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Future challenges for microsomal transport protein inhibitors.

机译:微粒体转运蛋白抑制剂的未来挑战。

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A review entitled "Future Challenges for Microsomal Transport Protein Inhibitors" 1 stated (page 281), based upon a manuscript 2 that "A mouse-specific ASO (Isis Pharmaceuticals 147764) demonstrated direct and specific inhibition of MTP in a murine model of hyperlipidemia". In that same paragraph, it was implied that MTP and apoB ASOs were directly compared in depth in that manuscript 2. As the primary author of this publication, I would like to point out that those statements are factually incorrect on both counts. As the title of the reference implies, ISIS 147764 is an ASO designed to specifically and selectively inhibit the apoB, not MTP, message. Furthermore, the data clearly show specific inhibition of apoB mRNA and protein. An MTP ASO was only used to demonstrate specificity and selectivity of the apoB drug and data obtained using the MTP ASO were not shown in the cited publication 2. It was also clearly stated in the manuscript 2 that MTP was not affected by apoB antisense treatment.
机译:一篇题为“微粒体转运蛋白抑制剂的未来挑战”[1]的评论指出(第281页),基于一份手稿[2],“小鼠特异性ASO(Isis Pharmaceuticals 147764)在高脂血症小鼠模型中证明了MTP的直接和特异性抑制”。在同一段中,暗示MTP和apoB ASO在该手稿中进行了直接深入比较[2]。作为本出版物的主要作者,我想指出,这些陈述在这两个方面都是不正确的。正如参考文献的标题所暗示的那样,ISIS 147764 是一种 ASO,旨在特异性和选择性地抑制 apoB,而不是 MTP 消息。此外,数据清楚地显示了对apoB mRNA和蛋白质的特异性抑制。MTP ASO仅用于证明apoB药物的特异性和选择性,使用MTP ASO获得的数据未在引用的文献中显示[2]。手稿[2]中也明确指出,MTP不受apoB反义处理的影响。

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