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Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain.
Pao W, Miller VA, Politi KA, Riely GJ, Somwar R, Zakowski MF, Kris MG, Varmus H. Pao W, et al. PLoS Med. 2005 Mar;2(3):e73. doi: 10.1371/journal.pmed.0020073. Epub 2005 Feb 22. PLoS Med. 2005. PMID: 15737014 Free PMC article.
Rationale for co-targeting IGF-1R and ALK in ALK fusion-positive lung cancer.
Lovly CM, McDonald NT, Chen H, Ortiz-Cuaran S, Heukamp LC, Yan Y, Florin A, Ozretić L, Lim D, Wang L, Chen Z, Chen X, Lu P, Paik PK, Shen R, Jin H, Buettner R, Ansén S, Perner S, Brockmann M, Bos M, Wolf J, Gardizi M, Wright GM, Solomon B, Russell PA, Rogers TM, Suehara Y, Red-Brewer M, Tieu R, de Stanchina E, Wang Q, Zhao Z, Johnson DH, Horn L, Wong KK, Thomas RK, Ladanyi M, Pao W. Lovly CM, et al. Nat Med. 2014 Sep;20(9):1027-34. doi: 10.1038/nm.3667. Epub 2014 Aug 31. Nat Med. 2014. PMID: 25173427 Free PMC article.
NF-κB drives acquired resistance to a novel mutant-selective EGFR inhibitor.
Galvani E, Sun J, Leon LG, Sciarrillo R, Narayan RS, Sjin RT, Lee K, Ohashi K, Heideman DA, Alfieri RR, Heynen GJ, Bernards R, Smit EF, Pao W, Peters GJ, Giovannetti E. Galvani E, et al. Oncotarget. 2015 Dec 15;6(40):42717-32. doi: 10.18632/oncotarget.3956. Oncotarget. 2015. PMID: 26015408 Free PMC article.
Epidermal growth factor receptor as a novel molecular target for aggressive papillary tumors in the middle ear and temporal bone.
Kawabata S, Hollander MC, Munasinghe JP, Brinster LR, Mercado-Matos JR, Li J, Regales L, Pao W, Jänne PA, Wong KK, Butman JA, Lonser RR, Hansen MR, Gurgel RK, Vortmeyer AO, Dennis PA. Kawabata S, et al. Oncotarget. 2015 May 10;6(13):11357-68. doi: 10.18632/oncotarget.3605. Oncotarget. 2015. PMID: 26027747 Free PMC article.
EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer.
Amato KR, Wang S, Tan L, Hastings AK, Song W, Lovly CM, Meador CB, Ye F, Lu P, Balko JM, Colvin DC, Cates JM, Pao W, Gray NS, Chen J. Amato KR, et al. Cancer Res. 2016 Jan 15;76(2):305-18. doi: 10.1158/0008-5472.CAN-15-0717. Epub 2016 Jan 7. Cancer Res. 2016. PMID: 26744526 Free PMC article.
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, Red Brewer M, Ichihara E, Sun J, Jin H, Ballard P, Al-Kadhimi K, Rowlinson R, Klinowska T, Richmond GH, Cantarini M, Kim DW, Ranson MR, Pao W. Cross DA, et al. Cancer Discov. 2014 Sep;4(9):1046-61. doi: 10.1158/2159-8290.CD-14-0337. Epub 2014 Jun 3. Cancer Discov. 2014. PMID: 24893891 Free PMC article.
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. Walter AO, et al. Cancer Discov. 2013 Dec;3(12):1404-15. doi: 10.1158/2159-8290.CD-13-0314. Epub 2013 Sep 24. Cancer Discov. 2013. PMID: 24065731 Free PMC article.
Maximizing the benefits of off-target kinase inhibitor activity.
Red Brewer M, Pao W. Red Brewer M, et al. Cancer Discov. 2013 Feb;3(2):138-40. doi: 10.1158/2159-8290.CD-12-0581. Cancer Discov. 2013. PMID: 23400472
MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib.
Bean J, Brennan C, Shih JY, Riely G, Viale A, Wang L, Chitale D, Motoi N, Szoke J, Broderick S, Balak M, Chang WC, Yu CJ, Gazdar A, Pass H, Rusch V, Gerald W, Huang SF, Yang PC, Miller V, Ladanyi M, Yang CH, Pao W. Bean J, et al. Proc Natl Acad Sci U S A. 2007 Dec 26;104(52):20932-7. doi: 10.1073/pnas.0710370104. Epub 2007 Dec 18. Proc Natl Acad Sci U S A. 2007. PMID: 18093943 Free PMC article.
MET Exon 14 Skipping in Non-Small Cell Lung Cancer.
Heist RS, Shim HS, Gingipally S, Mino-Kenudson M, Le L, Gainor JF, Zheng Z, Aryee M, Xia J, Jia P, Jin H, Zhao Z, Pao W, Engelman JA, Iafrate AJ. Heist RS, et al. Oncologist. 2016 Apr;21(4):481-6. doi: 10.1634/theoncologist.2015-0510. Epub 2016 Mar 28. Oncologist. 2016. PMID: 27022036 Free PMC article.
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