Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments.

ABSTRACT: Sulfur(VI) fluorides (SFs) have emerged as valuable electrophiles for the design of "beyond-cysteine" covalent inhibitors and offer potential for expansion of the liganded proteome. Since SFs target a broad range of nucleophilic amino acids, they deliver an approach for the covalent modification of proteins without requirement for a proximal cysteine residue. Further to this, libraries of reactive fragments present an innovative approach for the discovery of ligands and tools for proteins of interest by leveraging a breadth of mass spectrometry analytical approaches. Herein, we report a screening approach that exploits the unique properties of SFs for this purpose. Libraries of SF-containing reactive fragments were synthesized, and a direct-to-biology workflow was taken to efficiently iden

SUBMITTER: Aatkar A 

PROVIDER: S-EPMC10510102 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature