Expression of retinoic acid receptor genes and the ligand-binding selectivity of retinoic acid receptors (RAR's)

Biochem Biophys Res Commun. 1990 Feb 14;166(3):1300-7. doi: 10.1016/0006-291x(90)91007-f.

Abstract

Retinoids of a structurally new type, 4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenylcarbamoyl)benzoic acid (Am80) and (E)-4-[3-(3,5-di-tert-butylphenyl)-3-oxo-1-propenyl]-benzoic acid (Ch55), were used for the investigation of retinoid receptors in some human cell lines. Previously, using these retinoids, we have established that HL-60 cells possess two retinoid receptors, RAR-alpha and RAR-beta. In this paper, we report coexpression of RAR-alpha- and RAR-beta-genes established by Northern analysis. Further, the binding selectivity of the RAR products toward all-trans-retinoic acid (RA), Am80 and Ch55 was studied by filter binding assay. The affinity of the ligands toward RAR-alpha decreased in the order of Ch55 greater than RA greater than Am80. The affinity of the ligands toward RAR-beta decreased in the order of Ch55 greater than Am80 greater than RA.

MeSH terms

  • Blotting, Northern
  • Carrier Proteins / genetics*
  • Carrier Proteins / metabolism
  • Cell Line
  • Gene Expression*
  • Genes
  • HeLa Cells / metabolism
  • Humans
  • Kinetics
  • Ligands
  • Neoplasm Proteins / genetics*
  • RNA, Messenger / genetics
  • Receptors, Retinoic Acid
  • Substrate Specificity
  • Transcription, Genetic
  • Transfection
  • Tretinoin / metabolism*

Substances

  • Carrier Proteins
  • Ligands
  • Neoplasm Proteins
  • RNA, Messenger
  • Receptors, Retinoic Acid
  • Tretinoin