Tang Y, Ramakrishnan C, Thomas J, DeFranco D B
Department of Biological Sciences, University of Pittsburgh, Pennsylvania 15260, USA.
Mol Biol Cell. 1997 May;8(5):795-809. doi: 10.1091/mbc.8.5.795.
All steroid receptors possess a bipartite nuclear localization signal sequence (NLS) that localizes within the second zinc finger of their DNA-binding domain. Fine-structure mapping of the rat glucocorticoid receptor (rGS) NLS identified a composite signal composed of three distinct proto-NLSs that function effectively when present in unique pairs. At least one of the rGR proto-NLSs appears to influence receptor trafficking within the nucleus, as revealed by a unique nuclear staining pattern of receptors possessing a point mutation (i.e., arginine at position 496; R496), at proto-NLS, pNLS-2. Specifically, carboxyl-terminal-truncated rGRs possessing various point mutations at R496 localized within a limited number of large foci in nuclei of transiently transfected COS-1 cells. R496 mutations did not affect subnuclear targeting when present in full-length rGR, reflecting a protective effect of the receptor's ligand-binding domain that can be exerted in cis and in trans. The effects of rGR R496 mutations on subnuclear targeting were not autonomous because we also observed a coincident localization of hsp70, the 70-kDa heat shock protein, within nuclear foci that include r496 mutant receptors. The elimination of R496 mistargeting by overexpression of an hsp70 partner (i.e., the DnaJ homologue, HDJ-2/HSDJ) suggests that the hsp70/DnaJ chaperone system is mobilized to specific sites within the nucleus in response to inappropriate targeting or folding of specific mutant receptors. HDJ-2/HSDJ overexpression also corrects defective transactivation and transrepression activity of R496 mutant GRs. Thus, molecular chaperones, such as members of the hsp70 and DnaJ families, may survey the nucleus for misfolded proteins and actively participate in their refolding into biologically active conformational states.
所有类固醇受体都具有一个双功能核定位信号序列(NLS),该序列位于其DNA结合域的第二个锌指内。大鼠糖皮质激素受体(rGR)NLS的精细结构图谱确定了一个由三个不同的原NLS组成的复合信号,当以独特的配对形式存在时,它们能有效地发挥作用。rGR原NLS中至少有一个似乎会影响受体在细胞核内的运输,这一点通过在原NLS pNLS-2处具有点突变(即第496位的精氨酸;R496)的受体的独特核染色模式得以揭示。具体而言,在瞬时转染的COS-1细胞的细胞核中,在R496处具有各种点突变的羧基末端截短的rGR定位于有限数量的大核灶内。当R496突变存在于全长rGR中时,并不影响亚核靶向,这反映了受体配体结合域的一种可顺式和反式发挥作用的保护作用。rGR R496突变对亚核靶向的影响不是自主的,因为我们还观察到70 kDa热休克蛋白hsp70与包含r496突变受体的核灶共定位。通过过表达hsp70伴侣(即DnaJ同源物HDJ-2/HSDJ)消除R496的错误靶向表明,hsp70/DnaJ伴侣系统会响应特定突变受体的不适当靶向或折叠而被动员到细胞核内的特定部位。HDJ-2/HSDJ的过表达还能纠正R496突变GR的缺陷反式激活和反式抑制活性。因此,分子伴侣,如hsp70和DnaJ家族的成员,可能会在细胞核中检测错误折叠的蛋白质,并积极参与将它们重新折叠成生物活性构象状态的过程。