Laufer SA - Search Results

1

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

Wittlinger F, Ogboo BC, Shevchenko E, Damghani T, Pham CD, Schaeffner IK, Oligny BT, Chitnis SP, Beyett TS, Rasch A, Buckley B, Urul DA, Shaurova T, May EW, Schaefer EM, Eck MJ, Hershberger PA, Poso A, Laufer SA, Heppner DE. Wittlinger F, et al. Among authors: laufer sa. Commun Chem. 2024 Feb 20;7(1):38. doi: 10.1038/s42004-024-01108-3. Commun Chem. 2024. PMID: 38378740 Free PMC article.

2

Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity.

Fischer S, Wentsch HK, Mayer-Wrangowski SC, Zimmermann M, Bauer SM, Storch K, Niess R, Koeberle SC, Grütter C, Boeckler FM, Rauh D, Laufer SA. Fischer S, et al. Among authors: laufer sa. J Med Chem. 2013 Jan 10;56(1):241-53. doi: 10.1021/jm301539x. Epub 2012 Dec 27. J Med Chem. 2013. PMID: 23270382

3

Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.

Juchum M, Günther M, Döring E, Sievers-Engler A, Lämmerhofer M, Laufer S. Juchum M, et al. J Med Chem. 2017 Jun 8;60(11):4636-4656. doi: 10.1021/acs.jmedchem.7b00178. Epub 2017 May 23. J Med Chem. 2017. PMID: 28482151

4

Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.

Günther M, Lategahn J, Juchum M, Döring E, Keul M, Engel J, Tumbrink HL, Rauh D, Laufer S. Günther M, et al. J Med Chem. 2017 Jul 13;60(13):5613-5637. doi: 10.1021/acs.jmedchem.7b00316. Epub 2017 Jun 21. J Med Chem. 2017. PMID: 28603991

5

Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors.

Heider F, Ansideri F, Tesch R, Pantsar T, Haun U, Döring E, Kudolo M, Poso A, Albrecht W, Laufer SA, Koch P. Heider F, et al. Among authors: laufer sa. Eur J Med Chem. 2019 Aug 1;175:309-329. doi: 10.1016/j.ejmech.2019.04.035. Epub 2019 Apr 24. Eur J Med Chem. 2019. PMID: 31096153

6

Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.

Heppner DE, Günther M, Wittlinger F, Laufer SA, Eck MJ. Heppner DE, et al. Among authors: laufer sa. J Med Chem. 2020 Apr 23;63(8):4293-4305. doi: 10.1021/acs.jmedchem.0c00200. Epub 2020 Apr 14. J Med Chem. 2020. PMID: 32243152 Free PMC article.

7

The pre-clinical discovery and development of osimertinib used to treat non-small cell lung cancer.

Wittlinger F, Laufer SA. Wittlinger F, et al. Among authors: laufer sa. Expert Opin Drug Discov. 2021 Oct;16(10):1091-1103. doi: 10.1080/17460441.2021.1936496. Epub 2021 Jun 20. Expert Opin Drug Discov. 2021. PMID: 34053372

8

Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.

Wittlinger F, Heppner DE, To C, Günther M, Shin BH, Rana JK, Schmoker AM, Beyett TS, Berger LM, Berger BT, Bauer N, Vasta JD, Corona CR, Robers MB, Knapp S, Jänne PA, Eck MJ, Laufer SA. Wittlinger F, et al. Among authors: laufer sa. J Med Chem. 2022 Jan 27;65(2):1370-1383. doi: 10.1021/acs.jmedchem.1c00848. Epub 2021 Oct 20. J Med Chem. 2022. PMID: 34668706 Free PMC article.

9

Decisive role of water and protein dynamics in residence time of p38α MAP kinase inhibitors.

Pantsar T, Kaiser PD, Kudolo M, Forster M, Rothbauer U, Laufer SA. Pantsar T, et al. Among authors: laufer sa. Nat Commun. 2022 Jan 28;13(1):569. doi: 10.1038/s41467-022-28164-4. Nat Commun. 2022. PMID: 35091547 Free PMC article.

10

Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination.

Pillaiyar T, Flury P, Krüger N, Su H, Schäkel L, Barbosa Da Silva E, Eppler O, Kronenberger T, Nie T, Luedtke S, Rocha C, Sylvester K, Petry MRI, McKerrow JH, Poso A, Pöhlmann S, Gütschow M, O'Donoghue AJ, Xu Y, Müller CE, Laufer SA. Pillaiyar T, et al. Among authors: laufer sa. J Med Chem. 2022 Jul 14;65(13):9376-9395. doi: 10.1021/acs.jmedchem.2c00636. Epub 2022 Jun 16. J Med Chem. 2022. PMID: 35709506

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