-
1
-
-
0242721567
-
CI-1033, an irreversible pan-erbB receptor inhibitor and its potential application for the treatment of breast cancer
-
Allen L.F., Eiseman I.A., Fry D.W., Lenehan P.F. CI-1033, an irreversible pan-erbB receptor inhibitor and its potential application for the treatment of breast cancer. Semin. Oncol. 2003, 30(Suppl. 16):65-78.
-
(2003)
Semin. Oncol.
, vol.30
, pp. 65-78
-
-
Allen, L.F.1
Eiseman, I.A.2
Fry, D.W.3
Lenehan, P.F.4
-
2
-
-
84884308133
-
Mechanism for activation of mutated epidermal growth factor receptors in lung cancer
-
Brewer R., Yun C.H., Lai D., Lemmon M.A., Eck M.J., Pao W. Mechanism for activation of mutated epidermal growth factor receptors in lung cancer. Proc. Natl. Acad. Sci. U.S.A. 2013, 110:E3595-E3604.
-
(2013)
Proc. Natl. Acad. Sci. U.S.A.
, vol.110
, pp. E3595-E3604
-
-
Brewer, R.1
Yun, C.H.2
Lai, D.3
Lemmon, M.A.4
Eck, M.J.5
Pao, W.6
-
3
-
-
84872693463
-
Dacomitinib, a new therapy for the treatment of non-small cell lung cancer
-
Brzezniak C., Carter C.A., Giaccone G. Dacomitinib, a new therapy for the treatment of non-small cell lung cancer. Expert Opin. Pharmacother. 2013, 14:247-253.
-
(2013)
Expert Opin. Pharmacother.
, vol.14
, pp. 247-253
-
-
Brzezniak, C.1
Carter, C.A.2
Giaccone, G.3
-
4
-
-
8444221534
-
Administration of CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, is feasible on a 7-day on, 7-day off schedule: a phase I pharmacokinetic and food effect study
-
Calvo E., Tolcher A.W., Hammond L.A., Patnaik A., de Bono J.S., Eiseman I.A., Olson S.C., Lenehan P.F., McCreery H., LoRusso P., Rowinsky E.K. Administration of CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, is feasible on a 7-day on, 7-day off schedule: a phase I pharmacokinetic and food effect study. Clin. Cancer Res. 2004, 10:7112-7120.
-
(2004)
Clin. Cancer Res.
, vol.10
, pp. 7112-7120
-
-
Calvo, E.1
Tolcher, A.W.2
Hammond, L.A.3
Patnaik, A.4
de Bono, J.S.5
Eiseman, I.A.6
Olson, S.C.7
Lenehan, P.F.8
McCreery, H.9
LoRusso, P.10
Rowinsky, E.K.11
-
5
-
-
84905029258
-
Comprehensive molecular profiling of lung adenocarcinoma
-
Cancer Genome Atlas Research Network Comprehensive molecular profiling of lung adenocarcinoma. Nature 2014, 511:543-550.
-
(2014)
Nature
, vol.511
, pp. 543-550
-
-
-
6
-
-
33748066632
-
Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib
-
Carey K.D., Garton A.J., Romero M.S., Kahler J., Thomson S., Ross S., et al. Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib. Cancer Res. 2006, 66:8163-8171.
-
(2006)
Cancer Res.
, vol.66
, pp. 8163-8171
-
-
Carey, K.D.1
Garton, A.J.2
Romero, M.S.3
Kahler, J.4
Thomson, S.5
Ross, S.6
-
7
-
-
74549178560
-
MolProbity: all-atom structure validation for macromolecular crystallography
-
Chen V.B., Arendall W.B., Headd J.J., Keedy D.A., Immormino R.M., Kapral G.J., Murray L.W., Richardson J.S., Richardson D.C. MolProbity: all-atom structure validation for macromolecular crystallography. Acta Crystallogr. 2010, D66:12-21.
-
(2010)
Acta Crystallogr.
, vol.D66
, pp. 12-21
-
-
Chen, V.B.1
Arendall, W.B.2
Headd, J.J.3
Keedy, D.A.4
Immormino, R.M.5
Kapral, G.J.6
Murray, L.W.7
Richardson, J.S.8
Richardson, D.C.9
-
8
-
-
84904898065
-
AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer
-
Cross D.A., Ashton S.E., Ghiorghiu S., Eberlein C., Nebhan C.A., Spitzler P.J., et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discovery 2014, 4:1046-1061.
-
(2014)
Cancer Discovery
, vol.4
, pp. 1046-1061
-
-
Cross, D.A.1
Ashton, S.E.2
Ghiorghiu, S.3
Eberlein, C.4
Nebhan, C.A.5
Spitzler, P.J.6
-
9
-
-
53649083930
-
Small molecule recognition of c-Src via the Imatinib-binding conformation
-
Dar A.C., Lopez M.S., Shokat K.M. Small molecule recognition of c-Src via the Imatinib-binding conformation. Chem. Biol. 2008, 15:1015-1022.
-
(2008)
Chem. Biol.
, vol.15
, pp. 1015-1022
-
-
Dar, A.C.1
Lopez, M.S.2
Shokat, K.M.3
-
10
-
-
15944404601
-
The development of imatinib as a therapeutic agent for chronic myeloid leukemia
-
Deininger M., Buchdunger E., Druker B.J. The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood 2005, 105:2640-2653.
-
(2005)
Blood
, vol.105
, pp. 2640-2653
-
-
Deininger, M.1
Buchdunger, E.2
Druker, B.J.3
-
11
-
-
54549094903
-
Somatic mutations affect key pathways in lung adenocarcinoma
-
Ding L., Getz G., Wheeler D.A., Mardis E.R., McLellan M.D., Cibulskis K., et al. Somatic mutations affect key pathways in lung adenocarcinoma. Nature 2008, 455:1069-1075.
-
(2008)
Nature
, vol.455
, pp. 1069-1075
-
-
Ding, L.1
Getz, G.2
Wheeler, D.A.3
Mardis, E.R.4
McLellan, M.D.5
Cibulskis, K.6
-
12
-
-
77949535720
-
Features and development of coot
-
Emsley P., Lohkamp B., Scott W.G., Cowtan K. Features and development of coot. Acta Crystallogr. 2010, D66:486-501.
-
(2010)
Acta Crystallogr.
, vol.D66
, pp. 486-501
-
-
Emsley, P.1
Lohkamp, B.2
Scott, W.G.3
Cowtan, K.4
-
13
-
-
37549061078
-
PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib
-
Engelman J.A., Zejnullahu K., Gale C.-M., Lifshits E., Gonzales A.J., Shimamura T., Zhao F., Vincent P.W., Naumov G.N., Bradner J.E., Althaus I.W., Gandhi L., Shapiro G.I., Nelson J.M., Heymach J.V., Meyerson M., Wong K.-K., Jänne P.A. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007, 67:11924-11932.
-
(2007)
Cancer Res.
, vol.67
, pp. 11924-11932
-
-
Engelman, J.A.1
Zejnullahu, K.2
Gale, C.-M.3
Lifshits, E.4
Gonzales, A.J.5
Shimamura, T.6
Zhao, F.7
Vincent, P.W.8
Naumov, G.N.9
Bradner, J.E.10
Althaus, I.W.11
Gandhi, L.12
Shapiro, G.I.13
Nelson, J.M.14
Heymach, J.V.15
Meyerson, M.16
Wong, K.-K.17
Jänne, P.A.18
-
14
-
-
84879367781
-
How good are my data and what is the resolution?
-
Evans P.R., Murshudov G.N. How good are my data and what is the resolution?. Acta Crystallogr. Sect. D. 2013, D69:1204-1214.
-
(2013)
Acta Crystallogr. Sect. D.
, vol.D69
, pp. 1204-1214
-
-
Evans, P.R.1
Murshudov, G.N.2
-
15
-
-
84908371107
-
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor
-
Finlay M.R., Anderton M., Ashton S., Ballard P., Bethel P.A., Box M.R., et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J. Med. Chem. 2014, 57:8249-8267.
-
(2014)
J. Med. Chem.
, vol.57
, pp. 8249-8267
-
-
Finlay, M.R.1
Anderton, M.2
Ashton, S.3
Ballard, P.4
Bethel, P.A.5
Box, M.R.6
-
16
-
-
84873406911
-
Insights into the aberrant activity of mutant EGFR kinase domain and drug recognition
-
Gajiwala K.S., Feng J., Ferre R., Ryan K., Brodsky O., Weinrich S., et al. Insights into the aberrant activity of mutant EGFR kinase domain and drug recognition. Structure 2013, 21:209-219.
-
(2013)
Structure
, vol.21
, pp. 209-219
-
-
Gajiwala, K.S.1
Feng, J.2
Ferre, R.3
Ryan, K.4
Brodsky, O.5
Weinrich, S.6
-
17
-
-
51049123872
-
Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor
-
Gonzales A.J., Hook K.E., Althaus I.W., Ellis P.A., Trachet E., Delaney A.M., Harvey P.J., Ellis T.A., Amato D.M., Nelson J.M., Fry D.W., Zhu T., Loi C.-M., Fakhoury S.A., Schlosser K.M., Sexton K.E., Winters R.T., Reed J.E., Bridges A.J., Lettiere D.J., Baker D.A., Yang J., Lee H.T., Tecle H., Vincent P.W. Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol. Cancer Ther. 2008, 7:1880-1889.
-
(2008)
Mol. Cancer Ther.
, vol.7
, pp. 1880-1889
-
-
Gonzales, A.J.1
Hook, K.E.2
Althaus, I.W.3
Ellis, P.A.4
Trachet, E.5
Delaney, A.M.6
Harvey, P.J.7
Ellis, T.A.8
Amato, D.M.9
Nelson, J.M.10
Fry, D.W.11
Zhu, T.12
Loi, C.-M.13
Fakhoury, S.A.14
Schlosser, K.M.15
Sexton, K.E.16
Winters, R.T.17
Reed, J.E.18
Bridges, A.J.19
Lettiere, D.J.20
Baker, D.A.21
Yang, J.22
Lee, H.T.23
Tecle, H.24
Vincent, P.W.25
more..
-
18
-
-
79959758717
-
Understanding the impact of the P-loop conformation on kinase selectivity
-
Guimarães C.R., Rai B.K., Munchhof M.J., Liu S., Wang J., Bhattacharya S.K., et al. Understanding the impact of the P-loop conformation on kinase selectivity. J. Chem. Inf. Model. 2011, 51:1199-1204.
-
(2011)
J. Chem. Inf. Model.
, vol.51
, pp. 1199-1204
-
-
Guimarães, C.R.1
Rai, B.K.2
Munchhof, M.J.3
Liu, S.4
Wang, J.5
Bhattacharya, S.K.6
-
19
-
-
84890823201
-
Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src
-
Hari S.B., Perera B.G., Ranjitkar P., Seeliger M.A., Maly D.J. Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src. ACS Chem. Biol. 2013, 8:2734-2743.
-
(2013)
ACS Chem. Biol.
, vol.8
, pp. 2734-2743
-
-
Hari, S.B.1
Perera, B.G.2
Ranjitkar, P.3
Seeliger, M.A.4
Maly, D.J.5
-
20
-
-
19944426858
-
High frequency of epidermal growth factor receptor mutations with complex patterns in non-small cell lung cancers related to gefitinib responsiveness in Taiwan
-
Huang S.F., Liu H.P., Li L.H., Ku Y.C., Fu Y.N., Tsai H.Y., et al. High frequency of epidermal growth factor receptor mutations with complex patterns in non-small cell lung cancers related to gefitinib responsiveness in Taiwan. Clin. Cancer Res. 2004, 10:8195-8203.
-
(2004)
Clin. Cancer Res.
, vol.10
, pp. 8195-8203
-
-
Huang, S.F.1
Liu, H.P.2
Li, L.H.3
Ku, Y.C.4
Fu, Y.N.5
Tsai, H.Y.6
-
21
-
-
69949151386
-
Factors underlying sensitivity of cancers to small-molecule kinase inhibitors
-
Jänne P.A., Gray N., Settleman J. Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nat. Rev. Drug Discovery 2009, 8:709-723.
-
(2009)
Nat. Rev. Drug Discovery
, vol.8
, pp. 709-723
-
-
Jänne, P.A.1
Gray, N.2
Settleman, J.3
-
22
-
-
84904624695
-
Clinical activity of the mutant-selective EGFR inhibitor AZD9291 in patients (pts) with EGFR inhibitor-resistant non-small cell lung cancer (NSCLC)
-
Janne P.A., Ramalingam S.S., Yang J.C.-H., Ahn M.J., Kim D.-W., Kim S.-W., et al. Clinical activity of the mutant-selective EGFR inhibitor AZD9291 in patients (pts) with EGFR inhibitor-resistant non-small cell lung cancer (NSCLC). Clin. Oncol. 2014, 32:5s.
-
(2014)
Clin. Oncol.
, vol.32
, pp. 5s
-
-
Janne, P.A.1
Ramalingam, S.S.2
Yang, J.C.-H.3
Ahn, M.J.4
Kim, D.-W.5
Kim, S.-W.6
-
24
-
-
84859418112
-
The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor
-
Kim Y., Ko J., Cui Z.-Y., Abolhoda A., Ahn J.S., Ou S.-H., Ahn M.-Y., Park K. The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor. Mol. Cancer Ther. 2012, 11:784-791.
-
(2012)
Mol. Cancer Ther.
, vol.11
, pp. 784-791
-
-
Kim, Y.1
Ko, J.2
Cui, Z.-Y.3
Abolhoda, A.4
Ahn, J.S.5
Ou, S.-H.6
Ahn, M.-Y.7
Park, K.8
-
25
-
-
10844231985
-
Mutations of the epidermal growth factor receptor gene in lung cancer: biological and clinical implications
-
Kosaka T., Yatabe Y., Endoh H., Kuwano H., Takahashi T., Mitsudomi T. Mutations of the epidermal growth factor receptor gene in lung cancer: biological and clinical implications. Cancer Res. 2004, 64:8919-8923.
-
(2004)
Cancer Res.
, vol.64
, pp. 8919-8923
-
-
Kosaka, T.1
Yatabe, Y.2
Endoh, H.3
Kuwano, H.4
Takahashi, T.5
Mitsudomi, T.6
-
26
-
-
2342471392
-
Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
-
Lynch T.J., Bell D.W., Sordella R., Gurubhagavatula S., Okimoto R.A., Brannigan B.W., et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N. Engl. J. Med. 2004, 350:2129-2139.
-
(2004)
N. Engl. J. Med.
, vol.350
, pp. 2129-2139
-
-
Lynch, T.J.1
Bell, D.W.2
Sordella, R.3
Gurubhagavatula, S.4
Okimoto, R.A.5
Brannigan, B.W.6
-
27
-
-
77953930730
-
Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR
-
Maemondo M., Inoue A., Kobayashi K., Sugawara S., Oizumi S., Isobe H., et al. Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N. Engl. J. Med. 2010, 362:2380-2388.
-
(2010)
N. Engl. J. Med.
, vol.362
, pp. 2380-2388
-
-
Maemondo, M.1
Inoue, A.2
Kobayashi, K.3
Sugawara, S.4
Oizumi, S.5
Isobe, H.6
-
28
-
-
0036849859
-
Blu-Ice and the distributed control system: software for data acquisition and instrument control at macromolecular crystallography beamlines
-
McPhillips T.M., McPhillips S.E., Chiu H.J., Cohen A.E., Deacon A.M., Ellis P.J., Garman E., Gonzalez A., Sauter N.K., Phizackerley R.P., Soltis S.M., Kuhn P. Blu-Ice and the distributed control system: software for data acquisition and instrument control at macromolecular crystallography beamlines. J. Synchrotron Radiat. 2002, 9:401-406.
-
(2002)
J. Synchrotron Radiat.
, vol.9
, pp. 401-406
-
-
McPhillips, T.M.1
McPhillips, S.E.2
Chiu, H.J.3
Cohen, A.E.4
Deacon, A.M.5
Ellis, P.J.6
Garman, E.7
Gonzalez, A.8
Sauter, N.K.9
Phizackerley, R.P.10
Soltis, S.M.11
Kuhn, P.12
-
29
-
-
75249087060
-
Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial
-
Mitsudomi T., Morita S., Yatabe Y., Negoro S., Okamoto I., Tsurutani J., et al. Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial. Lancet Oncol. 2010, 11:121-128.
-
(2010)
Lancet Oncol.
, vol.11
, pp. 121-128
-
-
Mitsudomi, T.1
Morita, S.2
Yatabe, Y.3
Negoro, S.4
Okamoto, I.5
Tsurutani, J.6
-
30
-
-
69949162760
-
Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma
-
Mok T.S., Wu Y.L., Thongprasert S., Yang C.H., Chu D.T., Saijo N., et al. Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N. Engl. J. Med. 2009, 361:947-957.
-
(2009)
N. Engl. J. Med.
, vol.361
, pp. 947-957
-
-
Mok, T.S.1
Wu, Y.L.2
Thongprasert, S.3
Yang, C.H.4
Chu, D.T.5
Saijo, N.6
-
31
-
-
79953763877
-
REFMAC5 for the refinement of macromolecular crystal structures
-
Murshudov G.N., Skubák P., Lebedev A.A., Pannu N.S., Steiner R.A., Nicholls R.A., Winn M.D., Long F., Vagin A.A. REFMAC5 for the refinement of macromolecular crystal structures. Acta Crystallogr. 2011, D67:355-367.
-
(2011)
Acta Crystallogr.
, vol.D67
, pp. 355-367
-
-
Murshudov, G.N.1
Skubák, P.2
Lebedev, A.A.3
Pannu, N.S.4
Steiner, R.A.5
Nicholls, R.A.6
Winn, M.D.7
Long, F.8
Vagin, A.A.9
-
32
-
-
4444223238
-
Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes
-
Nunes M., Shi C., Grenberger L.M. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol. Cancer Ther. 2004, 3:21-27.
-
(2004)
Mol. Cancer Ther.
, vol.3
, pp. 21-27
-
-
Nunes, M.1
Shi, C.2
Grenberger, L.M.3
-
33
-
-
2342624080
-
EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy
-
Paez J.G., Jänne P.A., Lee J.C., Tracy S., Greulich H., Gabriel S., et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004, 304:1497-1500.
-
(2004)
Science
, vol.304
, pp. 1497-1500
-
-
Paez, J.G.1
Jänne, P.A.2
Lee, J.C.3
Tracy, S.4
Greulich, H.5
Gabriel, S.6
-
34
-
-
4444344330
-
EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib
-
Pao W., Miller V., Zakowski M., Doherty J., Politi K., Sarkaria I., et al. EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc. Natl. Acad. Sci. U.S.A. 2004, 101:13306-13311.
-
(2004)
Proc. Natl. Acad. Sci. U.S.A.
, vol.101
, pp. 13306-13311
-
-
Pao, W.1
Miller, V.2
Zakowski, M.3
Doherty, J.4
Politi, K.5
Sarkaria, I.6
-
35
-
-
18244371651
-
Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain
-
Pao W., Miller V.A., Politi K.A., Riely G.J., Somwar R., Zakowski M.F., et al. Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med. 2005, 2:e73.
-
(2005)
PLoS Med.
, vol.2
, pp. e73
-
-
Pao, W.1
Miller, V.A.2
Politi, K.A.3
Riely, G.J.4
Somwar, R.5
Zakowski, M.F.6
-
36
-
-
84857502654
-
Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial
-
Rosell R., Carcereny E., Gervais R., Vergnenegre A., Massuti B., Felip E., et al. Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial. Lancet Oncol. 2012, 13:239-246.
-
(2012)
Lancet Oncol.
, vol.13
, pp. 239-246
-
-
Rosell, R.1
Carcereny, E.2
Gervais, R.3
Vergnenegre, A.4
Massuti, B.5
Felip, E.6
-
37
-
-
84883313959
-
Irreversible kinase inhibitors gain traction
-
Sanderson K. Irreversible kinase inhibitors gain traction. Nat. Rev. Drug Discovery 2013, 12:649-651.
-
(2013)
Nat. Rev. Drug Discovery
, vol.12
, pp. 649-651
-
-
Sanderson, K.1
-
38
-
-
65549152514
-
Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations
-
Seeliger M.A., Ranjitkar P., Kasap C., Shan Y., Shaw D.E., Shah N.P., Kuriyan J., Maly D.J. Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations. Cancer Res. 2009, 69:2384-2392.
-
(2009)
Cancer Res.
, vol.69
, pp. 2384-2392
-
-
Seeliger, M.A.1
Ranjitkar, P.2
Kasap, C.3
Shan, Y.4
Shaw, D.E.5
Shah, N.P.6
Kuriyan, J.7
Maly, D.J.8
-
39
-
-
33847323129
-
Epidermal growth factor receptor mutations in lung cancer
-
Sharma S.V., Bell D.W., Settleman J., Haber D.A. Epidermal growth factor receptor mutations in lung cancer. Nat. Rev. Cancer 2007, 7:169-181.
-
(2007)
Nat. Rev. Cancer
, vol.7
, pp. 169-181
-
-
Sharma, S.V.1
Bell, D.W.2
Settleman, J.3
Haber, D.A.4
-
40
-
-
20044364940
-
Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers
-
Shigematsu H., Lin L., Takahashi T., Nomura M., Suzuki M., Wistuba I.I., et al. Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers. J. Natl. Cancer Inst. 2005, 97:339-346.
-
(2005)
J. Natl. Cancer Inst.
, vol.97
, pp. 339-346
-
-
Shigematsu, H.1
Lin, L.2
Takahashi, T.3
Nomura, M.4
Suzuki, M.5
Wistuba, I.I.6
-
41
-
-
0034611617
-
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions
-
Smaill J.B., Rewcastle G.W., Bridges A.J., Zhou H., Showalter H.D.H., Fry D.W., Nelson J.M., Sherwood V., Elliott W.L., Vincent P.W., DeJohn D., Loo J.A., Gries K.D., Chan O.H., Reyner E.L., Lipka E., Denny W.A. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J. Med. Chem. 2000, 43:1380-1397.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 1380-1397
-
-
Smaill, J.B.1
Rewcastle, G.W.2
Bridges, A.J.3
Zhou, H.4
Showalter, H.D.H.5
Fry, D.W.6
Nelson, J.M.7
Sherwood, V.8
Elliott, W.L.9
Vincent, P.W.10
DeJohn, D.11
Loo, J.A.12
Gries, K.D.13
Chan, O.H.14
Reyner, E.L.15
Lipka, E.16
Denny, W.A.17
-
42
-
-
84867621201
-
Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker
-
Solca F., Dahl G., Zoephel A., Bader G., Sanderson M., Klein C., Kraemer O., Himmelsbach F., Haaksma E., Adolf G.R. Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker. J. Pharm. Exp. Ther. 2012, 343:342-350.
-
(2012)
J. Pharm. Exp. Ther.
, vol.343
, pp. 342-350
-
-
Solca, F.1
Dahl, G.2
Zoephel, A.3
Bader, G.4
Sanderson, M.5
Klein, C.6
Kraemer, O.7
Himmelsbach, F.8
Haaksma, E.9
Adolf, G.R.10
-
43
-
-
76249108622
-
Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation
-
Sos M.L., Rode H.B., Heynck S., Peifer M., Fischer F., Klüter S., Pawar V.G., Reuter C., Heuckmann J.M., Weiss J., Ruddigkeit L., Rabiller M., Koker M., Simard J.R., Getlik M., Yuza Y., Chen T.-H., Greulich H., Thomas R.K., Rauh D. Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation. Cancer Res. 2010, 70:868-874.
-
(2010)
Cancer Res.
, vol.70
, pp. 868-874
-
-
Sos, M.L.1
Rode, H.B.2
Heynck, S.3
Peifer, M.4
Fischer, F.5
Klüter, S.6
Pawar, V.G.7
Reuter, C.8
Heuckmann, J.M.9
Weiss, J.10
Ruddigkeit, L.11
Rabiller, M.12
Koker, M.13
Simard, J.R.14
Getlik, M.15
Yuza, Y.16
Chen, T.-H.17
Greulich, H.18
Thomas, R.K.19
Rauh, D.20
more..
-
44
-
-
13944262091
-
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity
-
Tsou H.-R., Overbeek-Klumpers E.G., Hallett W.A., Reich M.F., Floyd M.B., Johnson B.D., Michalak R.S., Nilakantan R., Discafani C., Golas J., Rabindran S.K., Shen R., Shi X., Wang Y.-F., Upeslacis J., Wissner A. Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. J. Med. Chem. 2005, 48:1107-1131.
-
(2005)
J. Med. Chem.
, vol.48
, pp. 1107-1131
-
-
Tsou, H.-R.1
Overbeek-Klumpers, E.G.2
Hallett, W.A.3
Reich, M.F.4
Floyd, M.B.5
Johnson, B.D.6
Michalak, R.S.7
Nilakantan, R.8
Discafani, C.9
Golas, J.10
Rabindran, S.K.11
Shen, R.12
Shi, X.13
Wang, Y.-F.14
Upeslacis, J.15
Wissner, A.16
-
45
-
-
0037413550
-
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2)
-
Wissner A., Overbeek E., Reich M.F., Floyd M.B., Johnson B.D., Mamuya N., Rosfjord E.C., Discafani C., Davis R., Shi X., Rabindran S.K., Gruber B.C., Ye F., Hallet W.A., Nilakantan R., Shen R., Wang Y.-F., Greenberger L.M., Tsou H.-R. Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2). J. Med. Chem. 2003, 46:49-63.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 49-63
-
-
Wissner, A.1
Overbeek, E.2
Reich, M.F.3
Floyd, M.B.4
Johnson, B.D.5
Mamuya, N.6
Rosfjord, E.C.7
Discafani, C.8
Davis, R.9
Shi, X.10
Rabindran, S.K.11
Gruber, B.C.12
Ye, F.13
Hallet, W.A.14
Nilakantan, R.15
Shen, R.16
Wang, Y.-F.17
Greenberger, L.M.18
Tsou, H.-R.19
-
46
-
-
84924787590
-
The 1.65Å resolution structure of the complex of AZD4547 with the kinase domain of FGFR1 displays exquisite molecular recognition
-
Yosaatmadja Y., Patterson A.V., Smaill J.B., Squire C.J. The 1.65Å resolution structure of the complex of AZD4547 with the kinase domain of FGFR1 displays exquisite molecular recognition. Acta Crystallogr. Sect. D: Biol. Crystallogr. 2015, 71:525-533.
-
(2015)
Acta Crystallogr. Sect. D: Biol. Crystallogr.
, vol.71
, pp. 525-533
-
-
Yosaatmadja, Y.1
Patterson, A.V.2
Smaill, J.B.3
Squire, C.J.4
-
47
-
-
33847406095
-
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity
-
Yun C.H., Boggon T.J., Li Y., Woo M.S., Greulich H., Meyerson M., et al. Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. Cancer Cell 2007, 11:217-227.
-
(2007)
Cancer Cell
, vol.11
, pp. 217-227
-
-
Yun, C.H.1
Boggon, T.J.2
Li, Y.3
Woo, M.S.4
Greulich, H.5
Meyerson, M.6
-
48
-
-
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
-
49
-
-
72949092456
-
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
-
Zhou W., Ercan D., Chen L., Yun C.H., Li D., Capelletti M., Cortot A.B., Chirieac L., Iacob R.E., Padera R., Engen J.R., Wong K.K., Eck M.J., Gray N.S., Jänne P.A. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009, 462:1070-1074.
-
(2009)
Nature
, vol.462
, pp. 1070-1074
-
-
Zhou, W.1
Ercan, D.2
Chen, L.3
Yun, C.H.4
Li, D.5
Capelletti, M.6
Cortot, A.B.7
Chirieac, L.8
Iacob, R.E.9
Padera, R.10
Engen, J.R.11
Wong, K.K.12
Eck, M.J.13
Gray, N.S.14
Jänne, P.A.15
-
50
-
-
79960889662
-
Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 study
-
Zhou C., Wu Y.L., Chen G., Feng J., Liu X.Q., Wang C., et al. Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 study. Lancet Oncol. 2011, 12:735-742.
-
(2011)
Lancet Oncol.
, vol.12
, pp. 735-742
-
-
Zhou, C.1
Wu, Y.L.2
Chen, G.3
Feng, J.4
Liu, X.Q.5
Wang, C.6
|