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Combinatorially Screened Peptide as Targeted Covalent Binder: Alteration of Bait-Conjugated Peptide to Reactive Modifier.

Shuta UematsuYudai TabuchiYuji ItoMasumi Taki
Published in: Bioconjugate chemistry (2018)
A peptide-type covalent binder for a target protein was obtained by combinatorial screening of fluoroprobe-conjugated peptide libraries on bacteriophage T7. The solvatochromic fluoroprobe works as a bait during the affinity selection process of phage display. To obtain the targeted covalent binder, the bait in the selected consensus peptide was altered into a reactive warhead possessing a sulfonyl fluoride. The reaction efficiency and site/position specificity of the covalent conjugation between the binder and the target protein were evaluated by liquid chromatography-tandem mass spectrometry (LC-MS/MS), and rationalized by a protein-ligand docking simulation.
Keyphrases
  • liquid chromatography tandem mass spectrometry
  • protein protein
  • cancer therapy
  • simultaneous determination
  • molecular dynamics
  • drinking water
  • solid phase extraction
  • clinical practice