Discovery of selective aldo-keto reductase ligands--an on-bead assay strategy

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2938-42. doi: 10.1016/j.bmcl.2005.03.010.

Abstract

An enzyme labeling and screening strategy for the discovery of ligands selective in binding two structurally similar members of the aldo-keto reductase family of enzymes is reported. The resulting fluorescence microscope data obtained by screening a 74,088 member library led to the identification of selective ligands for aldose reductase (ALR2) and aldehyde reductase (ALR1). Resynthesis results validate the selectivity of these ligands.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alcohol Oxidoreductases / chemistry
  • Alcohol Oxidoreductases / metabolism*
  • Aldehyde Reductase / metabolism
  • Aldo-Keto Reductases
  • Ligands
  • Microscopy, Fluorescence
  • Models, Molecular

Substances

  • Ligands
  • Alcohol Oxidoreductases
  • Aldo-Keto Reductases
  • Aldehyde Reductase