Lategahn, Jonas published the artcileInhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S, Name: 3-(Methylthio)propan-1-ol, the main research area is nonsmall cell lung cancer osimertinib EGFR drug resistance.
Precision medicine has revolutionized the treatment of patients in EGFR driven non-small cell lung cancer (NSCLC). Targeted drugs show high response rates in genetically defined subsets of cancer patients and markedly increase their progression-free survival as compared to conventional chemotherapy. However, recurrent acquired drug resistance limits the success of targeted drugs in long-term treatment and requires the constant development of novel efficient inhibitors of drug resistant cancer subtypes. Herein, we present covalent inhibitors of the drug resistant gatekeeper mutant EGFR-L858R/T790M based on the pyrrolopyrimidine scaffold. Biochem. and cellular characterization, as well as kinase selectivity profiling and western blot anal., substantiate our approach. Moreover, the developed compounds possess high activity against multi drug resistant EGFR-L858R/T790M/C797S in biochem. assays due to their highly reversible binding character, that was revealed by characterization of the binding kinetics. In addition, we present the first x-ray crystal structures of covalent inhibitors in complex with C797S-mutated EGFR which provide detailed insight into their binding mode.
Chemical Science published new progress about Bioavailability. 505-10-2 belongs to class alcohols-buliding-blocks, name is 3-(Methylthio)propan-1-ol, and the molecular formula is C4H10OS, Name: 3-(Methylthio)propan-1-ol.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts