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Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors.
Wittlinger F, Ogboo BC, Shevchenko E, Damghani T, Pham CD, Schaeffner IK, Oligny BT, Chitnis SP, Beyett TS, Rasch A, Buckley B, Urul DA, Shaurova T, May EW, Schaefer EM, Eck MJ, Hershberger PA, Poso A, Laufer SA, Heppner DE. Wittlinger F, et al. Commun Chem. 2024 Feb 20;7(1):38. doi: 10.1038/s42004-024-01108-3. Commun Chem. 2024. PMID: 38378740 Free PMC article.
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.
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).
Heppner DE, Wittlinger F, Beyett TS, Shaurova T, Urul DA, Buckley B, Pham CD, Schaeffner IK, Yang B, Ogboo BC, May EW, Schaefer EM, Eck MJ, Laufer SA, Hershberger PA. Heppner DE, et al. ACS Med Chem Lett. 2022 Nov 10;13(12):1856-1863. doi: 10.1021/acsmedchemlett.2c00213. eCollection 2022 Dec 8. ACS Med Chem Lett. 2022. PMID: 36518696 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.
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. 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.
19 results