Nakagama H, Heinrich G, Pelletier J, Housman D E
Center for Cancer Research, Massachusetts Institute of Technology, Cambridge 02139.
Mol Cell Biol. 1995 Mar;15(3):1489-98. doi: 10.1128/MCB.15.3.1489.
The Wilms' tumor suppressor gene, WT1, encodes a zinc finger polypeptide which plays a key role regulating cell growth and differentiation in the urogenital system. Using the whole-genome PCR approach, we searched murine genomic DNA for high-affinity WT1 binding sites and identified a 10-bp motif 5'GCGTGGGAGT3' which we term WTE). The WTE motif is similar to the consensus binding sequence 5'GCG(G/T)GGGCG3' recognized by EGR-1 and is also suggested to function as a binding site for WT1, setting up a competitive regulatory loop. To evaluate the underlying biochemical basis for such competition, we compared the binding affinities of WT1 and EGR1 for both sequences. WT1 shows a 20- to 30-fold-higher affinity for the WTE sequence compared with that of the EGR-1 binding motif. Mutational analysis of the WTE motif revealed a significant contribution to binding affinity by the adenine nucleotide at the eighth position (5'GCGTGGGAGT3') as well as by the 3'-most thymine (5'GCGTGGGAGT3'), whereas mutations in either flanking nucleotides or other nucleotides in the core sequence did not significantly affect the specific binding affinity. Mutations within WT1 zinc fingers II to IV abolished the sequence-specific binding of WT1 to WTE, whereas alterations within the first WT1 zinc finger reduced the binding affinity approximately 10-fold but did not abolish sequence recognition. We have thus identified a WT1 target, which, although similar in sequence to the EGR-1 motif, shows a 20- to 30-fold-higher affinity for WT1. These results suggest that physiological action of WT1 is mediated by binding sites of significantly higher affinity than the 9-bp EGR-1 binding motif. The role of the thymine base in contributing to binding affinity is discussed in the context of recent structural analysis.
肾母细胞瘤抑癌基因WT1编码一种锌指多肽,该多肽在泌尿生殖系统中对细胞生长和分化起着关键的调节作用。我们采用全基因组PCR方法,在小鼠基因组DNA中搜索高亲和力的WT1结合位点,鉴定出一个10个碱基的基序5'GCGTGGGAGT3',我们将其命名为WTE。WTE基序与早期生长反应因子-1(EGR-1)识别的共有结合序列5'GCG(G/T)GGGCG3'相似,也被认为可作为WT1的结合位点,从而建立了一个竞争性调节环。为了评估这种竞争的潜在生化基础,我们比较了WT1和EGR1对这两个序列的结合亲和力。与EGR-1结合基序相比,WT1对WTE序列的亲和力高20至30倍。对WTE基序的突变分析表明,第八位的腺嘌呤核苷酸(5'GCGTGGGAGT3')以及最3'端的胸腺嘧啶(5'GCGTGGGAGT3')对结合亲和力有显著贡献,而侧翼核苷酸或核心序列中的其他核苷酸发生突变则不会显著影响特异性结合亲和力。WT1锌指II至IV内的突变消除了WT1与WTE的序列特异性结合,而WT1第一个锌指内的改变使结合亲和力降低了约10倍,但并未消除序列识别。因此,我们鉴定出了一个WT1靶点,尽管其序列与EGR-1基序相似,但对WT1的亲和力高了20至30倍。这些结果表明,WT1的生理作用是由亲和力明显高于9个碱基的EGR-1结合基序的结合位点介导的。我们结合最近的结构分析讨论了胸腺嘧啶碱基在贡献结合亲和力方面的作用。