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6 results in Authors: David Heppner

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

918

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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

489

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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

392

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Biological and Medicinal Chemistry

Working Paper

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

666

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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

713

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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

529

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6 results in David Heppner in Authors: David Heppner

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

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

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

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

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

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

6 results in Authors: David Heppner