Ontology highlight
ABSTRACT:
SUBMITTER: Zambaldo C
PROVIDER: S-EPMC7365253 | biostudies-literature | 2020 May
REPOSITORIES: biostudies-literature
Zambaldo Claudio C Vinogradova Ekaterina V EV Qi Xiaotian X Iaconelli Jonathan J Suciu Radu M RM Koh Minseob M Senkane Kristine K Chadwick Stormi R SR Sanchez Brittany B BB Chen Jason S JS Chatterjee Arnab K AK Liu Peng P Schultz Peter G PG Cravatt Benjamin F BF Bollong Michael J MJ
Journal of the American Chemical Society 20200429 19
The emerging use of covalent ligands as chemical probes and drugs would benefit from an expanded repertoire of cysteine-reactive electrophiles for efficient and diverse targeting of the proteome. Here we use the endogenous electrophile sensor of mammalian cells, the KEAP1-NRF2 pathway, to discover cysteine-reactive electrophilic fragments from a reporter-based screen for NRF2 activation. This strategy identified a series of 2-sulfonylpyridines that selectively react with biological thiols via nu ...[more]