-
1
-
-
0034992521
-
The epidermal growth factor receptor family as a central element for cellular signal transduction and diversification
-
Prenzel N, Fischer OM, Streit S, Hart S, Ullrich A. The epidermal growth factor receptor family as a central element for cellular signal transduction and diversification. Endocr Relat Cancer. 2001; 8:11-31.
-
(2001)
Endocr Relat Cancer
, vol.8
, pp. 11-31
-
-
Prenzel, N.1
Fischer, O.M.2
Streit, S.3
Hart, S.4
Ullrich, A.5
-
2
-
-
77958478674
-
Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer
-
Pao W, Chmielecki J. Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer. Nat Rev Cancer. 2010; 10:760-774.
-
(2010)
Nat Rev Cancer
, vol.10
, pp. 760-774
-
-
Pao, W.1
Chmielecki, J.2
-
3
-
-
84883347910
-
Mutation incidence and coincidence in non small-cell lung cancer: meta-analyses by ethnicity and histology (mutMap)
-
Dearden S, Stevens J, Wu YL, Blowers D. Mutation incidence and coincidence in non small-cell lung cancer: meta-analyses by ethnicity and histology (mutMap). Ann Oncol. 2013; 24:2371-2376.
-
(2013)
Ann Oncol
, vol.24
, pp. 2371-2376
-
-
Dearden, S.1
Stevens, J.2
Wu, Y.L.3
Blowers, D.4
-
4
-
-
40049099220
-
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
-
Yun CH, Mengwasser KE, Toms AV, Woo MS, Greulich H, Wong KK, Meyerson M, Eck MJ. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci U S A. 2008; 105:2070-2075.
-
(2008)
Proc Natl Acad Sci U S A
, vol.105
, pp. 2070-2075
-
-
Yun, C.H.1
Mengwasser, K.E.2
Toms, A.V.3
Woo, M.S.4
Greulich, H.5
Wong, K.K.6
Meyerson, M.7
Eck, M.J.8
-
5
-
-
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 LR, Padera RF, Shapiro GI, Baum A, Himmelsbach F, Rettig WJ, Meyerson M, Solca F, Greulich H, Wong KK. 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
Rettig, W.J.11
Meyerson, M.12
Solca, F.13
Greulich, H.14
Wong, K.K.15
-
6
-
-
84858669035
-
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap?. A review of the clinical evidence
-
Ou SH. Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence. Crit Rev Oncol Hematol. 2012; 83:407-421.
-
(2012)
Crit Rev Oncol Hematol
, vol.83
, pp. 407-421
-
-
Ou, S.H.1
-
7
-
-
0034611617
-
Tyrosine kinase inhibit. 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 JB, Rewcastle GW, Loo JA, Greis KD, Chan OH, Reyner EL, Lipka E, Showalter HD, Vincent PW, Elliott WL, Denny WA. 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
Loo, J.A.3
Greis, K.D.4
Chan, O.H.5
Reyner, E.L.6
Lipka, E.7
Showalter, H.D.8
Vincent, P.W.9
Elliott, W.L.10
Denny, W.A.11
-
8
-
-
84922753595
-
Toward precision medicine with nextgeneration EGFR inhibitors in non-small-cell lung cancer
-
Yap TA, Popat S. Toward precision medicine with nextgeneration EGFR inhibitors in non-small-cell lung cancer. Pharmgenomics Pers Med. 2014; 7:285-295.
-
(2014)
Pharmgenomics Pers Med
, vol.7
, pp. 285-295
-
-
Yap, T.A.1
Popat, S.2
-
9
-
-
84904898065
-
AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer
-
Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, Hughes G, Rahi A, Jacobs VN, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014; 4:1046-1061.
-
(2014)
Cancer Discov
, 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
Orme, J.P.7
Finlay, M.R.8
Ward, R.A.9
Mellor, M.J.10
Hughes, G.11
Rahi, A.12
Jacobs, V.N.13
-
10
-
-
84887977876
-
Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790Mmediated resistance in NSCLC
-
Walter AO, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z, Wang Z, Sheets M, St Martin T, Karp R, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790Mmediated resistance in NSCLC. Cancer Discov. 2013; 3:1404-1415.
-
(2013)
Cancer Discov
, vol.3
, pp. 1404-1415
-
-
Walter, A.O.1
Sjin, R.T.2
Haringsma, H.J.3
Ohashi, K.4
Sun, J.5
Lee, K.6
Dubrovskiy, A.7
Labenski, M.8
Zhu, Z.9
Wang, Z.10
Sheets, M.11
St Martin, T.12
Karp, R.13
-
11
-
-
84945568175
-
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells
-
Wu H, Wang A, Zhang W, Wang B, Chen C, Wang W, Hu C, Ye Z, Zhao Z, Wang L, Li X, Yu K, Liu J, Wu J, Yan XE, Zhao P, et al. Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. Oncotarget. 2015; 6:31313-31322. doi: 10.18632/oncotarget.5182.
-
(2015)
Oncotarget
, vol.6
, pp. 31313-31322
-
-
Wu, H.1
Wang, A.2
Zhang, W.3
Wang, B.4
Chen, C.5
Wang, W.6
Hu, C.7
Ye, Z.8
Zhao, Z.9
Wang, L.10
Li, X.11
Yu, K.12
Liu, J.13
Wu, J.14
Yan, X.E.15
Zhao, P.16
-
12
-
-
84929465568
-
Selective antitumor activity of ibrutinib in EGFR-mutant non-small cell lung cancer cells
-
Gao W, Wang M, Wang L, Lu H, Wu S, Dai B, Ou Z, Zhang L, Heymach JV, Gold KA, Minna J, Roth JA, Hofstetter WL, Swisher SG, Fang B. Selective antitumor activity of ibrutinib in EGFR-mutant non-small cell lung cancer cells. J Natl Cancer Inst. 2014; 106.
-
(2014)
J Natl Cancer Inst
, pp. 106
-
-
Gao, W.1
Wang, M.2
Wang, L.3
Lu, H.4
Wu, S.5
Dai, B.6
Ou, Z.7
Zhang, L.8
Heymach, J.V.9
Gold, K.A.10
Minna, J.11
Roth, J.A.12
Hofstetter, W.L.13
Swisher, S.G.14
Fang, B.15
-
13
-
-
84903534871
-
Discovery of a series of 2, 5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity
-
Li X, Zuo Y, Tang G, Wang Y, Zhou Y, Wang X, Guo T, Xia M, Ding N, Pan Z. Discovery of a series of 2, 5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem. 2014; 57:5112-5128.
-
(2014)
J Med Chem
, vol.57
, pp. 5112-5128
-
-
Li, X.1
Zuo, Y.2
Tang, G.3
Wang, Y.4
Zhou, Y.5
Wang, X.6
Guo, T.7
Xia, M.8
Ding, N.9
Pan, Z.10
-
14
-
-
84960866293
-
Computational Tools To Model Halogen Bonds in Medicinal Chemistry
-
Ford MC, Ho PS. Computational Tools To Model Halogen Bonds in Medicinal Chemistry. J Med Chem. 2016; 59:1655-1670.
-
(2016)
J Med Chem
, vol.59
, pp. 1655-1670
-
-
Ford, M.C.1
Ho, P.S.2
-
15
-
-
2342471392
-
Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
-
Lynch TJ, Bell DW, Sordella R, Gurubhagavatula S, Okimoto RA, Brannigan BW, Harris PL, Haserlat SM, Supko JG, Haluska FG, Louis DN, Christiani DC, Settleman J, Haber DA. 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
Harris, P.L.7
Haserlat, S.M.8
Supko, J.G.9
Haluska, F.G.10
Louis, D.N.11
Christiani, D.C.12
Settleman, J.13
Haber, D.A.14
-
16
-
-
72949092456
-
Novel mutantselective EGFR kinase inhibitors against EGFR T790M
-
Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Janne PA. Novel mutantselective 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
Janne, P.A.15
-
17
-
-
85007524757
-
Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer
-
Wang S, Cang S, Liu D. Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016; 9:34.
-
(2016)
J Hematol Oncol
, vol.9
, pp. 34
-
-
Wang, S.1
Cang, S.2
Liu, D.3
-
18
-
-
33847406095
-
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity
-
Yun CH, Boggon TJ, Li Y, Woo MS, Greulich H, Meyerson M, Eck MJ. 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
Eck, M.J.7
-
19
-
-
84995480469
-
Hyperglycemia Associated With Targeted Oncologic Treatment: Mechanisms and Management
-
Goldman JW, Mendenhall MA, Rettinger SR. Hyperglycemia Associated With Targeted Oncologic Treatment: Mechanisms and Management. Oncologist. 2016.
-
(2016)
Oncologist
-
-
Goldman, J.W.1
Mendenhall, M.A.2
Rettinger, S.R.3
-
20
-
-
84960130421
-
Management of hyperglycemia from epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) targeting T790M-mediated resistance
-
Villadolid J, Ersek JL, Fong MK, Sirianno L, Story ES. Management of hyperglycemia from epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) targeting T790M-mediated resistance. Transl Lung Cancer Res. 2015; 4:576-583.
-
(2015)
Transl Lung Cancer Res
, vol.4
, pp. 576-583
-
-
Villadolid, J.1
Ersek, J.L.2
Fong, M.K.3
Sirianno, L.4
Story, E.S.5
-
21
-
-
84955494360
-
Abstract 793: Insulin-like growth factor 1 (IGF1R)/insulin receptor (INSR) inhibitory activity of rociletinib (CO-1686) and its metabolites in nonclinical models
-
Andrew D. Simmons SJ-T, Henry J. Haringsma, Andrew Allen, Thomas C. Harding. Abstract 793: Insulin-like growth factor 1 (IGF1R)/insulin receptor (INSR) inhibitory activity of rociletinib (CO-1686) and its metabolites in nonclinical models. Cancer Research. 2015; 75:793-793.
-
(2015)
Cancer Research
, vol.75
, pp. 793-793
-
-
Andrew, D.1
Simmons, S.J.-T.2
Haringsma, H.J.3
Allen, A.4
Harding, T.C.5
-
22
-
-
84994230246
-
Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation
-
Wang A, Yan XE, Wu H, Wang W, Hu C, Chen C, Zhao Z, Zhao P, Li X, Wang L, Wang B, Ye Z, Wang J, et al. Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. Oncotarget. 2016; 7:69760-69769. doi: 10.18632/oncotarget.11951.
-
(2016)
Oncotarget
, vol.7
, pp. 69760-69769
-
-
Wang, A.1
Yan, X.E.2
Wu, H.3
Wang, W.4
Hu, C.5
Chen, C.6
Zhao, Z.7
Zhao, P.8
Li, X.9
Wang, L.10
Wang, B.11
Ye, Z.12
Wang, J.13
-
23
-
-
28544438023
-
Activated epidermal growth factor receptor-Stat-3 signaling promotes tumor survival in vivo in non-small cell lung cancer
-
Haura EB, Zheng Z, Song L, Cantor A, Bepler G. Activated epidermal growth factor receptor-Stat-3 signaling promotes tumor survival in vivo in non-small cell lung cancer. Clin Cancer Res. 2005; 11:8288-8294.
-
(2005)
Clin Cancer Res
, vol.11
, pp. 8288-8294
-
-
Haura, E.B.1
Zheng, Z.2
Song, L.3
Cantor, A.4
Bepler, G.5
-
24
-
-
84905726946
-
Drug resistance via feedback activation of Stat3 in oncogeneaddicted cancer cells
-
Lee HJ, Zhuang G, Cao Y, Du P, Kim HJ, Settleman J. Drug resistance via feedback activation of Stat3 in oncogeneaddicted cancer cells. Cancer Cell. 2014; 26:207-221.
-
(2014)
Cancer Cell
, vol.26
, pp. 207-221
-
-
Lee, H.J.1
Zhuang, G.2
Cao, Y.3
Du, P.4
Kim, H.J.5
Settleman, J.6
-
25
-
-
0028234529
-
Jak-STAT pathways and transcriptional activation in response to IFNs and other extracellular signaling proteins
-
Darnell JE, Jr., Kerr IM, Stark GR. Jak-STAT pathways and transcriptional activation in response to IFNs and other extracellular signaling proteins. Science. 1994; 264:1415-1421.
-
(1994)
Science
, vol.264
, pp. 1415-1421
-
-
Darnell, J.E.1
Kerr, I.M.2
Stark, G.R.3
-
26
-
-
84949568982
-
BIM and mTOR expression levels predict outcome to erlotinib in EGFR-mutant nonsmall-cell lung cancer
-
Karachaliou N, Codony-Servat J, Teixido C, Pilotto S, Drozdowskyj A, Codony-Servat C, Gimenez-Capitan A, Molina-Vila MA, Bertran-Alamillo J, Gervais R, Massuti B, Moran T, Majem M, et al. BIM and mTOR expression levels predict outcome to erlotinib in EGFR-mutant nonsmall-cell lung cancer. Sci Rep. 2015; 5:17499.
-
(2015)
Sci Rep
, vol.5
, pp. 17499
-
-
Karachaliou, N.1
Codony-Servat, J.2
Teixido, C.3
Pilotto, S.4
Drozdowskyj, A.5
Codony-Servat, C.6
Gimenez-Capitan, A.7
Molina-Vila, M.A.8
Bertran-Alamillo, J.9
Gervais, R.10
Massuti, B.11
Moran, T.12
Majem, M.13
-
27
-
-
33745933955
-
HKL-3000: the integration of data reduction and structure solution-from diffraction images to an initial model in minutes
-
Minor W, Cymborowski M, Otwinowski Z, Chruszcz M. HKL-3000: the integration of data reduction and structure solution-from diffraction images to an initial model in minutes. Acta crystallographica Section D, Biological crystallography. 2006; 62:859-866.
-
(2006)
Acta crystallographica Section D, Biological crystallography
, vol.62
, pp. 859-866
-
-
Minor, W.1
Cymborowski, M.2
Otwinowski, Z.3
Chruszcz, M.4
-
28
-
-
34447508216
-
Phaser crystallographic software
-
McCoy AJ, Grosse-Kunstleve RW, Adams PD, Winn MD, Storoni LC, Read RJ. Phaser crystallographic software. Journal of applied crystallography. 2007; 40:658-674.
-
(2007)
Journal of applied crystallography
, vol.40
, pp. 658-674
-
-
McCoy, A.J.1
Grosse-Kunstleve, R.W.2
Adams, P.D.3
Winn, M.D.4
Storoni, L.C.5
Read, R.J.6
-
29
-
-
33745002702
-
An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor
-
Zhang X, Gureasko J, Shen K, Cole PA, 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
-
31
-
-
76449098262
-
PHENIX: a comprehensive Python-based system for macromolecular structure solution
-
Adams PD, Afonine PV, Bunkoczi G, Chen VB, Davis IW, Echols N, Headd JJ, Hung LW, Kapral GJ, Grosse-Kunstleve RW, McCoy AJ, Moriarty NW, Oeffner R, et al. PHENIX: a comprehensive Python-based system for macromolecular structure solution. Acta Crystallogr D Biol Crystallogr. 2010; 66:213-221.
-
(2010)
Acta Crystallogr D Biol Crystallogr
, vol.66
, pp. 213-221
-
-
Adams, P.D.1
Afonine, P.V.2
Bunkoczi, G.3
Chen, V.B.4
Davis, I.W.5
Echols, N.6
Headd, J.J.7
Hung, L.W.8
Kapral, G.J.9
Grosse-Kunstleve, R.W.10
McCoy, A.J.11
Moriarty, N.W.12
Oeffner, R.13
-
32
-
-
7544226311
-
PRODRG: a tool for high-throughput crystallography of protein-ligand complexes
-
Schuttelkopf AW, van Aalten DM. PRODRG: a tool for high-throughput crystallography of protein-ligand complexes. Acta Crystallogr D Biol Crystallogr. 2004; 60:1355-1363.
-
(2004)
Acta Crystallogr D Biol Crystallogr
, vol.60
, pp. 1355-1363
-
-
Schuttelkopf, A.W.1
van Aalten, D.M.2
|