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Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)

David Heppner, Tyler Beyett, Tatiana Shaurova, Calvin Pham, Florian Wittlinger, Ilse Schaeffner, Bo Yang, Blessing Ogboo, Stefan Laufer, Michael Eck, Pamela Hershberger

Version 2 posted 08 September 2022

818

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Biological and Medicinal Chemistry

Working Paper

Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles

Moritz Schwarz, Maksym Kurkunov, Florian Wittlinger, Ramona Rudalska, Guiqun Wang, Martin P. Schwalm, Alexander Rasch, Benedikt Wagner, Stefan A. Laufer, Stefan Knapp, Daniel Dauch, Matthias Gehringer

Version 2 posted 25 March 2024

1,517

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Biological and Medicinal Chemistry

Working Paper

The origin of potency and mutant-selective inhibition by bivalent ATP-allosteric EGFR inhibitors

Florian Wittlinger, Surbhi P Chitnis, Calvin D Pham, Tahereh Damghani, Ilse K Schaeffner, Matthew Q Deng, Blessing C Ogboo, Alexander Rasch, Tyler S Beyett, Brian Buckley, Frederic Feru, Tatiana Shaurova, Cornelius Knappe, Michael J Eck, Pamela A Hershberger, David A Scott, Stefan A Laufer, David E Heppner

Version 1 posted 26 September 2023

631

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1

Citations

Biological and Medicinal Chemistry

Review

Structural elements that enable specificity for mutant EGFR kinase domains with next-generation small-molecule inhibitors.

Tahereh Damghani, Florian Wittlinger, Tyler S. Beyett, Michael J. Eck, Stefan A. Laufer, David E. Heppner

Version 1 posted 14 February 2023

621

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Biological and Medicinal Chemistry

Working Paper

Molecular Design of a “Two-in-One” Orthosteric-Allosteric Chimeric Mutant Selective EGFR Inhibitor

Florian Wittlinger, David E. Heppner, Ciric To, Marcel Guenther, Bo Hee Shin, Jaimin K. Rana, Anna M. Schmoker, Tyler S. Beyett, Pasi A. Jänne, Michael J. Eck, Stefan Laufer

Version 1 posted 21 December 2020

1,015

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Biological and Medicinal Chemistry

Working Paper

Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors

Florian Wittlinger, Blessing C. Ogboo, Ekaterina Shevchenko, Tahereh Damghani, Calvin D. Pham, Ilse K. Schaeffner, Brandon T Oligny, Surbhi P. Chitnis, Tyler S. Beyett, Alexander Rasch, Brian Buckley, Daniel A. Urul, Tatiana Shaurova, Earl W. May, Erik M. Schaefer, Michael J. Eck, Pamela A. Hershberger, Antti Poso, Stefan A. Laufer, David E. Heppner

Version 2 posted 19 September 2023

841

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1

Citations

Biological and Medicinal Chemistry

Working Paper

Pitfalls and considerations in determining the potency and mutant selectivity of covalent epidermal growth factor receptor inhibitors

Kristopher W Hoyt, Daniel A Urul, Blessing C Ogboo, Florian Wittlinger, Stefan A Laufer, Erik M Schaefer, Earl W May, David E Heppner

Version 1 posted 24 August 2023

623

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Biological and Medicinal Chemistry

Working Paper

Structure-activity relationships of inactive-conformation binding EGFR inhibitors: Linking the ATP and allosteric pockets

Surbhi P. Chitnis, Florian Wittlinger, Mareike Möllers, Tyler J. Hartman, Marcel Günther, Michael J. Eck, Stefan A. Laufer, David E. Heppner

Version 1 posted 13 May 2025

78

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8 results in Florian Wittlinger in Authors: Florian Wittlinger

Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)

Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles

The origin of potency and mutant-selective inhibition by bivalent ATP-allosteric EGFR inhibitors

Structural elements that enable specificity for mutant EGFR kinase domains with next-generation small-molecule inhibitors.

Molecular Design of a “Two-in-One” Orthosteric-Allosteric Chimeric Mutant Selective EGFR Inhibitor

Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors

Pitfalls and considerations in determining the potency and mutant selectivity of covalent epidermal growth factor receptor inhibitors

Structure-activity relationships of inactive-conformation binding EGFR inhibitors: Linking the ATP and allosteric pockets

8 results in Authors: Florian Wittlinger