[Binding activity of retinoids with recombinant human retinoic acid receptor RAR alpha].
OBJECTIVE
To establish a model for the rapid screening of differentiation-inducing agents.


METHODS
Human RAR alpha cDNA was cloned into the PT7-7 plasmids and the human recombinant RAR alpha protein was expressed in Escherichia coli. The ligand-binding activity of the receptor with all-trans retinoic acid was studied by competitive binding assay. For comparison of the binding activity, five retinoids, with different activities and chemical structures, were chosen. The binding of these retinoids to RAR alpha was investigated and compared with the NBT reduction and acid phosphatase activity of HL-60 cells induced by these compounds.


RESULTS
The binding activity of these retinoids was well correlated to their ability to induce differentiation of HL-60 cell line.


CONCLUSIONS
This model could be used to screen differentiation-inducing agents.
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing.
X
X
Cao
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Han
D000135:Acid Phosphatase / Q000378:metabolism; D002454:Cell Differentiation / Q000187:drug effects; D004926:Escherichia coli / Q000378:metabolism; D018922:HL-60 Cells / Q000201:enzymology / Q000473:pathology; D006801:Humans; D011485:Protein Binding; D018168:Receptors, Retinoic Acid / Q000096:biosynthesis / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D000072482:Retinoic Acid Receptor alpha; D014212:Tretinoin / Q000378:metabolism*
C000607071:RARA protein, human; D018168:Receptors, Retinoic Acid; D011994:Recombinant Proteins; D000072482:Retinoic Acid Receptor alpha; D014212:Tretinoin; D000135:Acid Phosphatase