-
1
-
-
0024337144
-
Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer
-
Slamon, D.J.; Godolphin, W.; Jones, L.A.; Holt, J.A.; Wong, S.G.; Keith, D.E.; Levin, W.J.; Stuart, S.G.; Udove, J.; Ullrich, A.; et al. Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer. Science 1989, 244, 707-712.
-
(1989)
Science
, vol.244
, pp. 707-712
-
-
Slamon, D.J.1
Godolphin, W.2
Jones, L.A.3
Holt, J.A.4
Wong, S.G.5
Keith, D.E.6
Levin, W.J.7
Stuart, S.G.8
Udove, J.9
Ullrich, A.10
-
2
-
-
0027946003
-
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
-
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
-
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
-
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
-
6
-
-
84890281328
-
Metastasis dormancy in estrogen receptor-positive breast cancer
-
Zhang, X.H.; Giuliano, M.; Trivedi, M.V.; Schiff, R.; Osborne, C.K. Metastasis dormancy in estrogen receptor-positive breast cancer. Clin. Cancer Res. 2013, 19, 6389-6397.
-
(2013)
Clin. Cancer Res.
, vol.19
, pp. 6389-6397
-
-
Zhang, X.H.1
Giuliano, M.2
Trivedi, M.V.3
Schiff, R.4
Osborne, C.K.5
-
8
-
-
18344390418
-
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
-
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
-
10
-
-
0032526729
-
Differential endocytic routing of homo-and hetero-dimeric erbb tyrosine kinases confers signaling superiority to receptor heterodimers
-
Lenferink, A.E.; Pinkas-Kramarski, R.; van de Poll, M.L.; van Vugt, M.J.; Klapper, L.N.; Tzahar, E.; Waterman, H.; Sela, M.; van Zoelen, E.J.; Yarden, Y. Differential endocytic routing of homo-and hetero-dimeric erbb tyrosine kinases confers signaling superiority to receptor heterodimers. EMBO J. 1998, 17, 3385-3397.
-
(1998)
EMBO J.
, vol.17
, pp. 3385-3397
-
-
Lenferink, A.E.1
Pinkas-Kramarski, R.2
Van De Poll, M.L.3
Van Vugt, M.J.4
Klapper, L.N.5
Tzahar, E.6
Waterman, H.7
Sela, M.8
Van Zoelen, E.J.9
Yarden, Y.10
-
11
-
-
84906685211
-
P95 HER2 fragments and breast cancer outcome
-
Tural, D.; Akar, E.; Mutlu, H.; Kilickap, S. P95 HER2 fragments and breast cancer outcome. Expert Rev. Anticancer Ther. 2014, 1-8.
-
(2014)
Expert Rev. Anticancer Ther.
, pp. 1-8
-
-
Tural, D.1
Akar, E.2
Mutlu, H.3
Kilickap, S.4
-
12
-
-
79952212888
-
P95HER2 and breast cancer
-
Arribas, J.; Baselga, J.; Pedersen, K.; Parra-Palau, J.L. P95HER2 and breast cancer. Cancer Res. 2011, 71, 1515-1519.
-
(2011)
Cancer Res.
, vol.71
, pp. 1515-1519
-
-
Arribas, J.1
Baselga, J.2
Pedersen, K.3
Parra-Palau, J.L.4
-
13
-
-
84907443858
-
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
-
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
-
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
-
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
-
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
-
18
-
-
84877998630
-
Recent advances in drug design of epidermal growth factor receptor inhibitors
-
Warnault, P.; Yasri, A.; Coisy-Quivy, M.; Cheve, G.; Bories, C.; Fauvel, B.; Benhida, R. Recent advances in drug design of epidermal growth factor receptor inhibitors. Curr. Med. Chem. 2013, 20, 2043-2067.
-
(2013)
Curr. Med. Chem.
, vol.20
, pp. 2043-2067
-
-
Warnault, P.1
Yasri, A.2
Coisy-Quivy, M.3
Cheve, G.4
Bories, C.5
Fauvel, B.6
Benhida, R.7
-
19
-
-
84876705235
-
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
-
20
-
-
84655162706
-
Treatment of HER2-positive breast cancer: Current status and future perspectives
-
Arteaga, C.L.; Sliwkowski, M.X.; Osborne, C.K.; Perez, E.A.; Puglisi, F.; Gianni, L. Treatment of HER2-positive breast cancer: Current status and future perspectives. Nat. Rev. Clin. Oncol. 2011, 9, 16-32.
-
(2011)
Nat. Rev. Clin. Oncol.
, vol.9
, pp. 16-32
-
-
Arteaga, C.L.1
Sliwkowski, M.X.2
Osborne, C.K.3
Perez, E.A.4
Puglisi, F.5
Gianni, L.6
-
21
-
-
80054866591
-
Beyond trastuzumab: New treatment options for HER2-positive breast cancer
-
Saini, K.S.; Azim, H.A., Jr.; Metzger-Filho, O.; Loi, S.; Sotiriou, C.; de Azambuja, E.; Piccart, M. Beyond trastuzumab: New treatment options for HER2-positive breast cancer. Breast 2011, 20 (Suppl. 3), S20-S27.
-
(2011)
Breast
, vol.20
, pp. S20-S27
-
-
Saini, K.S.1
Azim, H.A.2
Metzger-Filho, O.3
Loi, S.4
Sotiriou, C.5
De Azambuja, E.6
Piccart, M.7
-
22
-
-
84871713793
-
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
-
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
-
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
-
25
-
-
26844503270
-
Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer
-
Piccart-Gebhart, M.J.; Procter, M.; Leyland-Jones, B.; Goldhirsch, A.; Untch, M.; Smith, I.; Gianni, L.; Baselga, J.; Bell, R.; Jackisch, C.; et al. Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer. N. Engl. J. Med. 2005, 353, 1659-1672.
-
(2005)
N. Engl. J. Med.
, vol.353
, pp. 1659-1672
-
-
Piccart-Gebhart, M.J.1
Procter, M.2
Leyland-Jones, B.3
Goldhirsch, A.4
Untch, M.5
Smith, I.6
Gianni, L.7
Baselga, J.8
Bell, R.9
Jackisch, C.10
-
26
-
-
26844536978
-
Trastuzumab plus adjuvant chemotherapy for operable HER2-positive breast cancer
-
Romond, E.H.; Perez, E.A.; Bryant, J.; Suman, V.J.; Geyer, C.E., Jr.; Davidson, N.E.; Tan-Chiu, E.; Martino, S.; Paik, S.; Kaufman, P.A.; et al. Trastuzumab plus adjuvant chemotherapy for operable HER2-positive breast cancer. N. Engl. J. Med. 2005, 353, 1673-1684.
-
(2005)
N. Engl. J. Med.
, vol.353
, pp. 1673-1684
-
-
Romond, E.H.1
Perez, E.A.2
Bryant, J.3
Suman, V.J.4
Geyer, C.E.5
Davidson, N.E.6
Tan-Chiu, E.7
Martino, S.8
Paik, S.9
Kaufman, P.A.10
-
27
-
-
0035869407
-
Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2
-
Slamon, D.J.; Leyland-Jones, B.; Shak, S.; Fuchs, H.; Paton, V.; Bajamonde, A.; Fleming, T.; Eiermann, W.; Wolter, J.; Pegram, M.; et al. Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. N. Engl. J. Med. 2001, 344, 783-792.
-
(2001)
N. Engl. J. Med.
, vol.344
, pp. 783-792
-
-
Slamon, D.J.1
Leyland-Jones, B.2
Shak, S.3
Fuchs, H.4
Paton, V.5
Bajamonde, A.6
Fleming, T.7
Eiermann, W.8
Wolter, J.9
Pegram, M.10
-
28
-
-
0036534121
-
Phase II study of weekly docetaxel and trastuzumab for patients with HER-2-overexpressing metastatic breast cancer
-
Esteva, F.J.; Valero, V.; Booser, D.; Guerra, L.T.; Murray, J.L.; Pusztai, L.; Cristofanilli, M.; Arun, B.; Esmaeli, B.; Fritsche, H.A.; et al. Phase II study of weekly docetaxel and trastuzumab for patients with HER-2-overexpressing metastatic breast cancer. J. Clin. Oncol. 2002, 20, 1800-1808.
-
(2002)
J. Clin. Oncol.
, vol.20
, pp. 1800-1808
-
-
Esteva, F.J.1
Valero, V.2
Booser, D.3
Guerra, L.T.4
Murray, J.L.5
Pusztai, L.6
Cristofanilli, M.7
Arun, B.8
Esmaeli, B.9
Fritsche, H.A.10
-
29
-
-
3543091572
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
38
-
-
79956310563
-
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein
-
Aertgeerts, K.; Skene, R.; Yano, J.; Sang, B.C.; Zou, H.; Snell, G.; Jennings, A.; Iwamoto, K.; Habuka, N.; Hirokawa, A.; et al. Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. J. Biol. Chem. 2011, 286, 18756-18765.
-
(2011)
J. Biol. Chem.
, vol.286
, pp. 18756-18765
-
-
Aertgeerts, K.1
Skene, R.2
Yano, J.3
Sang, B.C.4
Zou, H.5
Snell, G.6
Jennings, A.7
Iwamoto, K.8
Habuka, N.9
Hirokawa, A.10
-
39
-
-
40049099848
-
Mechanism of activation and inhibition of the HER4/erbb4 kinase
-
Qiu, C.; Tarrant, M.K.; Choi, S.H.; Sathyamurthy, A.; Bose, R.; Banjade, S.; Pal, A.; Bornmann, W.G.; Lemmon, M.A.; Cole, P.A.; et al. Mechanism of activation and inhibition of the HER4/erbb4 kinase. Structure 2008, 16, 460-467.
-
(2008)
Structure
, vol.16
, pp. 460-467
-
-
Qiu, C.1
Tarrant, M.K.2
Choi, S.H.3
Sathyamurthy, A.4
Bose, R.5
Banjade, S.6
Pal, A.7
Bornmann, W.G.8
Lemmon, M.A.9
Cole, P.A.10
-
40
-
-
33745002702
-
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
-
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
-
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
-
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
-
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
-
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
-
46
-
-
49149118719
-
Bibw2992, an irreversible egfr/HER2 inhibitor highly effective in preclinical lung cancer models
-
Li, D.; Ambrogio, L.; Shimamura, T.; Kubo, S.; Takahashi, M.; Chirieac, L.R.; Padera, R.F.; Shapiro, G.I.; Baum, A.; Himmelsbach, F.; et al. Bibw2992, an irreversible egfr/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 2008, 27, 4702-4711.
-
(2008)
Oncogene
, vol.27
, pp. 4702-4711
-
-
Li, D.1
Ambrogio, L.2
Shimamura, T.3
Kubo, S.4
Takahashi, M.5
Chirieac, L.R.6
Padera, R.F.7
Shapiro, G.I.8
Baum, A.9
Himmelsbach, F.10
-
47
-
-
84884618137
-
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
-
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
-
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
-
50
-
-
84881459273
-
Discovery of azd8931, an equipotent, reversible inhibitor of signaling by egfr, HER2, and HER3 receptors
-
Barlaam, B.; Anderton, J.; Ballard, P.; Bradbury, R.H.; Hennequin, L.F.; Hickinson, D.M.; Kettle, J.G.; Kirk, G.; Klinowska, T.; Lambert-van der Brempt, C.; et al. Discovery of azd8931, an equipotent, reversible inhibitor of signaling by egfr, HER2, and HER3 receptors. ACS Med. Chem. Lett. 2013, 4, 742-746.
-
(2013)
ACS Med. Chem. Lett.
, vol.4
, pp. 742-746
-
-
Barlaam, B.1
Anderton, J.2
Ballard, P.3
Bradbury, R.H.4
Hennequin, L.F.5
Hickinson, D.M.6
Kettle, J.G.7
Kirk, G.8
Klinowska, T.9
Lambert-Van Der Brempt, C.10
-
51
-
-
84903560408
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
60
-
-
35448955219
-
Discovery and pharmacologic characterization of CP-724, 714, a selective ErbB2 tyrosine kinase inhibitor
-
Jani, J.P.; Finn, R.S.; Campbell, M.; Coleman, K.G.; Connell, R.D.; Currier, N.; Emerson, E.O.; Floyd, E.; Harriman, S.; Kath, J.C.; et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res. 2007, 67, 9887-9893.
-
(2007)
Cancer Res.
, vol.67
, pp. 9887-9893
-
-
Jani, J.P.1
Finn, R.S.2
Campbell, M.3
Coleman, K.G.4
Connell, R.D.5
Currier, N.6
Emerson, E.O.7
Floyd, E.8
Harriman, S.9
Kath, J.C.10
-
61
-
-
33947261180
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
70
-
-
79952267022
-
Phase i dose-escalation study of the pan-HER inhibitor, pf299804, in patients with advanced malignant solid tumors
-
Janne, P.A.; Boss, D.S.; Camidge, D.R.; Britten, C.D.; Engelman, J.A.; Garon, E.B.; Guo, F.; Wong, S.; Liang, J.; Letrent, S.; et al. Phase I dose-escalation study of the pan-HER inhibitor, pf299804, in patients with advanced malignant solid tumors. Clin. Cancer Res. 2011, 17, 1131-1139.
-
(2011)
Clin. Cancer Res.
, vol.17
, pp. 1131-1139
-
-
Janne, P.A.1
Boss, D.S.2
Camidge, D.R.3
Britten, C.D.4
Engelman, J.A.5
Garon, E.B.6
Guo, F.7
Wong, S.8
Liang, J.9
Letrent, S.10
-
71
-
-
84866133032
-
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
-
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
-
73
-
-
33744824672
-
Phase i study of ekb-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors
-
Erlichman, C.; Hidalgo, M.; Boni, J.P.; Martins, P.; Quinn, S.E.; Zacharchuk, C.; Amorusi, P.; Adjei, A.A.; Rowinsky, E.K. Phase I study of ekb-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors. J. Clin. Oncol. 2006, 24, 2252-2260.
-
(2006)
J. Clin. Oncol.
, vol.24
, pp. 2252-2260
-
-
Erlichman, C.1
Hidalgo, M.2
Boni, J.P.3
Martins, P.4
Quinn, S.E.5
Zacharchuk, C.6
Amorusi, P.7
Adjei, A.A.8
Rowinsky, E.K.9
-
74
-
-
0035553174
-
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
-
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
-
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
-
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
-
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
-
79
-
-
84875754212
-
Design and synthesis of novel pyrimido[ 4,5-b]azepine derivatives as HER2/EGFR dual inhibitors
-
Kawakita, Y.; Seto, M.; Ohashi, T.; Tamura, T.; Yusa, T.; Miki, H.; Iwata, H.; Kamiguchi, H.; Tanaka, T.; Sogabe, S.; et al. Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. Bioorg. Med. Chem. 2013, 21, 2250-2261.
-
(2013)
Bioorg. Med. Chem.
, vol.21
, pp. 2250-2261
-
-
Kawakita, Y.1
Seto, M.2
Ohashi, T.3
Tamura, T.4
Yusa, T.5
Miki, H.6
Iwata, H.7
Kamiguchi, H.8
Tanaka, T.9
Sogabe, S.10
-
80
-
-
71049165969
-
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
-
81
-
-
78651250889
-
Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of egfr and HER2 protein tyrosine kinases
-
Fink, B.E.; Norris, D.; Mastalerz, H.; Chen, P.; Goyal, B.; Zhao, Y.; Kim, S.H.; Vite, G.D.; Lee, F.Y.; Zhang, H.; et al. Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of egfr and HER2 protein tyrosine kinases. Bioorg. Med. Chem. Lett. 2011, 21, 781-785.
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 781-785
-
-
Fink, B.E.1
Norris, D.2
Mastalerz, H.3
Chen, P.4
Goyal, B.5
Zhao, Y.6
Kim, S.H.7
Vite, G.D.8
Lee, F.Y.9
Zhang, H.10
-
82
-
-
84896328689
-
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
-
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
-
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
-
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
-
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
-
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
-
88
-
-
84891495297
-
Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer
-
Sridhar, J.; Sfondouris, M.E.; Bratton, M.R.; Nguyen, T.L.; Townley, I.; Klein Stevens, C.L.; Jones, F.E. Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer. Bioorg. Med. Chem. Lett. 2013, 24, 126-131.
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.24
, pp. 126-131
-
-
Sridhar, J.1
Sfondouris, M.E.2
Bratton, M.R.3
Nguyen, T.L.4
Townley, I.5
Klein Stevens, C.L.6
Jones, F.E.7
|