Search Results - "Lategahn, Jonas"
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Organocatalytic, Oxidative, Intramolecular CH Bond Amination and Metal-free Cross-Amination of Unactivated Arenes at Ambient Temperature
Published in Angewandte Chemie International Edition (05-09-2011)“…The twinkling of an I: In a new atom‐economical and environmentally friendly organocatalytic method for intramolecular CH amination, the CN bond forms at…”
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2
Metal-free direct oxidative intermolecular diarylation of anilides at ambient temperature assisted by cascade selective formation of C-C and C-N bonds
Published in Chemical communications (Cambridge, England) (01-01-2012)“…A new atom-economical process of direct oxidative intermolecular functionalization of aniline derivatives by simple arenes was developed. The products were…”
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Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site
Published in Journal of medicinal chemistry (13-07-2017)“…Inhibition of the epidermal growth factor receptor represents one of the most promising strategies in the treatment of lung cancer. Acquired resistance…”
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Resistance to Avapritinib in PDGFRA-Driven GIST Is Caused by Secondary Mutations in the PDGFRA Kinase Domain
Published in Cancer discovery (01-01-2021)“…Gastrointestinal stromal tumors (GIST) harboring activating mutations of respond to imatinib, with the notable exception of the most common mutation, D842V…”
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5
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor
Published in Journal of medicinal chemistry (23-03-2017)“…The specific targeting of oncogenic mutant epidermal growth factor receptor (EGFR) is a breakthrough in targeted cancer therapy and marks a drastic change in…”
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A novel scaffold for EGFR inhibition: Introducing N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives
Published in Scientific reports (09-01-2019)“…Clinical data acquired over the last decade on non-small cell lung cancer (NSCLC) treatment with small molecular weight Epidermal Growth Factor Receptor (EGFR)…”
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Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
Published in Nature communications (07-11-2018)“…The emergence of acquired resistance against targeted drugs remains a major clinical challenge in lung adenocarcinoma patients. In a subgroup of these patients…”
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Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
Published in Nature communications (01-11-2018)“…The emergence of acquired resistance against targeted drugs remains a major clinical challenge in lung adenocarcinoma patients. In a subgroup of these patients…”
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Lessons To Be Learned: The Molecular Basis of Kinase‐Targeted Therapies and Drug Resistance in Non‐Small Cell Lung Cancer
Published in Angewandte Chemie International Edition (23-02-2018)“…The treatment of non‐small cell lung cancer (NSCLC) is currently experiencing a revolution. Over the last decade, the knowledge gained about the biochemical…”
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C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer?
Published in ACS medicinal chemistry letters (09-08-2018)“…The first evidence of osimertinib resistance mediated by the epidermal growth factor receptor (EGFR) mutation C797S was reported three years ago. Since then,…”
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Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer
Published in ACS medicinal chemistry letters (14-01-2016)“…In the last five years, the detailed understanding of how to overcome T790M drug resistance in non-small cell lung cancer (NSCLC) has culminated in the…”
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12
Organokatalytische, oxidative, intramolekulare C‐H‐Bindungsaminierung und metallfreie Kreuzaminierung nichtaktivierter Arene bei Raumtemperatur
Published in Angewandte Chemie (05-09-2011)“…Metallfrei: Eine atomökonomische, umweltverträgliche und organokatalytische Methode zur intramolekularen C‐H‐Aminierung wurde entwickelt. Die Bildung der…”
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Structure Defines Function: Clinically Relevant Mutations in ErbB Kinases
Published in Journal of medicinal chemistry (09-01-2020)“…The ErbB receptor tyrosine kinase family members EGFR (epidermal growth factor receptor) and Her2 are among the prominent mutated oncogenic drivers of…”
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Structure Defines Function: Clinically Relevant Mutations in ErbB Kinases: Miniperspective
Published in Journal of medicinal chemistry (09-01-2020)“…The ErbB receptor tyrosine kinase family members EGFR (epidermal growth factor receptor) and Her2 are among the prominent mutated oncogenic drivers of…”
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15
Characterization of Covalent Pyrazolopyrimidine–MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7)
Published in Journal of medicinal chemistry (13-06-2019)“…Pyrazolopyrimidines are well-established as covalent inhibitors of protein kinases such as the epidermal growth factor receptor or Bruton’s tyrosine kinase,…”
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Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR
Published in Angewandte Chemie International Edition (26-08-2016)“…Targeting acquired drug resistance represents the major challenge in the treatment of EGFR‐driven non‐small‐cell lung cancer (NSCLC). Herein, we describe the…”
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Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands
Published in ACS medicinal chemistry letters (10-12-2020)“…Osimertinib is a third-generation tyrosine kinase inhibitor (TKI) and currently the gold-standard for the treatment of patients suffering from non-small cell…”
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Targeting the MKK7–JNK (Mitogen-Activated Protein Kinase Kinase 7–c-Jun N‑Terminal Kinase) Pathway with Covalent Inhibitors
Published in Journal of medicinal chemistry (14-03-2019)“…The protein kinase MKK7 is linked to neuronal development and the onset of cancer. The field, however, lacks high-quality functional probes that would allow…”
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Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach
Published in Journal of medicinal chemistry (10-09-2015)“…Receptor tyrosine kinases represent one of the prime targets in cancer therapy, as the dysregulation of these elementary transducers of extracellular signals,…”
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KIT ATP-Binding Pocket/Activation Loop Mutations in GI Stromal Tumor: Emerging Mechanisms of Kinase Inhibitor Escape
Published in Journal of clinical oncology (20-04-2024)“…Imatinib resistance in GI stromal tumors (GISTs) is primarily caused by secondary mutations, and clonal heterogeneity of these secondary mutations represents a…”
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