Judit E. Debreczeni

TL;DR: A novel series of small-molecule inhibitors developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with gefitinib and erlotinib, demonstrates high levels of activity and shows selectivity over wild-type EGFR.

TL;DR: This compound demonstrated good preclinical drug metabolism and pharmacokinetics (DMPK) properties and, after oral dosing, showed pharmacodynamic knockdown of phosphorylation of Akt and downstream biomarkers in vivo, and inhibition of tumor growth in a breast cancer xenograft model.

TL;DR: Coot is a molecular-graphics program designed to assist in the building of protein and other macromolecular models and the current state of ligand tools is presented.

TL;DR: DARPin K27 is a potent, non-covalent inhibitor of nucleotide exchange, showing consistent effects across different isoforms of Ras, including wild-type and oncogenic mutant forms.

TL;DR: Multiple series of highly selective covalent ERK1/2 inhibitors informed by structure-based drug design (SBDD) are identified for potential in vitro and in vivo studies to assess the risks and or benefits of targeting this pathway through such a mechanism of action.