Selection of a human butyrylcholinesterase-like antibody single-chain variable fragment resistant to AChE inhibitors from a phage library expressed in E. coli

MAbs. 2014 Jul-Aug;6(4):1084-93. doi: 10.4161/mabs.28635.

Abstract

Organophosphates are potent poisoning agents that cause severe cholinergic toxicity. Current treatment has been reported to be unsatisfactory and novel antidotes are needed. In this study, we used a single-chain variable fragment (scFv) library to select a recombinant antibody fragment (WZ1-14.2.1) with butyrylcholinesterase-like catalytic activity by using an innovative method integrating genetic selection and the bait-and-switch strategy. Ellman assay demonstrated that WZ1-14.2.1 has Michaelis-Menten kinetics in the hydrolysis of all the three substrates used, acetylthiocholine, propionylthiocholine and butyrylthiocholine. Notably, the catalytic activity was resistant to the following acetylcholinesterase inhibitors: neostigmine, iso-OMPA, chlorpyrifos oxon, dichlorvos, and paraoxon ethyl. Otherwise, the enzymatic activity of WZ1-14.2.1 was inhibited by the selective butyrylcholinesterase inhibitor, ethopropazine, and by the Ser-blocking agent phenylmethanesuphonyl fluoride. A hypothetical 3D structure of the WZ1-14.2.1 catalytic site, compatible with functional results, is proposed on the basis of a molecular modeling analysis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Butyrylcholinesterase / chemistry*
  • Butyrylcholinesterase / genetics
  • Butyrylcholinesterase / immunology
  • Cholinesterase Inhibitors / chemistry*
  • Escherichia coli*
  • Gene Expression*
  • Gene Library*
  • Humans
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / genetics
  • Recombinant Proteins / immunology
  • Single-Chain Antibodies* / biosynthesis
  • Single-Chain Antibodies* / chemistry
  • Single-Chain Antibodies* / genetics
  • Single-Chain Antibodies* / immunology

Substances

  • Cholinesterase Inhibitors
  • Recombinant Proteins
  • Single-Chain Antibodies
  • Butyrylcholinesterase