Can small molecule inhibitors of glutaminyl cyclase be used as a therapeutic for Alzheimer's disease?

Future Med Chem. 2017 Nov;9(17):1979-1981. doi: 10.4155/fmc-2017-0190. Epub 2017 Oct 27.

Abstract

Alzheimer's disease (AD) is a multifactorial and socioeconomically burdensome disease. In view of the failures of anti-AD candidates, we should try to rethink what we did before and what we should do next, in part at least. Research shows that the more neurotoxic factor, pyroglutamate-Aβs, and the more important inflammatory mediators, pyroglutamate-CCL2, both contribute to the initiation of AD specifically and the generation of N-terminal intramolecular cyclization catalyzed by glutaminyl cyclase quality control, the over-expression of which correlates positively with the severity of AD. Subsequently, lowering pyroglutamate-Aβs and pyroglutamate-CCL2 levels by quality control inhibition using small molecule inhibitors could be expected as an amazing strategy for the prevention and treatment of AD.

Keywords: Alzheimer's disease; glutaminyl cyclase; inhibitors.

Publication types

  • Editorial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / metabolism
  • Aminoacyltransferases / antagonists & inhibitors*
  • Aminoacyltransferases / metabolism
  • Biocatalysis
  • Humans
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*

Substances

  • Small Molecule Libraries
  • Aminoacyltransferases
  • glutaminyl-peptide cyclotransferase