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Cathepsin-Targeting SARS-CoV-2 Inhibitors: Design, Synthesis, and Biological Activity

Philipp Flury, Julian Breidenbach, Nadine Krüger, Rabea Voget, Laura Schäkel, Yaoyao Si, Vesa Krasniqi, Sara Calistri, Matthias Olfert, Katharina Sylvester, Cheila Rocha, Raphael Ditzinger, Alexander Rasch, Stefan Pöhlmann, Thales Kronenberger, Antti Poso, Katharina Rox, Stefan A. Laufer, Christa E. Müller, Michael Gütschow, Thanigaimalai Pillaiyar

Version 1 posted 07 November 2023

323

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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

1,253

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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

932

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Biological and Medicinal Chemistry

Working Paper

SARS-CoV-2 Mutations in Brazil: From Genomics to Clinical Conditions

Luis Timmers, Julia Peixoto, Rodrigo Ducati, Jose Fernando Bachega, Leandro Mattos Pereira, Rafael Andrade Caceres, Fernanda Majolo, Guilherme Liberato Da Silva, Debora Bublitz Anton, Marcia Inês Goettert, Odir Antônio Dellagostin, Joao Henriques, Leder Xavier, Stefan Laufer

Version 1 posted 19 February 2021

719

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1

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Biological and Medicinal Chemistry

Working Paper

Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

Ricardo Serafim, André Santiago, Caio dos Reis, Jessica Takarada, Priscila Mezzomo, Katlin Massirer, Martin P. Schwalm, Mark Kudolo, Stefan Gerstenecker, Apirat Chaikuad, Stefan Knapp, Stefan Laufer, Rafael Counago, Matthias Gehringer

Version 1 posted 20 May 2021

977

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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

443

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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

535

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1

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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

695

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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

744

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1

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Biological and Medicinal Chemistry

Working Paper

Discovery of a Potent and Highly Isoform-Selective Inhibitor of the Neglected Ribosomal Protein S6 Kinase Beta 2 (S6K2)

Stefan Gerstenecker, Lisa Haarer, Martin Schröder, Mark Kudolo, Martin P. Schwalm, Valentin Wydra, Ricardo Serafim, Apirat Chaikuad, Stefan Knapp, Stefan Laufer, Matthias Gehringer

Version 1 posted 15 July 2021

363

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13 results in Stefan A. Laufer in Authors: Stefan A. Laufer

Cathepsin-Targeting SARS-CoV-2 Inhibitors: Design, Synthesis, and Biological Activity

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

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

SARS-CoV-2 Mutations in Brazil: From Genomics to Clinical Conditions

Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

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

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

Discovery of a Potent and Highly Isoform-Selective Inhibitor of the Neglected Ribosomal Protein S6 Kinase Beta 2 (S6K2)

13 results in Authors: Stefan A. Laufer