Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay

Bioorg Med Chem Lett. 2000 Mar 20;10(6):559-62. doi: 10.1016/s0960-894x(00)00045-7.

Abstract

Several fluoresceinated FKBP12 ligands have been prepared for a high-throughput fluorescence polarization assay. K(i)s for FKBP12 rotamase inhibition by these ligands range from 1.3 microM to 32 nM, and their design is based on X-ray crystal structures of FKBP12 complexed with known immunophilin ligands.

MeSH terms

  • Crystallography, X-Ray
  • Fluorescein / chemistry
  • Fluorescence Polarization Immunoassay
  • Fluorescent Dyes / chemical synthesis*
  • Fluorescent Dyes / pharmacology
  • Immunophilins / chemistry*
  • Ligands
  • Protein Binding
  • Tacrolimus / metabolism
  • Tacrolimus Binding Proteins

Substances

  • Fluorescent Dyes
  • Ligands
  • Tacrolimus Binding Proteins
  • Immunophilins
  • Fluorescein
  • Tacrolimus