Penalver, Lilian; Schmid, Philipp; Szamosvari, David; Schildknecht, Stefan; Globisch, Christoph; Sawade, Kevin; Peter, Christine; Boettcher, Thomas published the artcile< A ligand selection strategy identifies chemical probes targeting the proteases of SARS-CoV-2>, Synthetic Route of 324579-90-0, the main research area is ligand selection strategy probe targeting protease SARS CoV2; COVID19 SARS CoV2 protease 3CLpro PLpro labeling inhibitor; ABPP; chemical probes; enzyme inhibitors; labeling; proteases.
Activity-based probes are valuable tools for chem. biol. However, finding probes that specifically target the active site of an enzyme remains a challenging task. Herein, we present a ligand selection strategy that allows to rapidly tailor electrophilic probes to a target of choice and showcase its application for the two cysteine proteases of SARS-CoV-2 as proof of concept. The resulting probes were specific for the active site labeling of 3CLpro and PLpro with sufficient selectivity in a live cell model as well as in the background of a native human proteome. Exploiting the probes as tools for competitive profiling of a natural product library identified salvianolic acid derivatives as promising 3CLpro inhibitors. We anticipate that our ligand selection strategy will be useful to rapidly develop customized probes and discover inhibitors for a wide range of target proteins also beyond corona virus proteases.
Angewandte Chemie, International Editionpublished new progress about Alkynyl groups (in enzyme probe). 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Synthetic Route of 324579-90-0.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica