Review of human butyrylcholinesterase structure, function, genetic variants, history of use in the clinic, and potential therapeutic uses

Pharmacol Ther. 2015 Apr:148:34-46. doi: 10.1016/j.pharmthera.2014.11.011. Epub 2014 Nov 20.

Abstract

Phase I clinical trials have shown that pure human butyrylcholinesterase (BChE) is safe when administered to humans. A potential therapeutic use of BChE is for prevention of nerve agent toxicity. A recombinant mutant of BChE that rapidly inactivates cocaine is being developed as a treatment to help recovering cocaine addicts avoid relapse into drug taking. These clinical applications rely on knowledge of the structure, stability, and properties of BChE, information that is reviewed here. Gene therapy with a vector that sustains expression for a year from a single injection is a promising method for delivering therapeutic quantities of BChE.

Keywords: Butyrylcholinesterase; Clinical use; Cocaine; Genetic variants; Nerve agent.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Butyrylcholinesterase* / chemistry
  • Butyrylcholinesterase* / genetics
  • Butyrylcholinesterase* / metabolism
  • Butyrylcholinesterase* / therapeutic use
  • Cocaine-Related Disorders / drug therapy
  • Genetic Variation
  • Humans
  • Nerve Agents / toxicity
  • Protein Conformation

Substances

  • Nerve Agents
  • Butyrylcholinesterase