Synthesis of novel fluorescent probes for the molecular chaperone Hsp90

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3975-8. doi: 10.1016/j.bmcl.2003.08.065.

Abstract

Heat shock protein 90 (Hsp90) is a molecular chaperone necessary for maintaining oncogenic transformation. There is substantial interest in developing novel agents that bind to the N-terminal of the chaperone. Here we report the synthesis and characterization of two fluorescent Hsp90 inhibitors and probe their use in an Hsp90 fluorescent polarization assay.

Publication types

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

MeSH terms

  • Binding, Competitive
  • Fluorescent Dyes / chemical synthesis*
  • Fluorescent Dyes / pharmacology
  • HSP90 Heat-Shock Proteins / chemistry*
  • HSP90 Heat-Shock Proteins / drug effects
  • Kinetics
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Fluorescent Dyes
  • HSP90 Heat-Shock Proteins