Julia Hardick
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View article: Optimization of Covalent MKK7 Inhibitors <i>via</i> Crude Nanomole-Scale Libraries
Optimization of Covalent MKK7 Inhibitors <i>via</i> Crude Nanomole-Scale Libraries Open
High-throughput nanomole-scale synthesis allows for late-stage functionalization (LSF) of compounds in an efficient and economical manner. Here, we demonstrated that copper-catalyzed azide-alkyne cycloaddition could be used for the LSF of …
View article: Targeting Her2-insYVMA with Covalent Inhibitors—A Focused Compound Screening and Structure-Based Design Approach
Targeting Her2-insYVMA with Covalent Inhibitors—A Focused Compound Screening and Structure-Based Design Approach Open
Mutated or amplified Her2 serves as a driver of non-small cell lung cancer or mediates resistance toward the inhibition of its family member epidermal growth factor receptor with small-molecule inhibitors. To date, small-molecule inhibitor…
View article: CCDC 1876852: Experimental Crystal Structure Determination
CCDC 1876852: Experimental Crystal Structure Determination Open
View article: Targeting the MKK7–JNK (Mitogen-Activated Protein Kinase Kinase 7–c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors
Targeting the MKK7–JNK (Mitogen-Activated Protein Kinase Kinase 7–c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors Open
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 for the dissection of its detailed functions. Against this background, we describe…
View article: Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S
Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S Open
We present inhibitors of drug resistant mutants of EGFR including T790M and C797S. In addition, we present the first X-ray crystal structures of covalent inhibitors in complex with C797S-mutated EGFR to gain insight into their binding mode.
View article: Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt
Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt Open
Structure-based driven synthesis and biological evaluation provide innovative novel covalent-allosteric Akt inhibitors.
View article: Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT Open
In modern cancer therapy, the use of small organic molecules against receptor tyrosine kinases (RTKs) has been shown to be a valuable strategy. The association of cancer cells with dysregulated signaling pathways linked to RTKs represents …
View article: Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK
Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK Open
In protein kinase research, identifying and addressing small molecule binding sites other than the highly conserved ATP-pocket are of intense interest because this line of investigation extends our understanding of kinase function beyond t…