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Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors.
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.
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Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Amrhein JA, Beyett TS, Feng WW, Krämer A, Weckesser J, Schaeffner IK, Rana JK, Jänne PA, Eck MJ, Knapp S, Hanke T.
Amrhein JA, et al. Among authors: schaeffner ik.
J Med Chem. 2022 Dec 8;65(23):15679-15697. doi: 10.1021/acs.jmedchem.2c01041. Epub 2022 Nov 16.
J Med Chem. 2022.
PMID: 36384036
Free PMC article.
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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. Among authors: schaeffner ik.
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.
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A Constitutive EGFR Kinase Dimer to Study Inhibitor Pharmacology.
Kim JJ, Schaeffner IK, Heppner DE, To C, Jänne PA, Beyett TS, Eck MJ.
Kim JJ, et al. Among authors: schaeffner ik.
Mol Pharmacol. 2024 Jan 10;105(2):97-103. doi: 10.1124/molpharm.123.000768.
Mol Pharmacol. 2024.
PMID: 38164587
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Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase.
Beyett TS, Rana JK, Schaeffner IK, Heppner DE, Eck MJ.
Beyett TS, et al. Among authors: schaeffner ik.
ChemMedChem. 2024 Mar 24:e202300343. doi: 10.1002/cmdc.202300343. Online ahead of print.
ChemMedChem. 2024.
PMID: 38523074
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