Issue.18 , pp. 6652-6659
    • Wood, E.R.1    Truesdale, A.T.2    McDonald, O.B.3
  • 35
    • 0037068741 scopus 로고    scopus 로고
    • Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB-2 and downstream Erk1/2 and AKT pathways
    • Xia, W., Mullin, R. J., Keith, B. R., et al. (2002). Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB-2 and downstream Erk1/2 and AKT pathways. Oncogene. 21 (41), 6255-6263.
    • (2002) Oncogene. , vol.21 , Issue.41 , pp. 6255-6263
    • Xia, W.1    Mullin, R.J.2    Keith, B.R.3
  • 36
    • 0035256698 scopus 로고    scopus 로고
    • Untangling the erbB signaling network
    • Yarden, Y., and Sliwkowski, M. X. (2001). Untangling the erbB signaling network. Nature Rev. 2, 127-137.
    • (2001) Nature Rev. , vol.2 , pp. 127-137
    • Yarden, Y.1    Sliwkowski, M.X.2


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