重组维甲酸受体RARα和RARβ的配体特异性
Ligand specificities of recombinant retinoic acid receptors RAR alpha and RAR beta.
作者信息
Crettaz M, Baron A, Siegenthaler G, Hunziker W
机构信息
Department of Pharmaceutical Research, F. Hoffmann-La Roche Ltd., Basle, Switzerland.
出版信息
Biochem J. 1990 Dec 1;272(2):391-7. doi: 10.1042/bj2720391.
Binding of retinoic acid (RA) to specific RA receptors alpha and beta (RAR alpha and RAR beta) was studied. Receptors were obtained in two ways: (1) full-length receptors were produced by transient expression of the respective human cDNAs in COS 1 cells; and (2) the ligand-binding domains of RAR alpha and RAR beta were produced in Escherichia coli. RA binding to the wild-type and truncated forms of the receptor was identical for both RAR alpha and RAR beta, indicating that the ligand-binding domains have retained the binding characteristics of the intact receptors. Furthermore, RA bound with the same affinity to both RAR alpha and RAR beta. Only retinoid analogues with an acidic end-group were able to actively bind to both receptors. On measuring the binding of various retinoids, we have found that the properties of the ligand-binding sites of RAR alpha and RAR beta were rather similar. Two retinoid analogues were capable of binding preferentially to either RAR alpha or RAR beta, suggesting that it may be possible to synthesize specific ligands for RAR alpha and RAR beta.
研究了视黄酸（RA）与特异性视黄酸受体α和β（RARα和RARβ）的结合。受体通过两种方式获得：（1）全长受体通过在COS 1细胞中瞬时表达各自的人cDNA产生；（2）RARα和RARβ的配体结合结构域在大肠杆菌中产生。对于RARα和RARβ，RA与受体野生型和截短形式的结合是相同的，这表明配体结合结构域保留了完整受体的结合特性。此外，RA与RARα和RARβ的结合亲和力相同。只有具有酸性端基的类视黄醇类似物能够与两种受体有效结合。在测量各种类视黄醇的结合时，我们发现RARα和RARβ配体结合位点的性质相当相似。两种类视黄醇类似物能够优先与RARα或RARβ结合，这表明有可能合成针对RARα和RARβ的特异性配体。
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