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Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors.
Heppner D, Wittlinger F, Ogboo B, Shevchenko E, Damghani T, Pham C, Schaeffner I, Oligny B, Chitnis S, Beyett T, Rasch A, Buckley B, Urul D, Shaurova T, May E, Schaefer E, Eck M, Hershberger P, Poso A, Laufer S. Heppner D, et al. Res Sq [Preprint]. 2023 Sep 13:rs.3.rs-3286949. doi: 10.21203/rs.3.rs-3286949/v1. Res Sq. 2023. PMID: 37790373 Free PMC article. Updated. Preprint.
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. Among authors: heppner de. 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.
A driving test for oncogenic mutations.
Heppner DE, Beyett TS, Eck MJ. Heppner DE, et al. J Biol Chem. 2019 Jun 14;294(24):9390-9391. doi: 10.1074/jbc.H119.009452. J Biol Chem. 2019. PMID: 31201242 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: heppner de. 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.
Architecture of the NADPH oxidase family of enzymes.
Ogboo BC, Grabovyy UV, Maini A, Scouten S, van der Vliet A, Mattevi A, Heppner DE. Ogboo BC, et al. Redox Biol. 2022 Jun;52:102298. doi: 10.1016/j.redox.2022.102298. Epub 2022 Mar 18. Redox Biol. 2022. PMID: 35334249 Free PMC article. Review.
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. Among authors: heppner de. 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.
170 results