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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

1,151

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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

957

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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

922

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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

351

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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

718

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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

535

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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

704

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1

Citations

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

669

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Biological and Medicinal Chemistry

Working Paper

Novel Small-Molecule Atypical Chemokine Receptor 3 (ACKR3) Agonists: Design, Synthesis, and Pharmacological Evaluation for Antiplatelet Therapy

Alp Bayrak, Martyna Szpakowska, Valerie Dicenta-Baunach, Manuel Counson, Alexander Rasch, Anne-Katrin Rohlfing, Andy Chevigné, Meinrad Gawaz, Stefan A. Laufer, Thanigaimalai Pillaiyar

Version 1 posted 19 June 2024

181

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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

403

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Refine Search

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

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

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

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

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

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.

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

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

Novel Small-Molecule Atypical Chemokine Receptor 3 (ACKR3) Agonists: Design, Synthesis, and Pharmacological Evaluation for Antiplatelet Therapy

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

13 results in Authors: Stefan A Laufer