Rensburg Gerrit van, Mackedenski Sebastian, Lee Chow H
Chemistry Program, University of Northern British Columbia, Prince George, British Columbia, Canada.
PLoS One. 2017 Feb 9;12(2):e0171196. doi: 10.1371/journal.pone.0171196. eCollection 2017.
Coding region determinant-binding protein (CRD-BP) binds to the 3'-UTR of microphthalmia-associated transcription factor (MITF) mRNA to prevent its targeted degradation by miR-340. Here, we aim to further understand the molecular interaction between CRD-BP and MITF RNA. Using point mutation in the GXXG motif of each KH domains, we showed that all four KH domains of CRD-BP are important for their physical association with MITF RNA. We mapped the CRD-BP-binding site in the 3'-UTR of MITF RNA from nts 1330-1740 and showed that the 49-nt fragment 1621-1669 is the minimal size MITF RNA for binding. Upon deletion of nts 1621-1669 within the nts1550-1740 of MITF RNA, there was a 3-fold increase in dissociation constant Kd, which further confirms the critical role sequences within nts 1621-1669 in binding to CRD-BP. Amongst the eight antisense oligonucleotides designed against MITF RNA 1550-1740, we found MHO-1 and MHO-7 as potent inhibitors of the CRD-BP-MITF RNA interaction. Using RNase protection and fluorescence polarization assays, we showed that both MHO-1 and MHO-7 have affinity for the MITF RNA, suggesting that both antisense oligonucleotides inhibited CRD-BP-MITF RNA interaction by directly binding to MITF RNA. The new molecular insights provided in this study have important implications for understanding the oncogenic function of CRD-BP and development of specific inhibitors against CRD-BP-MITF RNA interaction.
编码区决定簇结合蛋白(CRD-BP)与小眼畸形相关转录因子(MITF)mRNA的3'-非翻译区结合,以防止其被miR-340靶向降解。在此,我们旨在进一步了解CRD-BP与MITF RNA之间的分子相互作用。通过对每个KH结构域的GXXG基序进行点突变,我们发现CRD-BP的所有四个KH结构域对于它们与MITF RNA的物理结合都很重要。我们绘制了MITF RNA 3'-非翻译区中从第1330至1740位核苷酸的CRD-BP结合位点,并表明49个核苷酸的片段1621 - 1669是结合所需的最小尺寸的MITF RNA。在删除MITF RNA第1550至1740位核苷酸内的1621 - 1669位核苷酸后,解离常数Kd增加了3倍,这进一步证实了1621 - 1669位核苷酸内的序列在与CRD-BP结合中的关键作用。在针对MITF RNA 1550 - 1740设计的八个反义寡核苷酸中,我们发现MHO-1和MHO-7是CRD-BP-MITF RNA相互作用的有效抑制剂。使用核糖核酸酶保护和荧光偏振分析,我们表明MHO-1和MHO-7都对MITF RNA具有亲和力,这表明这两种反义寡核苷酸通过直接结合MITF RNA来抑制CRD-BP-MITF RNA相互作用。本研究中提供的新分子见解对于理解CRD-BP的致癌功能以及开发针对CRD-BP-MITF RNA相互作用的特异性抑制剂具有重要意义。