메뉴 건너뛰기




Volumn 19, Issue 9, 2014, Pages 15196-15212

Small molecule tyrosine kinase inhibitors of ErbB2/HER2/Neu in the treatment of aggressive breast cancer

Author keywords

HER2 inhibition; Human epidermal growth factor 2 (HER2); Kinase domain; Monoclonal antibodies; Small molecule inhibitors

Indexed keywords

ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR 2; ERBB2 PROTEIN, HUMAN; PROTEIN KINASE INHIBITOR;

EID: 84907439121     PISSN: None     EISSN: 14203049     Source Type: Journal    
DOI: 10.3390/molecules190915196     Document Type: Review
Times cited : (80)

References (88)
  • 2
    • 0027946003 scopus 로고
    • Expression of the erbb-2 family of growth factor receptors and their ligands in breast cancers. Implication for tumor biology and clinical behavior
    • Bacus, S.S.; Zelnick, C.R.; Plowman, G.; Yarden, Y. Expression of the erbb-2 family of growth factor receptors and their ligands in breast cancers. Implication for tumor biology and clinical behavior. Am. J. Clin. Pathol. 1994, 102, S13-S24.
    • (1994) Am. J. Clin. Pathol. , vol.102 , pp. S13-S24
    • Bacus, S.S.1    Zelnick, C.R.2    Plowman, G.3    Yarden, Y.4
  • 3
    • 37049183697 scopus 로고
    • Human breast cancer: Correlation of relapse and survival with amplification of the HER-2/neu oncogene
    • Slamon, D.J.; Clark, G.M.; Wong, S.G.; Levin, W.J.; Ullrich, A.; McGuire, W.L. Human breast cancer: Correlation of relapse and survival with amplification of the HER-2/neu oncogene. Science 1987, 235, 177-182.
    • (1987) Science , vol.235 , pp. 177-182
    • Slamon, D.J.1    Clark, G.M.2    Wong, S.G.3    Levin, W.J.4    Ullrich, A.5    Mc Guire, W.L.6
  • 4
    • 0031903646 scopus 로고    scopus 로고
    • Phase II study of receptor-enhanced chemosensitivity using recombinant humanized anti-p185HER2/neu monoclonal antibody plus cisplatin in patients with HER2/neu-overexpressing metastatic breast cancer refractory to chemotherapy treatment
    • Pegram, M.D.; Lipton, A.; Hayes, D.F.; Weber, B.L.; Baselga, J.M.; Tripathy, D.; Baly, D.; Baughman, S.A.; Twaddell, T.; Glaspy, J.A.; et al. Phase II study of receptor-enhanced chemosensitivity using recombinant humanized anti-p185HER2/neu monoclonal antibody plus cisplatin in patients with HER2/neu-overexpressing metastatic breast cancer refractory to chemotherapy treatment. J. Clin. Oncol. 1998, 16, 2659-2671.
    • (1998) J. Clin. Oncol. , vol.16 , pp. 2659-2671
    • Pegram, M.D.1    Lipton, A.2    Hayes, D.F.3    Weber, B.L.4    Baselga, J.M.5    Tripathy, D.6    Baly, D.7    Baughman, S.A.8    Twaddell, T.9    Glaspy, J.A.10
  • 5
    • 84890257395 scopus 로고    scopus 로고
    • Progress in breast cancer: Overview
    • Arteaga, C.L. Progress in breast cancer: Overview. Clin. Cancer Res. 2013, 19, 6353-6359.
    • (2013) Clin. Cancer Res. , vol.19 , pp. 6353-6359
    • Arteaga, C.L.1
  • 8
    • 18344390418 scopus 로고    scopus 로고
    • Erbb receptors and cancer: The complexity of targeted inhibitors
    • Hynes, N.E.; Lane, H.A. Erbb receptors and cancer: The complexity of targeted inhibitors. Nat. Rev. Cancer 2005, 5, 341-354.
    • (2005) Nat. Rev. Cancer , vol.5 , pp. 341-354
    • Hynes, N.E.1    Lane, H.A.2
  • 9
    • 0031840484 scopus 로고    scopus 로고
    • Erbb-1 and erbb-2 acquire distinct signaling properties dependent upon their dimerization partner
    • Olayioye, M.A.; Graus-Porta, D.; Beerli, R.R.; Rohrer, J.; Gay, B.; Hynes, N.E. Erbb-1 and erbb-2 acquire distinct signaling properties dependent upon their dimerization partner. Mol. Cell. Biol. 1998, 18, 5042-5051.
    • (1998) Mol. Cell. Biol. , vol.18 , pp. 5042-5051
    • Olayioye, M.A.1    Graus-Porta, D.2    Beerli, R.R.3    Rohrer, J.4    Gay, B.5    Hynes, N.E.6
  • 13
    • 84907443858 scopus 로고    scopus 로고
    • Small-molecule inhibitors of the receptor tyrosine kinases: Promising tools for targeted cancer therapies
    • Hojjat-Farsangi, M. Small-molecule inhibitors of the receptor tyrosine kinases: Promising tools for targeted cancer therapies. Int. J. Mol. Sci. 2014, 15, 13768-13801.
    • (2014) Int. J. Mol. Sci. , vol.15 , pp. 13768-13801
    • Hojjat-Farsangi, M.1
  • 14
    • 84906216493 scopus 로고    scopus 로고
    • Inducible tyrosine kinase inhibitors: A review of the patent literature 2010-2013
    • Norman, P. Inducible tyrosine kinase inhibitors: A review of the patent literature (2010-2013). Expert Opin. Ther. Pat. 2014, 24, 979-991.
    • (2014) Expert Opin. Ther. Pat. , vol.24 , pp. 979-991
    • Norman, P.1
  • 15
    • 84903581634 scopus 로고    scopus 로고
    • Erbb/HER protein-tyrosine kinases: Structures and small molecule inhibitors
    • Roskoski, R., Jr. Erbb/HER protein-tyrosine kinases: Structures and small molecule inhibitors. Pharmacol. Res. 2014, 87C, 42-59.
    • (2014) Pharmacol. Res. , vol.87 C , pp. 42-59
    • Roskoski, R.1
  • 16
    • 84902449207 scopus 로고    scopus 로고
    • Targeting receptor tyrosine kinase met in cancer: Small molecule inhibitors and clinical progress
    • Cui, J.J. Targeting receptor tyrosine kinase met in cancer: Small molecule inhibitors and clinical progress. J. Med. Chem. 2014, 57, 4427-4453.
    • (2014) J. Med. Chem. , vol.57 , pp. 4427-4453
    • Cui, J.J.1
  • 17
    • 84885432971 scopus 로고    scopus 로고
    • Targeting receptor tyrosine kinases in HER2-negative breast cancer
    • Anandappa, G.; Turner, N.C. Targeting receptor tyrosine kinases in HER2-negative breast cancer. Curr. Opin. Oncol. 2013, 25, 594-601.
    • (2013) Curr. Opin. Oncol. , vol.25 , pp. 594-601
    • Anandappa, G.1    Turner, N.C.2
  • 19
    • 84876705235 scopus 로고    scopus 로고
    • Targeting HER receptors in cancer
    • Ocana, A.; Pandiella, A. Targeting HER receptors in cancer. Curr. Pharm. Des. 2013, 19, 808-817.
    • (2013) Curr. Pharm. Des. , vol.19 , pp. 808-817
    • Ocana, A.1    Pandiella, A.2
  • 22
    • 84871713793 scopus 로고    scopus 로고
    • Efficacy of HER2-targeted therapy in metastatic breast cancer. Monoclonal antibodies and tyrosine kinase inhibitors
    • Nielsen, D.L.; Kümler, I.; Palshof, J.A.; Andersson, M. Efficacy of HER2-targeted therapy in metastatic breast cancer. Monoclonal antibodies and tyrosine kinase inhibitors. Breast 2013, 22, 1-12.
    • (2013) Breast , vol.22 , pp. 1-12
    • Nielsen, D.L.1    Kümler, I.2    Palshof, J.A.3    Andersson, M.4
  • 23
    • 0029991439 scopus 로고    scopus 로고
    • Phase II study of weekly intravenous recombinant humanized anti-p185HER2 monoclonal antibody in patients with HER2/neu-overexpressing metastatic breast cancer
    • Baselga, J.; Tripathy, D.; Mendelsohn, J.; Baughman, S.; Benz, C.C.; Dantis, L.; Sklarin, N.T.; Seidman, A.D.; Hudis, C.A.; Moore, J.; et al. Phase II study of weekly intravenous recombinant humanized anti-p185HER2 monoclonal antibody in patients with HER2/neu-overexpressing metastatic breast cancer. J. Clin. Oncol. 1996, 14, 737-744.
    • (1996) J. Clin. Oncol. , vol.14 , pp. 737-744
    • Baselga, J.1    Tripathy, D.2    Mendelsohn, J.3    Baughman, S.4    Benz, C.C.5    Dantis, L.6    Sklarin, N.T.7    Seidman, A.D.8    Hudis, C.A.9    Moore, J.10
  • 24
    • 0032850677 scopus 로고    scopus 로고
    • Multinational study of the efficacy and safety of humanized anti-HER2 monoclonal antibody in women who have HER2-overexpressing metastatic breast cancer that has progressed after chemotherapy for metastatic disease
    • Cobleigh, M.A.; Vogel, C.L.; Tripathy, D.; Robert, N.J.; Scholl, S.; Fehrenbacher, L.; Wolter, J.M.; Paton, V.; Shak, S.; Lieberman, G.; et al. Multinational study of the efficacy and safety of humanized anti-HER2 monoclonal antibody in women who have HER2-overexpressing metastatic breast cancer that has progressed after chemotherapy for metastatic disease. J. Clin. Oncol. 1999, 17, 2639-2648.
    • (1999) J. Clin. Oncol. , vol.17 , pp. 2639-2648
    • Cobleigh, M.A.1    Vogel, C.L.2    Tripathy, D.3    Robert, N.J.4    Scholl, S.5    Fehrenbacher, L.6    Wolter, J.M.7    Paton, V.8    Shak, S.9    Lieberman, G.10
  • 29
    • 3543091572 scopus 로고    scopus 로고
    • Phase II study of trastuzumab plus gemcitabine in chemotherapy-pretreated patients with metastatic breast cancer
    • O?Shaughnessy, J.A.; Vukelja, S.; Marsland, T.; Kimmel, G.; Ratnam, S.; Pippen, J.E. Phase II study of trastuzumab plus gemcitabine in chemotherapy-pretreated patients with metastatic breast cancer. Clin. Breast Cancer 2004, 5, 142-147.
    • (2004) Clin. Breast Cancer , vol.5 , pp. 142-147
    • Oshaughnessy, J.A.1    Vukelja, S.2    Marsland, T.3    Kimmel, G.4    Ratnam, S.5    Pippen, J.E.6
  • 30
    • 2942659576 scopus 로고    scopus 로고
    • Rational combinations of trastuzumab with chemotherapeutic drugs used in the treatment of breast cancer
    • Pegram, M.D.; Konecny, G.E.; O?Callaghan, C.; Beryt, M.; Pietras, R.; Slamon, D.J. Rational combinations of trastuzumab with chemotherapeutic drugs used in the treatment of breast cancer. J. Natl. Cancer Inst. 2004, 96, 739-749.
    • (2004) J. Natl. Cancer Inst. , vol.96 , pp. 739-749
    • Pegram, M.D.1    Konecny, G.E.2    Ocallaghan, C.3    Beryt, M.4    Pietras, R.5    Slamon, D.J.6
  • 31
    • 0035873815 scopus 로고    scopus 로고
    • Weekly trastuzumab and paclitaxel therapy for metastatic breast cancer with analysis of efficacy by HER2 immunophenotype and gene amplification
    • Seidman, A.D.; Fornier, M.N.; Esteva, F.J.; Tan, L.; Kaptain, S.; Bach, A.; Panageas, K.S.; Arroyo, C.; Valero, V.; Currie, V.; et al. Weekly trastuzumab and paclitaxel therapy for metastatic breast cancer with analysis of efficacy by HER2 immunophenotype and gene amplification. J. Clin. Oncol. 2001, 19, 2587-2595.
    • (2001) J. Clin. Oncol. , vol.19 , pp. 2587-2595
    • Seidman, A.D.1    Fornier, M.N.2    Esteva, F.J.3    Tan, L.4    Kaptain, S.5    Bach, A.6    Panageas, K.S.7    Arroyo, C.8    Valero, V.9    Currie, V.10
  • 32
    • 0034879275 scopus 로고    scopus 로고
    • Mechanism of action of anti-HER2 monoclonal antibodies
    • Baselga, J.; Albanell, J. Mechanism of action of anti-HER2 monoclonal antibodies. Ann. Oncol. 2001, 12, S35-S41.
    • (2001) Ann. Oncol. , vol.12 , pp. S35-S41
    • Baselga, J.1    Albanell, J.2
  • 33
    • 84907434747 scopus 로고    scopus 로고
    • Mechanisms of trastuzumab resistance and opportunities to overcome therapeutic resistance
    • Dokmanovic, M.; Wu, J.W. Mechanisms of trastuzumab resistance and opportunities to overcome therapeutic resistance. J. Mol. Biomark. Diagn. 2013, 4, doi:10.4172/2155-9929.1000e116.
    • (2013) J. Mol. Biomark. Diagn. , pp. 4
    • Dokmanovic, M.1    Wu, J.W.2
  • 34
    • 84991650697 scopus 로고    scopus 로고
    • Pertuzumab in neoadjuvant treatment of HER2-positive early breast cancer
    • Abraham, J.; Stenger, M. Pertuzumab in neoadjuvant treatment of HER2-positive early breast cancer. J. Community Support. Oncol. 2014, 12, 84-86.
    • (2014) J. Community Support. Oncol. , vol.12 , pp. 84-86
    • Abraham, J.1    Stenger, M.2
  • 35
    • 84906092045 scopus 로고    scopus 로고
    • A phase IIa dose-finding and safety study of first-line pertuzumab in combination with trastuzumab, capecitabine and cisplatin in patients with HER2-positive advanced gastric cancer
    • Kang, Y.K.; Rha, S.Y.; Tassone, P.; Barriuso, J.; Yu, R.; Szado, T.; Garg, A.; Bang, Y.J. A phase IIa dose-finding and safety study of first-line pertuzumab in combination with trastuzumab, capecitabine and cisplatin in patients with HER2-positive advanced gastric cancer. Br. J. Cancer 2014, 111, 660-666.
    • (2014) Br. J. Cancer , vol.111 , pp. 660-666
    • Kang, Y.K.1    Rha, S.Y.2    Tassone, P.3    Barriuso, J.4    Yu, R.5    Szado, T.6    Garg, A.7    Bang, Y.J.8
  • 36
    • 84903641743 scopus 로고    scopus 로고
    • The european medicines agency review of pertuzumab for the treatment of adult patients with HER2-positive metastatic or locally recurrent unresectable breast cancer: Summary of the scientific assessment of the committee for medicinal products for human use
    • Boix-Perales, H.; Borregaard, J.; Jensen, K.B.; Ersboll, J.; Galluzzo, S.; Giuliani, R.; Ciceroni, C.; Melchiorri, D.; Salmonson, T.; Bergh, J.; et al. The european medicines agency review of pertuzumab for the treatment of adult patients with HER2-positive metastatic or locally recurrent unresectable breast cancer: Summary of the scientific assessment of the committee for medicinal products for human use. Oncologist 2014, 19, 766-773.
    • (2014) Oncologist , vol.19 , pp. 766-773
    • Boix-Perales, H.1    Borregaard, J.2    Jensen, K.B.3    Ersboll, J.4    Galluzzo, S.5    Giuliani, R.6    Ciceroni, C.7    Melchiorri, D.8    Salmonson, T.9    Bergh, J.10
  • 37
    • 1642323740 scopus 로고    scopus 로고
    • Protein kinase inhibitors: Insights into drug design from structure
    • Noble, M.E.; Endicott, J.A.; Johnson, L.N. Protein kinase inhibitors: Insights into drug design from structure. Science 2004, 303, 1800-1805.
    • (2004) Science , vol.303 , pp. 1800-1805
    • Noble, M.E.1    Endicott, J.A.2    Johnson, L.N.3
  • 40
    • 33745002702 scopus 로고    scopus 로고
    • An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor
    • Zhang, X.; Gureasko, J.; Shen, K.; Cole, P.A.; Kuriyan, J. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 2006, 125, 1137-1149.
    • (2006) Cell , vol.125 , pp. 1137-1149
    • Zhang, X.1    Gureasko, J.2    Shen, K.3    Cole, P.A.4    Kuriyan, J.5
  • 41
    • 36749011864 scopus 로고    scopus 로고
    • Inhibition of the egf receptor by binding of mig6 to an activating kinase domain interface
    • Zhang, X.; Pickin, K.A.; Bose, R.; Jura, N.; Cole, P.A.; Kuriyan, J. Inhibition of the egf receptor by binding of mig6 to an activating kinase domain interface. Nature 2007, 450, 741-744.
    • (2007) Nature , vol.450 , pp. 741-744
    • Zhang, X.1    Pickin, K.A.2    Bose, R.3    Jura, N.4    Cole, P.A.5    Kuriyan, J.6
  • 42
    • 31544457665 scopus 로고    scopus 로고
    • Blockade of EGFR and erbB2 by the novel dual EGFR and erbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma geo cells to apoptosis
    • Zhou, Y.; Li, S.; Hu, Y.P.; Wang, J.; Hauser, J.; Conway, A.N.; Vinci, M.A.; Humphrey, L.; Zborowska, E.; Willson, J.K.; et al. Blockade of EGFR and erbB2 by the novel dual EGFR and erbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma geo cells to apoptosis. Cancer Res. 2006, 66, 404-411.
    • (2006) Cancer Res. , vol.66 , pp. 404-411
    • Zhou, Y.1    Li, S.2    Hu, Y.P.3    Wang, J.4    Hauser, J.5    Conway, A.N.6    Vinci, M.A.7    Humphrey, L.8    Zborowska, E.9    Willson, J.K.10
  • 43
    • 0035893560 scopus 로고    scopus 로고
    • Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo
    • Moulder, S.L.; Yakes, F.M.; Muthuswamy, S.K.; Bianco, R.; Simpson, J.F.; Arteaga, C.L. Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer Res. 2001, 61, 8887-8895.
    • (2001) Cancer Res. , vol.61 , pp. 8887-8895
    • Moulder, S.L.1    Yakes, F.M.2    Muthuswamy, S.K.3    Bianco, R.4    Simpson, J.F.5    Arteaga, C.L.6
  • 44
    • 84905920752 scopus 로고    scopus 로고
    • First results from the phase III ALTTO trial (BIG 2-06; NCCTG [alliance] N063D) comparing one year of anti-HER2 therapy with lapatinib alone (L), trastuzumab alone (T), their sequence (T?L), or their combination (T+L) in the adjuvant treatment of HER2-positive early breast cancer (EBC)
    • Abstract LBA4
    • Piccart-Gebhart, M.J.; Holmes, A.P.; Baselga, J.; Azambuja, E.D.; Dueck, A.C.; Viale, G.; Zujewski, J.A.; Goldhirsch, A.; Santillana, S.; Pritchard, K.I.; et al. First results from the phase III ALTTO trial (BIG 2-06; NCCTG [alliance] N063D) comparing one year of anti-HER2 therapy with lapatinib alone (L), trastuzumab alone (T), their sequence (T?L), or their combination (T+L) in the adjuvant treatment of HER2-positive early breast cancer (EBC). J. Clin. Oncol. 2014, 32 (Suppl.), 5s, Abstract LBA4.
    • (2014) J. Clin. Oncol. , vol.32 , pp. 5s
    • Piccart-Gebhart, M.J.1    Holmes, A.P.2    Baselga, J.3    Azambuja, E.D.4    Dueck, A.C.5    Viale, G.6    Zujewski, J.A.7    Goldhirsch, A.8    Santillana, S.9    Pritchard, K.I.10
  • 45
    • 84869206583 scopus 로고    scopus 로고
    • Potential of afatinib in the treatment of patients with HER2-positive breast cancer
    • Geuna, E.; Montemurro, F.; Aglietta, M.; Valabrega, G. Potential of afatinib in the treatment of patients with HER2-positive breast cancer. Breast Cancer (Dove Med. Press) 2012, 4, 131-137.
    • (2012) Breast Cancer (Dove Med. Press) , vol.4 , pp. 131-137
    • Geuna, E.1    Montemurro, F.2    Aglietta, M.3    Valabrega, G.4
  • 47
    • 84884618137 scopus 로고    scopus 로고
    • Lux-lung 4: A phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both
    • Katakami, N.; Atagi, S.; Goto, K.; Hida, T.; Horai, T.; Inoue, A.; Ichinose, Y.; Koboyashi, K.; Takeda, K.; Kiura, K.; et al. Lux-lung 4: A phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both. J. Clin. Oncol. 2013, 31, 3335-3341.
    • (2013) J. Clin. Oncol. , vol.31 , pp. 3335-3341
    • Katakami, N.1    Atagi, S.2    Goto, K.3    Hida, T.4    Horai, T.5    Inoue, A.6    Ichinose, Y.7    Koboyashi, K.8    Takeda, K.9    Kiura, K.10
  • 48
    • 38049038935 scopus 로고    scopus 로고
    • A phase i dose escalation study of bibw 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (egfr) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours
    • Eskens, F.A.; Mom, C.H.; Planting, A.S.; Gietema, J.A.; Amelsberg, A.; Huisman, H.; van Doorn, L.; Burger, H.; Stopfer, P.; Verweij, J.; et al. A phase I dose escalation study of bibw 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (egfr) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours. Br. J. Cancer 2008, 98, 80-85.
    • (2008) Br. J. Cancer , vol.98 , pp. 80-85
    • Eskens, F.A.1    Mom, C.H.2    Planting, A.S.3    Gietema, J.A.4    Amelsberg, A.5    Huisman, H.6    Van Doorn, L.7    Burger, H.8    Stopfer, P.9    Verweij, J.10
  • 49
    • 77957585027 scopus 로고    scopus 로고
    • Phase i trial of the irreversible egfr and HER2 kinase inhibitor bibw 2992 in patients with advanced solid tumors
    • Yap, T.A.; Vidal, L.; Adam, J.; Stephens, P.; Spicer, J.; Shaw, H.; Ang, J.; Temple, G.; Bell, S.; Shahidi, M.; et al. Phase I trial of the irreversible egfr and HER2 kinase inhibitor bibw 2992 in patients with advanced solid tumors. J. Clin. Oncol. 2010, 28, 3965-3972.
    • (2010) J. Clin. Oncol. , vol.28 , pp. 3965-3972
    • Yap, T.A.1    Vidal, L.2    Adam, J.3    Stephens, P.4    Spicer, J.5    Shaw, H.6    Ang, J.7    Temple, G.8    Bell, S.9    Shahidi, M.10
  • 51
    • 84903560408 scopus 로고    scopus 로고
    • AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: Preclinical activity in HER2 non-amplified inflammatory breast cancer models
    • Mu, Z.; Klinowska, T.; Dong, X.; Foster, E.; Womack, C.; Fernandez, S.V.; Cristofanilli, M. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: Preclinical activity in HER2 non-amplified inflammatory breast cancer models. J. Exp. Clin. Cancer Res. 2014, 33,47.
    • (2014) J. Exp. Clin. Cancer Res. , vol.33 , pp. 47
    • Mu, Z.1    Klinowska, T.2    Dong, X.3    Foster, E.4    Womack, C.5    Fernandez, S.V.6    Cristofanilli, M.7
  • 52
    • 84930697083 scopus 로고    scopus 로고
    • Inhibition of egfr, HER2 and HER3 signaling with azd8931 alone and in combination with paclitaxel: Phase i study in japanese patients with advanced solid malignancies and advanced breast cancer
    • . Kurata, T.; Tsurutani, J.; Fujisaka, Y.; Okamoto, W.; Hayashi, H.; Kawakami, H.; Shin, E.; Hayashi, N.; Nakagawa, K. Inhibition of egfr, HER2 and HER3 signaling with azd8931 alone and in combination with paclitaxel: Phase I study in japanese patients with advanced solid malignancies and advanced breast cancer. Investig. New Drugs 2014, doi:10.1007/s10637-014-0112-7.
    • (2014) Investig. New Drugs
    • Kurata, T.1    Tsurutani, J.2    Fujisaka, Y.3    Okamoto, W.4    Hayashi, H.5    Kawakami, H.6    Shin, E.7    Hayashi, N.8    Nakagawa, K.9
  • 53
    • 84899085552 scopus 로고    scopus 로고
    • Phase i dose-finding study of AZD8931, an inhibitor of EGFR (erbB1), HER2 (erbB2) and HER3 (erbB3) signaling, in patients with advanced solid tumors
    • Tjulandin, S.; Moiseyenko, V.; Semiglazov, V.; Manikhas, G.; Learoyd, M.; Saunders, A.; Stuart, M.; Keilholz, U. Phase I, dose-finding study of AZD8931, an inhibitor of EGFR (erbB1), HER2 (erbB2) and HER3 (erbB3) signaling, in patients with advanced solid tumors. Investig. New Drugs 2014, 32, 145-153.
    • (2014) Investig. New Drugs , vol.32 , pp. 145-153
    • Tjulandin, S.1    Moiseyenko, V.2    Semiglazov, V.3    Manikhas, G.4    Learoyd, M.5    Saunders, A.6    Stuart, M.7    Keilholz, U.8
  • 54
    • 79960577238 scopus 로고    scopus 로고
    • Ast1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo
    • Xie, H.; Lin, L.; Tong, L.; Jiang, Y.; Zheng, M.; Chen, Z.; Jiang, X.; Zhang, X.; Ren, X.; Qu, W.; et al. Ast1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One 2011, 6, e21487.
    • (2011) PLoS One , vol.6 , pp. e21487
    • Xie, H.1    Lin, L.2    Tong, L.3    Jiang, Y.4    Zheng, M.5    Chen, Z.6    Jiang, X.7    Zhang, X.8    Ren, X.9    Qu, W.10
  • 55
    • 84907444509 scopus 로고    scopus 로고
    • A phase i study of ast1306, a novel irreversible egfr and HER2 kinase inhibitor, in patients with advanced solid tumors
    • Zhang, J.; Cao, J.; Li, J.; Zhang, Y.; Chen, Z.; Peng, W.; Sun, S.; Zhao, N.; Wang, J.; Zhong, D.; et al. A phase I study of ast1306, a novel irreversible egfr and HER2 kinase inhibitor, in patients with advanced solid tumors. J. Hematol. Oncol. 2014, 7,22.
    • (2014) J. Hematol. Oncol. , vol.7 , pp. 22
    • Zhang, J.1    Cao, J.2    Li, J.3    Zhang, Y.4    Chen, Z.5    Peng, W.6    Sun, S.7    Zhao, N.8    Wang, J.9    Zhong, D.10
  • 56
    • 77957867584 scopus 로고    scopus 로고
    • Effect of additional inhibition of human epidermal growth factor receptor 2 with the bispecific tyrosine kinase inhibitor aee788 on the resistance to specific egfr inhibition in glioma cells
    • . Berezowska, S.; Diermeier-Daucher, S.; Brockhoff, G.; Busch, R.; Duyster, J.; Grosu, A.L.; Schlegel, J. Effect of additional inhibition of human epidermal growth factor receptor 2 with the bispecific tyrosine kinase inhibitor aee788 on the resistance to specific egfr inhibition in glioma cells. Int. J. Mol. Med. 2010, 26, 713-721.
    • (2010) Int. J. Mol. Med. , vol.26 , pp. 713-721
    • Berezowska, S.1    Diermeier-Daucher, S.2    Brockhoff, G.3    Busch, R.4    Duyster, J.5    Grosu, A.L.6    Schlegel, J.7
  • 57
    • 77950793617 scopus 로고    scopus 로고
    • EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ERpositive breast cancer cells but functions synergistically with endocrine therapy
    • Evans, A.H.; Pancholi, S.; Farmer, I.; Thornhill, A.; Evans, D.B.; Johnston, S.R.; Dowsett, M.; Martin, L.A. EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ERpositive breast cancer cells but functions synergistically with endocrine therapy. Br. J. Cancer 2010, 102, 1235-1243.
    • (2010) Br. J. Cancer , vol.102 , pp. 1235-1243
    • Evans, A.H.1    Pancholi, S.2    Farmer, I.3    Thornhill, A.4    Evans, D.B.5    Johnston, S.R.6    Dowsett, M.7    Martin, L.A.8
  • 58
    • 34249934555 scopus 로고    scopus 로고
    • The pan-erbB tyrosine kinase inhibitor CI-1033 inhibits human esophageal cancer cells in vitro and in vivo
    • Ako, E.; Yamashita, Y.; Ohira, M.; Yamazaki, M.; Hori, T.; Kubo, N.; Sawada, T.; Hirakawa, K. The pan-erbB tyrosine kinase inhibitor CI-1033 inhibits human esophageal cancer cells in vitro and in vivo. Oncol. Rep. 2007, 17, 887-893.
    • (2007) Oncol. Rep. , vol.17 , pp. 887-893
    • Ako, E.1    Yamashita, Y.2    Ohira, M.3    Yamazaki, M.4    Hori, T.5    Kubo, N.6    Sawada, T.7    Hirakawa, K.8
  • 59
    • 69049101061 scopus 로고    scopus 로고
    • A randomized, phase II, dose-finding study of the pan-erbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer
    • Rixe, O.; Franco, S.X.; Yardley, D.A.; Johnston, S.R.; Martin, M.; Arun, B.K.; Letrent, S.P.; Rugo, H.S. A randomized, phase II, dose-finding study of the pan-erbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer. Cancer Chemother. Pharmacol. 2009, 64, 1139-1148.
    • (2009) Cancer Chemother. Pharmacol. , vol.64 , pp. 1139-1148
    • Rixe, O.1    Franco, S.X.2    Yardley, D.A.3    Johnston, S.R.4    Martin, M.5    Arun, B.K.6    Letrent, S.P.7    Rugo, H.S.8
  • 61
    • 33947261180 scopus 로고    scopus 로고
    • First study of the safety, tolerability, and pharmacokinetics of CP-724,714 in patients with advanced malignant solid HER2-expressing tumors
    • Munster, P.N.; Britten, C.D.; Mita, M.; Gelmon, K.; Minton, S.E.; Moulder, S.; Slamon, D.J.; Guo, F.; Letrent, S.P.; Denis, L.; et al. First study of the safety, tolerability, and pharmacokinetics of CP-724,714 in patients with advanced malignant solid HER2-expressing tumors. Clin. Cancer Res. 2007, 13, 1238-1245.
    • (2007) Clin. Cancer Res. , vol.13 , pp. 1238-1245
    • Munster, P.N.1    Britten, C.D.2    Mita, M.3    Gelmon, K.4    Minton, S.E.5    Moulder, S.6    Slamon, D.J.7    Guo, F.8    Letrent, S.P.9    Denis, L.10
  • 62
    • 77949353758 scopus 로고    scopus 로고
    • Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer
    • Cai, X.; Zhai, H.X.; Wang, J.; Forrester, J.; Qu, H.; Yin, L.; Lai, C.J.; Bao, R.; Qian, C. Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. J. Med. Chem. 2010, 53, 2000-2009.
    • (2010) J. Med. Chem. , vol.53 , pp. 2000-2009
    • Cai, X.1    Zhai, H.X.2    Wang, J.3    Forrester, J.4    Qu, H.5    Yin, L.6    Lai, C.J.7    Bao, R.8    Qian, C.9
  • 63
    • 77951708371 scopus 로고    scopus 로고
    • CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity
    • Lai, C.J.; Bao, R.; Tao, X.; Wang, J.; Atoyan, R.; Qu, H.; Wang, D.G.; Yin, L.; Samson, M.; Forrester, J.; et al. CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity. Cancer Res. 2010, 70, 3647-3656.
    • (2010) Cancer Res. , vol.70 , pp. 3647-3656
    • Lai, C.J.1    Bao, R.2    Tao, X.3    Wang, J.4    Atoyan, R.5    Qu, H.6    Wang, D.G.7    Yin, L.8    Samson, M.9    Forrester, J.10
  • 64
    • 84907450176 scopus 로고    scopus 로고
    • A phase i study of CUDC-101, a multitarget inhibitor of HDACs, EGFR, and HER2, in combination with chemoradiation in patients with intermediate/high risk locally advanced squamous cell carcinoma of the head and neck
    • Jimeno, A.; Galloway, T.; Wirth, L.; Gilbert, J.; Saba, N.; Bauman, J.; Colevas, D.; Mehra, R.; Raben, D.; Lai, C.-J.; et al. A phase I study of CUDC-101, a multitarget inhibitor of HDACs, EGFR, and HER2, in combination with chemoradiation in patients with intermediate/high risk locally advanced squamous cell carcinoma of the head and neck. Mol. Cancer Ther. 2013, 12 (Suppl. 11), doi:10.1158/1535-7163.TARG-13-B268.
    • (2013) Mol. Cancer Ther. , vol.12
    • Jimeno, A.1    Galloway, T.2    Wirth, L.3    Gilbert, J.4    Saba, N.5    Bauman, J.6    Colevas, D.7    Mehra, R.8    Raben, D.9    Lai, C.-J.10
  • 65
    • 82555187407 scopus 로고    scopus 로고
    • Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold
    • Ishikawa, T.; Seto, M.; Banno, H.; Kawakita, Y.; Oorui, M.; Taniguchi, T.; Ohta, Y.; Tamura, T.; Nakayama, A.; Miki, H.; et al. Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. J. Med. Chem. 2011, 54, 8030-8050.
    • (2011) J. Med. Chem. , vol.54 , pp. 8030-8050
    • Ishikawa, T.1    Seto, M.2    Banno, H.3    Kawakita, Y.4    Oorui, M.5    Taniguchi, T.6    Ohta, Y.7    Tamura, T.8    Nakayama, A.9    Miki, H.10
  • 66
    • 84862810837 scopus 로고    scopus 로고
    • Verification of brain penetration of the unbound fraction of a novel HER2/EGFR dual kinase inhibitor (TAK-285) by microdialysis in rats
    • Erdo, F.; Gordon, J.; Wu, J.T.; Sziraki, I. Verification of brain penetration of the unbound fraction of a novel HER2/EGFR dual kinase inhibitor (TAK-285) by microdialysis in rats. Brain Res. Bull. 2012, 87, 413-419.
    • (2012) Brain Res. Bull. , vol.87 , pp. 413-419
    • Erdo, F.1    Gordon, J.2    Wu, J.T.3    Sziraki, I.4
  • 67
    • 84856822581 scopus 로고    scopus 로고
    • Phase i first-in-human study of tak-285, a novel investigational dual HER2/egfr inhibitor, in cancer patients
    • Doi, T.; Takiuchi, H.; Ohtsu, A.; Fuse, N.; Goto, M.; Yoshida, M.; Dote, N.; Kuze, Y.; Jinno, F.; Fujimoto, M.; et al. Phase I first-in-human study of tak-285, a novel investigational dual HER2/egfr inhibitor, in cancer patients. Br. J. Cancer 2012, 106, 666-672.
    • (2012) Br. J. Cancer , vol.106 , pp. 666-672
    • Doi, T.1    Takiuchi, H.2    Ohtsu, A.3    Fuse, N.4    Goto, M.5    Yoshida, M.6    Dote, N.7    Kuze, Y.8    Jinno, F.9    Fujimoto, M.10
  • 68
    • 79959743541 scopus 로고    scopus 로고
    • Ac480, formerly bms-599626, a pan HER inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo
    • Torres, M.A.; Raju, U.; Molkentine, D.; Riesterer, O.; Milas, L.; Ang, K.K. Ac480, formerly bms-599626, a pan HER inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Investig. New Drugs 2011, 29, 554-561.
    • (2011) Investig. New Drugs , vol.29 , pp. 554-561
    • Torres, M.A.1    Raju, U.2    Molkentine, D.3    Riesterer, O.4    Milas, L.5    Ang, K.K.6
  • 69
    • 84954374160 scopus 로고    scopus 로고
    • Synergistic apoptosis in head and neck squamous cell carcinoma cells by co-inhibition of insulin-like growth factor-1 receptor signaling and compensatory signaling pathways
    • Axelrod, M.J.; Mendez, R.E.; Khalil, A.; Leimgruber, S.S.; Sharlow, E.R.; Capaldo, B.; Conaway, M.; Gioeli, D.G.; Weber, M.J.; Jameson, M.J. Synergistic apoptosis in head and neck squamous cell carcinoma cells by co-inhibition of insulin-like growth factor-1 receptor signaling and compensatory signaling pathways. Head Neck 2014, doi:10.1002/hed.23822.
    • (2014) Head Neck
    • Axelrod, M.J.1    Mendez, R.E.2    Khalil, A.3    Leimgruber, S.S.4    Sharlow, E.R.5    Capaldo, B.6    Conaway, M.7    Gioeli, D.G.8    Weber, M.J.9    Jameson, M.J.10
  • 71
    • 84866133032 scopus 로고    scopus 로고
    • Dacomitinib (pf-00299804), an irreversible pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib
    • Kalous, O.; Conklin, D.; Desai, A.J.; O?Brien, N.A.; Ginther, C.; Anderson, L.; Cohen, D.J.; Britten, C.D.; Taylor, I.; Christensen, J.G.; et al. Dacomitinib (pf-00299804), an irreversible pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib. Mol. Cancer Ther. 2012, 11, 1978-1987.
    • (2012) Mol. Cancer Ther. , vol.11 , pp. 1978-1987
    • Kalous, O.1    Conklin, D.2    Desai, A.J.3    Obrien, N.A.4    Ginther, C.5    Anderson, L.6    Cohen, D.J.7    Britten, C.D.8    Taylor, I.9    Christensen, J.G.10
  • 72
    • 84898023610 scopus 로고    scopus 로고
    • A phase 2 trial of dacomitinib (pf-00299804), an oral, irreversible pan-HER (human epidermal growth factor receptor) inhibitor, in patients with advanced non-small cell lung cancer after failure of prior chemotherapy and erlotinib
    • Reckamp, K.L.; Giaccone, G.; Camidge, D.R.; Gadgeel, S.M.; Khuri, F.R.; Engelman, J.A.; Koczywas, M.; Rajan, A.; Campbell, A.K.; Gernhardt, D.; et al. A phase 2 trial of dacomitinib (pf-00299804), an oral, irreversible pan-HER (human epidermal growth factor receptor) inhibitor, in patients with advanced non-small cell lung cancer after failure of prior chemotherapy and erlotinib. Cancer 2014, 120, 1145-1154.
    • (2014) Cancer , vol.120 , pp. 1145-1154
    • Reckamp, K.L.1    Giaccone, G.2    Camidge, D.R.3    Gadgeel, S.M.4    Khuri, F.R.5    Engelman, J.A.6    Koczywas, M.7    Rajan, A.8    Campbell, A.K.9    Gernhardt, D.10
  • 74
    • 0035553174 scopus 로고    scopus 로고
    • The effects of the novel, reversible epidermal growth factor receptor/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.; Wood, E.R.; Alligood, K.J.; Rhodes, N.; Keith, B.R.; Murray, D.M.; Knight, W.B.; Mullin, R.J.; et al. The effects of the novel, reversible epidermal growth factor receptor/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. 2001, 1, 85-94.
    • (2001) Mol. Cancer Ther. , vol.1 , pp. 85-94
    • Rusnak, D.W.1    Lackey, K.2    Affleck, K.3    Wood, E.R.4    Alligood, K.J.5    Rhodes, N.6    Keith, B.R.7    Murray, D.M.8    Knight, W.B.9    Mullin, R.J.10
  • 75
    • 84864246491 scopus 로고    scopus 로고
    • Irreversible protein kinase inhibitors: Balancing the benefits and risks
    • Barf, T.; Kaptein, A. Irreversible protein kinase inhibitors: Balancing the benefits and risks. J. Med. Chem. 2012, 55, 6243-6262.
    • (2012) J. Med. Chem. , vol.55 , pp. 6243-6262
    • Barf, T.1    Kaptein, A.2
  • 76
    • 3142774878 scopus 로고    scopus 로고
    • AEE788: A dual family epidermal growth factor receptor/erbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity
    • Traxler, P.; Allegrini, P.R.; Brandt, R.; Brueggen, J.; Cozens, R.; Fabbro, D.; Grosios, K.; Lane, H.A.; McSheehy, P.; Mestan, J.; et al. AEE788: A dual family epidermal growth factor receptor/erbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2004, 64, 4931-4941.
    • (2004) Cancer Res. , vol.64 , pp. 4931-4941
    • Traxler, P.1    Allegrini, P.R.2    Brandt, R.3    Brueggen, J.4    Cozens, R.5    Fabbro, D.6    Grosios, K.7    Lane, H.A.8    Mc Sheehy, P.9    Mestan, J.10
  • 77
    • 0035253847 scopus 로고    scopus 로고
    • Tyrosine kinase inhibitors6-substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor
    • Smaill, J.B.; Showalter, H.D.; Zhou, H.; Bridges, A.J.; McNamara, D.J.; Fry, D.W.; Nelson, J.M.; Sherwood, V.; Vincent, P.W.; Roberts, B.J.; et al. Tyrosine kinase inhibitors. 6-substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor. J. Med. Chem. 2001, 44, 429-440.
    • (2001) J. Med. Chem. , vol.44 , pp. 429-440
    • Smaill, J.B.1    Showalter, H.D.2    Zhou, H.3    Bridges, A.J.4    Mc Namara, D.J.5    Fry, D.W.6    Nelson, J.M.7    Sherwood, V.8    Vincent, P.W.9    Roberts, B.J.10
  • 78
    • 77649204688 scopus 로고    scopus 로고
    • Selectively nonselective kinase inhibition: Striking the right balance
    • Morphy, R. Selectively nonselective kinase inhibition: Striking the right balance. J. Med. Chem. 2010, 53, 1413-1437.
    • (2010) J. Med. Chem. , vol.53 , pp. 1413-1437
    • Morphy, R.1
  • 80
    • 71049165969 scopus 로고    scopus 로고
    • Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1h-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][ 1,2,4]triazin-6-yl]carbamic acid, (3s)-3-morpholinylmethyl ester (bms-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases
    • Gavai, A.V.; Fink, B.E.; Fairfax, D.J.; Martin, G.S.; Rossiter, L.M.; Holst, C.L.; Kim, S.H.; Leavitt, K.J.; Mastalerz, H.; Han, W.C.; et al. Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1h-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3s)-3-morpholinylmethyl ester (bms-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. J. Med. Chem. 2009, 52, 6527-6530.
    • (2009) J. Med. Chem. , vol.52 , pp. 6527-6530
    • Gavai, A.V.1    Fink, B.E.2    Fairfax, D.J.3    Martin, G.S.4    Rossiter, L.M.5    Holst, C.L.6    Kim, S.H.7    Leavitt, K.J.8    Mastalerz, H.9    Han, W.C.10
  • 82
    • 84896328689 scopus 로고    scopus 로고
    • Discovery of new HER2/egfr dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agents
    • Sadek, M.M.; Serrya, R.A.; Kafafy, A.H.; Ahmed, M.; Wang, F.; Abouzid, K.A. Discovery of new HER2/egfr dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agents. J. Enzym. Inhib. Med. Chem. 2014, 29, 215-222.
    • (2014) J. Enzym. Inhib. Med. Chem. , vol.29 , pp. 215-222
    • Sadek, M.M.1    Serrya, R.A.2    Kafafy, A.H.3    Ahmed, M.4    Wang, F.5    Abouzid, K.A.6
  • 83
    • 84881020003 scopus 로고    scopus 로고
    • Optimization of substituted 6-salicyl-4-anilinoquinazoline derivatives as dual egfr/HER2 tyrosine kinase inhibitors
    • Li, D.D.; Qin, Y.J.; Sun, J.; Li, J.R.; Fang, F.; Du, Q.R.; Qian, Y.; Gong, H.B.; Zhu, H.L. Optimization of substituted 6-salicyl-4-anilinoquinazoline derivatives as dual egfr/HER2 tyrosine kinase inhibitors. PLoS One 2013, 8, e69427.
    • (2013) PLoS One , vol.8 , pp. e69427
    • Li, D.D.1    Qin, Y.J.2    Sun, J.3    Li, J.R.4    Fang, F.5    Du, Q.R.6    Qian, Y.7    Gong, H.B.8    Zhu, H.L.9
  • 84
    • 84866910818 scopus 로고    scopus 로고
    • Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/egfr dual inhibitors: Improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy
    • Kawakita, Y.; Miwa, K.; Seto, M.; Banno, H.; Ohta, Y.; Tamura, T.; Yusa, T.; Miki, H.; Kamiguchi, H.; Ikeda, Y.; et al. Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/egfr dual inhibitors: Improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy. Bioorg. Med. Chem. 2012, 20, 6171-6180.
    • (2012) Bioorg. Med. Chem. , vol.20 , pp. 6171-6180
    • Kawakita, Y.1    Miwa, K.2    Seto, M.3    Banno, H.4    Ohta, Y.5    Tamura, T.6    Yusa, T.7    Miki, H.8    Kamiguchi, H.9    Ikeda, Y.10
  • 85
    • 84860305840 scopus 로고    scopus 로고
    • Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: Exploration of novel back-pocket binders
    • Kawakita, Y.; Banno, H.; Ohashi, T.; Tamura, T.; Yusa, T.; Nakayama, A.; Miki, H.; Iwata, H.; Kamiguchi, H.; Tanaka, T.; et al. Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: Exploration of novel back-pocket binders. J. Med. Chem. 2012, 55, 3975-3991.
    • (2012) J. Med. Chem. , vol.55 , pp. 3975-3991
    • Kawakita, Y.1    Banno, H.2    Ohashi, T.3    Tamura, T.4    Yusa, T.5    Nakayama, A.6    Miki, H.7    Iwata, H.8    Kamiguchi, H.9    Tanaka, T.10
  • 86
    • 78651260008 scopus 로고    scopus 로고
    • Discovery of selective irreversible inhibitors for EGFR-T790M
    • Zhou, W.; Ercan, D.; Janne, P.A.; Gray, N.S. Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorg. Med. Chem. Lett. 2011, 21, 638-643.
    • (2011) Bioorg. Med. Chem. Lett. , vol.21 , pp. 638-643
    • Zhou, W.1    Ercan, D.2    Janne, P.A.3    Gray, N.S.4
  • 87
    • 84865175881 scopus 로고    scopus 로고
    • Emodin inhibits invasion and migration of prostate and lung cancer cells by downregulating the expression of chemokine receptor cxcr4
    • Ok, S.; Kim, S.M.; Kim, C.; Nam, D.; Shim, B.S.; Kim, S.H.; Ahn, K.S.; Choi, S.H. Emodin inhibits invasion and migration of prostate and lung cancer cells by downregulating the expression of chemokine receptor cxcr4. Immunopharmacol. Immunotoxicol. 2012, 34, 768-778.
    • (2012) Immunopharmacol. Immunotoxicol. , vol.34 , pp. 768-778
    • Ok, S.1    Kim, S.M.2    Kim, C.3    Nam, D.4    Shim, B.S.5    Kim, S.H.6    Ahn, K.S.7    Choi, S.H.8


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.