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Biological and Medicinal Chemistry

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David E Heppner

6 results in Authors: David E Heppner

Biological and Medicinal Chemistry

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

1,019

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Biological and Medicinal Chemistry

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

639

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1

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Biological and Medicinal Chemistry

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

858

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1

Citations

Biological and Medicinal Chemistry

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

665

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Biological and Medicinal Chemistry

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

629

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Biological and Medicinal Chemistry

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

106

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