Regulation of the cellular machinery requires both cleavage and transfer of phosphate bonds by ATPases, G-proteins, kinases, and polymerases. By replacing the 5'-triphosphate moieties of ATP and GTP for electrophilic 4-fluorosulfonylbenzoyl (FSB) residues, the corresponding analogs FSBA and FSBG have been devised as
Furthermore, recent advances in the field of SuFEx-Chemistry allow us to access numerous sulfonyl fluoride motifs. Please inquire for structures.
Scheme 1: A) The structures of FSBA and FSBG with the reactive sulfonyl fluoride moieties highlighted in blue. B) Sulfonyl fluorides are molecular warheads with sufficient stability in aqueous solution under physiological conditions. When exposed to an activated nucleophile such as serine, threonine, lysine, tyrosine or histidine at the active site of a target enzyme, covalent adducts are formed, permitting the context-specific probing of functionally important residues.
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