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Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Ward RA, Anderton MJ, Ashton S, Bethel PA, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross DA, Dakin LA, Debreczeni JÉ, Eberlein C, Finlay MR, Hill GB, Grist M, Klinowska TC, Lane C, Martin S, Orme JP, Smith P, Wang F, Waring MJ. Ward RA, et al. Among authors: eberlein c. J Med Chem. 2013 Sep 12;56(17):7025-48. doi: 10.1021/jm400822z. Epub 2013 Aug 30. J Med Chem. 2013. PMID: 23930994
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. Among authors: eberlein c. 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.
Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation.
Hennessy EJ, Chuaqui C, Ashton S, Colclough N, Cross DA, Debreczeni JÉ, Eberlein C, Gingipalli L, Klinowska TC, Orme JP, Sha L, Wu X. Hennessy EJ, et al. Among authors: eberlein c. ACS Med Chem Lett. 2016 Mar 21;7(5):514-9. doi: 10.1021/acsmedchemlett.6b00058. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190603 Free PMC article.
MEDI0639: a novel therapeutic antibody targeting Dll4 modulates endothelial cell function and angiogenesis in vivo.
Jenkins DW, Ross S, Veldman-Jones M, Foltz IN, Clavette BC, Manchulenko K, Eberlein C, Kendrew J, Petteruti P, Cho S, Damschroder M, Peng L, Baker D, Smith NR, Weir HM, Blakey DC, Bedian V, Barry ST. Jenkins DW, et al. Among authors: eberlein c. Mol Cancer Ther. 2012 Aug;11(8):1650-60. doi: 10.1158/1535-7163.MCT-11-1027. Epub 2012 Jun 7. Mol Cancer Ther. 2012. PMID: 22679110
AKT-mTORC1 reactivation is the dominant resistance driver for PI3Kβ/AKT inhibitors in PTEN-null breast cancer and can be overcome by combining with Mcl-1 inhibitors.
Dunn S, Eberlein C, Yu J, Gris-Oliver A, Ong SH, Yelland U, Cureton N, Staniszewska A, McEwen R, Fox M, Pilling J, Hopcroft P, Coker EA, Jaaks P, Garnett MJ, Isherwood B, Serra V, Davies BR, Barry ST, Lynch JT, Yusa K. Dunn S, et al. Among authors: eberlein c. Oncogene. 2022 Nov;41(46):5046-5060. doi: 10.1038/s41388-022-02482-9. Epub 2022 Oct 14. Oncogene. 2022. PMID: 36241868 Free PMC article.
93 results