Selective covalent targeting of SARS-CoV-2 main protease by enantiopure chlorofluoroacetamide
Daiki Yamane, Satsuki Onitsuka, Suyong Re, Hikaru Isogai, Rui Hamada, Tadanari Hiramoto, Eiji Kawanishi, Kenji Mizuguchi, Naoya Shindo, Akio Ojida
Abstract
. Our findings highlight the prominent influence of the CFA chirality on the covalent modification of proteinous cysteines and provide the basis for improving the potency and selectivity of CFA-based covalent inhibitors.
Topics & Concepts
Enantiopure drugProteaseSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2)Coronavirus disease 2019 (COVID-19)ChemistryCovalent bondVirology2019-20 coronavirus outbreakCombinatorial chemistryBiologyEnzymeMedicineBiochemistryOrganic chemistryInternal medicineEnantioselective synthesisCatalysisInfectious disease (medical specialty)OutbreakDiseaseComputational Drug Discovery MethodsSynthesis and biological activityClick Chemistry and Applications