Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach

Julian Engel, André Richters, Matthäus Getlik, +24

Journal of Medicinal Chemistry

Covalent InhibitorsDrug TargetMolecular BiologyChemical BiologyDrug Resistance +20

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

Marcel Günther, Jonas Lategahn, Michael Juchum, +6

Journal of Medicinal Chemistry

Drug TargetBoth Hydrophobic RegionsChemical BiologyMutant Egfr InhibitionPharmaceutical Chemistry +19

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer

Julian Engel, Jonas Lategahn, Daniel Rauh

ACS Medicinal Chemistry Letters

Covalent InhibitorsPharmacotherapyTumor BiologyDrug ResistanceAnti-cancer Agent +15

Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors

Dennis Plenker, M Riedel, Johannes Brägelmann, +32

Science Translational Medicine

Insight into the Inhibition of Drug‐Resistant Mutants of the Receptor Tyrosine Kinase EGFR

Julian Engel, Christian Becker, Jonas Lategahn, +8

Angewandte Chemie International Edition

Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34

Lucas Robke, Luca Laraia, Marjorie A. Carnero Corrales, +12

Angewandte Chemie International Edition

Cell AutophagyMitophagyPotent Autophagy InhibitorSignal TransductionPhenotypic Identification +13

Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor

Stefano Tomassi, Jonas Lategahn, Julian Engel, +8

Journal of Medicinal Chemistry

Drug TargetPharmacotherapyDermatologyTumor BiologyMedicinal Chemistry +14

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

Jonas Lategahn, Marina Keul, Philip Klövekorn, +26

Chemical Science

Identification of Type II and III DDR2 Inhibitors

André Richters, Hoang Duc Nguyen, Trang Thi Phuong Phan, +4

Journal of Medicinal Chemistry

Type IiSignal TransductionSignaling PathwayMedicineReceptor Tyrosine Kinase +11

Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor

Julian Engel, Steven P. Smith, Jonas Lategahn, +12

Journal of Medicinal Chemistry

Drug TargetMolecular BiologyDrug ResistanceMutant-selective PyrazolopyrimidinesAnti-cancer Agent +15