Multiplexed Thiol Reactivity Profiling for Target Discovery of Electrophilic Natural Products.
Sign Up to like & getrecommendations! Published in 2017 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2017.08.022
Abstract: Electrophilic groups, such as Michael acceptors, expoxides, are common motifs in natural products (NPs). Electrophilic NPs can act through covalent modification of cysteinyl thiols on functional proteins, and exhibit potent cytotoxicity and anti-inflammatory/cancer activities. Here… read more here.
Keywords: reactivity profiling; target; discovery; reactivity ... See more keywords
Masking thiol reactivity with thioamide, thiourea, and thiocarbamate-based MBPs.
Sign Up to like & getrecommendations! Published in 2023 at "Chemical communications"
DOI: 10.1039/d2cc06596g
Abstract: Thioamides, thioureas, and thiocarbamates are introduced as stable, sulfur-based metal-binding pharmacophores (MBPs) for use in metalloenzyme fragment-based drug discovery (mFBDD). MBP reactivity, bioactivity, and structural studies show that these molecules can act as ligands for… read more here.
Keywords: thiourea thiocarbamate; thiol reactivity; thioamide thiourea; masking thiol ... See more keywords