Castillo S O, Xiao Q, Kostrouch Z, Dozin B, Nikodem V M
National Institutes of Health, National Institute of Diabetes and Digestive and Kidney Diseases, Genetics and Biochemistry Branch, Mechanisms of Gene Regulation Section, Bethesda, MD 20892-1766, USA.
Gene Expr. 1998;7(1):1-12.
Orphan nuclear receptors such as Nurr1 and Nur77 have conserved amino acid sequences in the zinc finger DNA binding domains and similar COOH-terminal regions, but have no known ligands. These receptors can bind DNA sequences (response elements) as monomers and can also heterodimerize with the retinoid X receptor to activate transcription. We report here the identification and initial characterization of a novel COOH-terminal truncated isoform of Nurr1, Nurr1a. Internal splicing of Nurr1 generates a frameshift such that a stop codon is prematurely encoded resulting in a naturally occurring COOH-terminal truncation. Embryonic and postnatal mouse brain showed both Nurr1 and Nurr1a mRNAs expressed during development. To characterize essential COOH-terminal elements that may be deleted from Nurr1a and determine function in putative ligand binding, we created COOH-terminal deletion mutants. Nurr1, Nur77, and 3'-truncated mutants bind in gel mobility shift assays to the monomeric Nur77 response element (B1A-RE). However, in transient transfection assays, a truncation of as little as 15 Nurr1 COOH-terminal amino acids diminished transcriptional activation of B1A-thymidine kinase-chloramphenicol acetyltransferase reporter. This result was not seen for a similar Nur77 deletion mutant, Nur77-586. Unlike full-length Nurr1 and Nur77, transactivation by Nur77-586 was not augmented in response to the presence of retinoid-like receptor and 9-cis-retinoic acid. Thus, the interaction of putative ligand binding and transactivation for Nurr1 and Nur77 may function differently.
诸如Nurr1和Nur77等孤儿核受体在锌指DNA结合结构域以及相似的COOH末端区域具有保守的氨基酸序列,但目前尚未发现其配体。这些受体能够以单体形式结合DNA序列(反应元件),也能与视黄酸X受体形成异源二聚体以激活转录。我们在此报告了一种新型的Nurr1的COOH末端截短异构体Nurr1a的鉴定及初步特征。Nurr1的内部剪接产生移码突变,使得提前编码了一个终止密码子,从而导致自然发生的COOH末端截短。胚胎期和出生后的小鼠脑在发育过程中均表达Nurr1和Nurr1a的mRNA。为了表征可能从Nurr1a中缺失的必需COOH末端元件,并确定其在假定配体结合中的功能,我们构建了COOH末端缺失突变体。在凝胶迁移率变动分析中,Nurr1、Nur77和3'-截短突变体与单体Nur77反应元件(B1A-RE)结合。然而,在瞬时转染分析中,Nurr1的COOH末端仅截短15个氨基酸就会减弱B1A-胸苷激酶-氯霉素乙酰转移酶报告基因的转录激活。对于类似的Nur77缺失突变体Nur77-586,未观察到这种结果。与全长Nurr1和Nur77不同,Nur77-586的反式激活不会因类视黄酸受体和9-顺式视黄酸的存在而增强。因此,Nurr1和Nur77在假定配体结合和反式激活方面的相互作用可能具有不同的功能。