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Items: 1 to 20 of 86

1.

In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing.

Tjin Tham Sjin R, Lee K, Walter AO, Dubrovskiy A, Sheets M, Martin TS, Labenski MT, Zhu Z, Tester R, Karp R, Medikonda A, Chaturvedi P, Ren Y, Haringsma H, Etter J, Raponi M, Simmons AD, Harding TC, Niu D, Nacht M, Westlin WF, Petter RC, Allen A, Singh J.

Mol Cancer Ther. 2014 Jun;13(6):1468-79. doi: 10.1158/1535-7163.MCT-13-0966. Epub 2014 Apr 10.

2.

The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor.

Godin-Heymann N, Ulkus L, Brannigan BW, McDermott U, Lamb J, Maheswaran S, Settleman J, Haber DA.

Mol Cancer Ther. 2008 Apr;7(4):874-9. doi: 10.1158/1535-7163.MCT-07-2387.

3.

Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647.

Gendreau SB, Ventura R, Keast P, Laird AD, Yakes FM, Zhang W, Bentzien F, Cancilla B, Lutman J, Chu F, Jackman L, Shi Y, Yu P, Wang J, Aftab DT, Jaeger CT, Meyer SM, De Costa A, Engell K, Chen J, Martini JF, Joly AH.

Clin Cancer Res. 2007 Jun 15;13(12):3713-23.

4.

Combined therapy with mutant-selective EGFR inhibitor and Met kinase inhibitor for overcoming erlotinib resistance in EGFR-mutant lung cancer.

Nakagawa T, Takeuchi S, Yamada T, Nanjo S, Ishikawa D, Sano T, Kita K, Nakamura T, Matsumoto K, Suda K, Mitsudomi T, Sekido Y, Uenaka T, Yano S.

Mol Cancer Ther. 2012 Oct;11(10):2149-57. doi: 10.1158/1535-7163.MCT-12-0195. Epub 2012 Jul 25.

5.

Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated 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, van Kalken D, Chaturvedi P, Niu D, Nacht M, Petter RC, Westlin W, Lin K, Jaw-Tsai S, Raponi M, Van Dyke T, Etter J, Weaver Z, Pao W, Singh J, Simmons AD, Harding TC, Allen A.

Cancer Discov. 2013 Dec;3(12):1404-15. doi: 10.1158/2159-8290.CD-13-0314. Epub 2013 Sep 24.

6.

Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant.

Zhou W, Liu X, Tu Z, Zhang L, Ku X, Bai F, Zhao Z, Xu Y, Ding K, Li H.

J Med Chem. 2013 Oct 24;56(20):7821-37. doi: 10.1021/jm401045n. Epub 2013 Oct 9.

PMID:
24053674
7.

TAE226, a Bis-Anilino Pyrimidine Compound, Inhibits the EGFR-Mutant Kinase Including T790M Mutant to Show Anti-Tumor Effect on EGFR-Mutant Non-Small Cell Lung Cancer Cells.

Otani H, Yamamoto H, Takaoka M, Sakaguchi M, Soh J, Jida M, Ueno T, Kubo T, Asano H, Tsukuda K, Kiura K, Hatakeyama S, Kawahara E, Naomoto Y, Miyoshi S, Toyooka S.

PLoS One. 2015 Jun 19;10(6):e0129838. doi: 10.1371/journal.pone.0129838. eCollection 2015.

8.

Curcumin induces EGFR degradation in lung adenocarcinoma and modulates p38 activation in intestine: the versatile adjuvant for gefitinib therapy.

Lee JY, Lee YM, Chang GC, Yu SL, Hsieh WY, Chen JJ, Chen HW, Yang PC.

PLoS One. 2011;6(8):e23756. doi: 10.1371/journal.pone.0023756. Epub 2011 Aug 17.

9.

EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.

Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Pferdekamper AC, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, DiDonato M, Bursulaya B, Lelais G, Barretina J, McNeill M, Epple R, Marsilje TH, Pathan N, Engelman JA, Michellys PY, McNamara P, Harris J, Bender S, Kasibhatla S.

Cancer Res. 2016 Mar 15;76(6):1591-602. doi: 10.1158/0008-5472.CAN-15-2581. Epub 2016 Jan 29.

10.

Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant.

Chang S, Zhang L, Xu S, Luo J, Lu X, Zhang Z, Xu T, Liu Y, Tu Z, Xu Y, Ren X, Geng M, Ding J, Pei D, Ding K.

J Med Chem. 2012 Mar 22;55(6):2711-23. doi: 10.1021/jm201591k. Epub 2012 Mar 1.

PMID:
22339342
11.

SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo.

Pan Y, Xu Y, Feng S, Luo S, Zheng R, Yang J, Wang L, Zhong L, Yang HY, Wang BL, Yu Y, Liu J, Cao Z, Wang X, Ji P, Wang Z, Chen X, Zhang S, Wei YQ, Yang SY.

Mol Cancer Ther. 2012 Apr;11(4):952-62. doi: 10.1158/1535-7163.MCT-11-0679. Epub 2012 Feb 8.

12.

Recent Development of the Second and Third Generation Irreversible Epidermal Growth Factor Receptor Inhibitors.

Han W, Du Y.

Chem Biodivers. 2017 Jul;14(7). doi: 10.1002/cbdv.201600372. Epub 2017 Jun 9. Review.

PMID:
28075527
13.

MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation.

Rho JK, Choi YJ, Kim SY, Kim TW, Choi EK, Yoon SJ, Park BM, Park E, Bae JH, Choi CM, Lee JC.

Cancer Res. 2014 Jan 1;74(1):253-62. doi: 10.1158/0008-5472.CAN-13-1103. Epub 2013 Oct 28.

14.

Transcriptional profiling identifies cyclin D1 as a critical downstream effector of mutant epidermal growth factor receptor signaling.

Kobayashi S, Shimamura T, Monti S, Steidl U, Hetherington CJ, Lowell AM, Golub T, Meyerson M, Tenen DG, Shapiro GI, Halmos B.

Cancer Res. 2006 Dec 1;66(23):11389-98.

15.

Hsp90 inhibition by WK88-1 potently suppresses the growth of gefitinib-resistant H1975 cells harboring the T790M mutation in EGFR.

Hong YS, Jang WJ, Chun KS, Jeong CH.

Oncol Rep. 2014 Jun;31(6):2619-24. doi: 10.3892/or.2014.3161. Epub 2014 Apr 28.

PMID:
24789511
16.

Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models.

Suzuki T, Fujii A, Ohya J, Nakamura H, Fujita F, Koike M, Fujita M.

Cancer Sci. 2009 Aug;100(8):1526-31. doi: 10.1111/j.1349-7006.2009.01197.x. Epub 2009 May 13.

17.

Addition of S-1 to the epidermal growth factor receptor inhibitor gefitinib overcomes gefitinib resistance in non-small cell lung cancer cell lines with MET amplification.

Okabe T, Okamoto I, Tsukioka S, Uchida J, Hatashita E, Yamada Y, Yoshida T, Nishio K, Fukuoka M, Jänne PA, Nakagawa K.

Clin Cancer Res. 2009 Feb 1;15(3):907-13. doi: 10.1158/1078-0432.CCR-08-2251.

18.

Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.

Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY.

J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19.

PMID:
27433829
19.

Highly sensitive and noninvasive detection of epidermal growth factor receptor T790M mutation in non-small cell lung cancer.

He C, Zheng L, Xu Y, Liu M, Li Y, Xu J.

Clin Chim Acta. 2013 Oct 21;425:119-24. doi: 10.1016/j.cca.2013.07.012. Epub 2013 Jul 23.

PMID:
23886554
20.

Antitumor activity of selective MEK1/2 inhibitor AZD6244 in combination with PI3K/mTOR inhibitor BEZ235 in gefitinib-resistant NSCLC xenograft models.

Qu Y, Wu X, Yin Y, Yang Y, Ma D, Li H.

J Exp Clin Cancer Res. 2014 Jun 17;33:52. doi: 10.1186/1756-9966-33-52.

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