Fluorescent probes for retinoic acid receptors: molecular measures for the ligand binding pocket

Biochem Biophys Res Commun. 1991 Oct 15;180(1):249-54. doi: 10.1016/s0006-291x(05)81284-7.

Abstract

Two fluorescent probes for nuclear retinoic acid receptors (RARs) have been developed, both containing a biologically active retinoid moiety and a fluorescent dansyl moiety, but differing in the length of the spacer arm connecting the two moieties. Both probes bind RARs at their retinoid-binding sites, revealing the usefulness of the compounds as fluorescent RAR probes. By measuring the specific increase of the probes' fluorescence intensity caused by the binding to RARs, the linearized length of the RAR's retinoid-binding pocket could be estimated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding, Competitive
  • Carrier Proteins / chemistry*
  • Dansyl Compounds / chemical synthesis
  • Fluorescence
  • Fluorescent Dyes* / chemical synthesis
  • HeLa Cells / metabolism
  • Humans
  • Ligands
  • Receptors, Retinoic Acid
  • Tetrahydronaphthalenes / chemical synthesis
  • Tretinoin / chemistry*

Substances

  • Carrier Proteins
  • Dansyl Compounds
  • Fluorescent Dyes
  • Ligands
  • Receptors, Retinoic Acid
  • Tetrahydronaphthalenes
  • 2-(3-(5-dimethylaminonaphthalene-1-sulfonyl)aminopropyl-1-oxyl)-4-((5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carboxamido)benzoic acid
  • 2-(aminopropyl-1-oxyl)-4-((5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carboxamido)benzoic acid
  • Tretinoin