Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in <i>KRAS</i>-Mutant Pancreatic and Colorectal Cancer

Jörn Weisner, Ina Landel, Christoph Reintjes, +28

Cancer Research

Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt

Niklas Uhlenbrock, Steven P. Smith, Jörn Weisner, +13

Chemical Science

Molecular BiologyChemical BiologyPharmaceutical ChemistryMolecular PharmacologyMedicinal Chemistry +16

Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S

Jonas Lategahn, Marina Keul, Philip Klövekorn, +26

Chemical Science

Targeting the MKK7–JNK (Mitogen-Activated Protein Kinase Kinase 7–c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors

Patrik Wolle, Julia Hardick, Shane J. F. Cronin, +5

Journal of Medicinal Chemistry

Covalent InhibitorsDrug TargetEffective Covalent InhibitorMolecular PharmacologyMedicinal Chemistry +15

Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants

Mike Bührmann, Julia Hardick, Jörn Weisner, +2

Angewandte Chemie International Edition

Targeting Her2-insYVMA with Covalent Inhibitors—A Focused Compound Screening and Structure-Based Design Approach

Jonas Lategahn, Julia Hardick, Tobias Grabe, +17

Journal of Medicinal Chemistry

Molecular BiologyChemical BiologyPharmaceutical ChemistryCovalent Inhibitors—aMedicinal Chemistry +17

Optimization of Covalent MKK7 Inhibitors <i>via</i> Crude Nanomole-Scale Libraries

Paul Gehrtz, Shir Marom, Mike Bührmann, +15

Journal of Medicinal Chemistry

Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK

Mike Bührmann, Bianca Wiedemann, Matthias Müller, +3

PLoS ONE

Drug TargetLipid Pocket LigandsProtein Kinase ResearchOrganic ChemistryChemistry +20

Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT

Helena Kaitsiotou, Marina Keul, Julia Hardick, +9

Journal of Medicinal Chemistry

Tumor BiologyReceptor Tyrosine KinaseOvercome Secondary MutationsRelevant RtkAnti-cancer Agent +15