Disease-associated acrolein: A possible diagnostic and therapeutic substrate for in vivo synthetic chemistry

Bioorg Med Chem. 2020 Dec 15;28(24):115831. doi: 10.1016/j.bmc.2020.115831. Epub 2020 Oct 31.


Acrolein, a highly reactive α,β-unsaturated aldehyde, is a compound to which humans are exposed in many different situations and often causes various human diseases. This paper summarizes the reports over the past twenty-five years regarding disease-associated acrolein detected in clinical patients and the role acrolein plays in various diseases. In several diseases, it was found that the increased acrolein acts as a pathogenetic factor. Thus, we propose the utility of over-produced acrolein as a substrate for a promising therapeutic or diagnostic method applicable to a wide range of diseases based on an in vivo synthetic chemistry strategy.

Keywords: Acrolein; Diagnosis; Disease-associated substrate; In vivo synthetic chemistry; Therapy.

Publication types

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

MeSH terms

  • Acrolein / analysis
  • Acrolein / chemistry*
  • Acrolein / metabolism
  • Alzheimer Disease / diagnosis*
  • Alzheimer Disease / pathology
  • Alzheimer Disease / therapy
  • Autoimmune Diseases / diagnosis*
  • Autoimmune Diseases / therapy
  • Brain Diseases / diagnosis*
  • Brain Diseases / therapy
  • Humans
  • Lysine / analogs & derivatives
  • Lysine / blood
  • Lysine / cerebrospinal fluid
  • Lysine / chemistry
  • Lysine / urine
  • Polyamines / chemistry
  • Proteins / chemistry


  • N(epsilon)-(3-formyl-3,4-dihydropiperidino)lysine
  • Polyamines
  • Proteins
  • Acrolein
  • Lysine