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Page 1
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor.
To C, Jang J, Chen T, Park E, Mushajiang M, De Clercq DJH, Xu M, Wang S, Cameron MD, Heppner DE, Shin BH, Gero TW, Yang A, Dahlberg SE, Wong KK, Eck MJ, Gray NS, Jänne PA. To C, et al. Cancer Discov. 2019 Jul;9(7):926-943. doi: 10.1158/2159-8290.CD-18-0903. Epub 2019 May 15. Cancer Discov. 2019. PMID: 31092401 Free PMC article.
Discovery of a potent dual ALK and EGFR T790M inhibitor.
Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne PA, Choi HG, Gray NS. Jang J, et al. Among authors: to c. Eur J Med Chem. 2017 Aug 18;136:497-510. doi: 10.1016/j.ejmech.2017.04.079. Epub 2017 May 3. Eur J Med Chem. 2017. PMID: 28528303 Free PMC article.
EGFR-Mutated Lung Cancers Resistant to Osimertinib through EGFR C797S Respond to First-Generation Reversible EGFR Inhibitors but Eventually Acquire EGFR T790M/C797S in Preclinical Models and Clinical Samples.
Rangachari D, To C, Shpilsky JE, VanderLaan PA, Kobayashi SS, Mushajiang M, Lau CJ, Paweletz CP, Oxnard GR, Jänne PA, Costa DB. Rangachari D, et al. Among authors: to c. J Thorac Oncol. 2019 Nov;14(11):1995-2002. doi: 10.1016/j.jtho.2019.07.016. Epub 2019 Aug 1. J Thorac Oncol. 2019. PMID: 31377341 Free PMC article.
Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway.
Kurppa KJ, Liu Y, To C, Zhang T, Fan M, Vajdi A, Knelson EH, Xie Y, Lim K, Cejas P, Portell A, Lizotte PH, Ficarro SB, Li S, Chen T, Haikala HM, Wang H, Bahcall M, Gao Y, Shalhout S, Boettcher S, Shin BH, Thai T, Wilkens MK, Tillgren ML, Mushajiang M, Xu M, Choi J, Bertram AA, Ebert BL, Beroukhim R, Bandopadhayay P, Awad MM, Gokhale PC, Kirschmeier PT, Marto JA, Camargo FD, Haq R, Paweletz CP, Wong KK, Barbie DA, Long HW, Gray NS, Jänne PA. Kurppa KJ, et al. Among authors: to c. Cancer Cell. 2020 Jan 13;37(1):104-122.e12. doi: 10.1016/j.ccell.2019.12.006. Cancer Cell. 2020. PMID: 31935369 Free PMC article.
Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR-mutant lung cancer.
Eser PÖ, Paranal RM, Son J, Ivanova E, Kuang Y, Haikala HM, To C, Okoro JJ, Dholakia KH, Choi J, Eum Y, Ogino A, Missios P, Ercan D, Xu M, Poitras MJ, Wang S, Ngo K, Dills M, Yanagita M, Lopez T, Lin M, Tsai J, Floch N, Chambers ES, Heng J, Anjum R, Santucci AD, Michael K, Schuller AG, Cross D, Smith PD, Oxnard GR, Barbie DA, Sholl LM, Bahcall M, Palakurthi S, Gokhale PC, Paweletz CP, Daley GQ, Jänne PA. Eser PÖ, et al. Among authors: to c. Sci Transl Med. 2021 Sep;13(609):eabb3738. doi: 10.1126/scitranslmed.abb3738. Epub 2021 Sep 1. Sci Transl Med. 2021. PMID: 34516823 Free PMC article.
Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
Wittlinger F, Heppner DE, To C, Günther M, Shin BH, Rana JK, Schmoker AM, Beyett TS, Berger LM, Berger BT, Bauer N, Vasta JD, Corona CR, Robers MB, Knapp S, Jänne PA, Eck MJ, Laufer SA. Wittlinger F, et al. Among authors: to c. J Med Chem. 2022 Jan 27;65(2):1370-1383. doi: 10.1021/acs.jmedchem.1c00848. Epub 2021 Oct 20. J Med Chem. 2022. PMID: 34668706 Free PMC article.
Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC.
Gero TW, Heppner DE, Beyett TS, To C, Azevedo SC, Jang J, Bunnell T, Feru F, Li Z, Shin BH, Soroko KM, Gokhale PC, Gray NS, Jänne PA, Eck MJ, Scott DA. Gero TW, et al. Among authors: to c. Bioorg Med Chem Lett. 2022 Jul 15;68:128718. doi: 10.1016/j.bmcl.2022.128718. Epub 2022 Apr 1. Bioorg Med Chem Lett. 2022. PMID: 35378251 Free PMC article.
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer.
To C, Beyett TS, Jang J, Feng WW, Bahcall M, Haikala HM, Shin BH, Heppner DE, Rana JK, Leeper BA, Soroko KM, Poitras MJ, Gokhale PC, Kobayashi Y, Wahid K, Kurppa KJ, Gero TW, Cameron MD, Ogino A, Mushajiang M, Xu C, Zhang Y, Scott DA, Eck MJ, Gray NS, Jänne PA. To C, et al. Nat Cancer. 2022 Apr;3(4):402-417. doi: 10.1038/s43018-022-00351-8. Epub 2022 Apr 14. Nat Cancer. 2022. PMID: 35422503 Free PMC article.
408 results