Format
Sort by
Items per page

Send to

Choose Destination

Links from PubMed

Items: 1 to 20 of 122

1.

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.

Michalczyk A, Klüter S, Rode HB, Simard JR, Grütter C, Rabiller M, Rauh D.

Bioorg Med Chem. 2008 Apr 1;16(7):3482-8. doi: 10.1016/j.bmc.2008.02.053. Epub 2008 Feb 20.

PMID:
18316192
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.

Resistance to an irreversible epidermal growth factor receptor (EGFR) inhibitor in EGFR-mutant lung cancer reveals novel treatment strategies.

Yu Z, Boggon TJ, Kobayashi S, Jin C, Ma PC, Dowlati A, Kern JA, Tenen DG, Halmos B.

Cancer Res. 2007 Nov 1;67(21):10417-27.

4.

Combined treatment with silibinin and epidermal growth factor receptor tyrosine kinase inhibitors overcomes drug resistance caused by T790M mutation.

Rho JK, Choi YJ, Jeon BS, Choi SJ, Cheon GJ, Woo SK, Kim HR, Kim CH, Choi CM, Lee JC.

Mol Cancer Ther. 2010 Dec;9(12):3233-43. doi: 10.1158/1535-7163.MCT-10-0625.

5.

Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance.

Klüter S, Simard JR, Rode HB, Grütter C, Pawar V, Raaijmakers HC, Barf TA, Rabiller M, van Otterlo WA, Rauh D.

Chembiochem. 2010 Dec 10;11(18):2557-66. doi: 10.1002/cbic.201000352.

PMID:
21080395
6.

An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor.

Kobayashi S, Ji H, Yuza Y, Meyerson M, Wong KK, Tenen DG, Halmos B.

Cancer Res. 2005 Aug 15;65(16):7096-101.

7.

Identification of novel drug-resistant EGFR mutant inhibitors by in silico screening using comprehensive assessments of protein structures.

Sato T, Watanabe H, Tsuganezawa K, Yuki H, Mikuni J, Yoshikawa S, Kukimoto-Niino M, Fujimoto T, Terazawa Y, Wakiyama M, Kojima H, Okabe T, Nagano T, Shirouzu M, Yokoyama S, Tanaka A, Honma T.

Bioorg Med Chem. 2012 Jun 15;20(12):3756-67. doi: 10.1016/j.bmc.2012.04.042. Epub 2012 Apr 27.

PMID:
22607878
8.

Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.

Wissner A, Fraser HL, Ingalls CL, Dushin RG, Floyd MB, Cheung K, Nittoli T, Ravi MR, Tan X, Loganzo F.

Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. Epub 2007 Mar 23.

PMID:
17416531
9.

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.

10.

Homology models of the mutated EGFR and their response towards quinazoline analogues.

Kotra S, Madala KK, Jamil K.

J Mol Graph Model. 2008 Oct;27(3):244-54. doi: 10.1016/j.jmgm.2008.04.010. Epub 2008 May 3.

PMID:
18585943
11.

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.

Proc Natl Acad Sci U S A. 2008 Feb 12;105(6):2070-5. doi: 10.1073/pnas.0709662105. Epub 2008 Jan 28.

12.

Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library.

Zhang Q, Liu Y, Gao F, Ding Q, Cho C, Hur W, Jin Y, Uno T, Joazeiro CA, Gray N.

J Am Chem Soc. 2006 Feb 22;128(7):2182-3.

PMID:
16478150
13.

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.

14.

Discovery of 6-substituted 4-anilinoquinazolines with dioxygenated rings as novel EGFR tyrosine kinase inhibitors.

Li DD, Fang F, Li JR, Du QR, Sun J, Gong HB, Zhu HL.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5870-5. doi: 10.1016/j.bmcl.2012.07.079. Epub 2012 Jul 31.

PMID:
22901387
15.

Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.

Zhang X, Peng T, Ji X, Li J, Tong L, Li Z, Yang W, Xu Y, Li M, Ding J, Jiang H, Xie H, Liu H.

Bioorg Med Chem. 2013 Dec 15;21(24):7988-98. doi: 10.1016/j.bmc.2013.09.049. Epub 2013 Oct 2.

PMID:
24183742
16.

Comparison of the EGFR resistance mutation profiles generated by EGFR-targeted tyrosine kinase inhibitors and the impact of drug combinations.

Avizienyte E, Ward RA, Garner AP.

Biochem J. 2008 Oct 15;415(2):197-206. doi: 10.1042/BJ20080728.

PMID:
18588508
17.

A water-based mechanism of specificity and resistance for lapatinib with ErbB family kinases.

Huang Y, Rizzo RC.

Biochemistry. 2012 Mar 27;51(12):2390-406. doi: 10.1021/bi2016553. Epub 2012 Mar 12.

PMID:
22352796
19.

Novel mutant-selective 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, Jänne PA.

Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622.

20.

Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib.

Gilmer TM, Cable L, Alligood K, Rusnak D, Spehar G, Gallagher KT, Woldu E, Carter HL, Truesdale AT, Shewchuk L, Wood ER.

Cancer Res. 2008 Jan 15;68(2):571-9. doi: 10.1158/0008-5472.CAN-07-2404.

Supplemental Content

Support Center