Synthesis of synthetic small molecule transcription factors (STF).
Synthesis of synthetic small molecule transcription factors (STF).
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DOI：
10.1093/nass/nrl015
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发表时间：
2006-11
期刊：
影响因子：
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通讯作者：
Ayato Sato;Yoshinori Kawazoe;Shinji Kamisuki;M. Uesugi
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文献类型：
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作者：
Ayato Sato;Yoshinori Kawazoe;Shinji Kamisuki;M. Uesugi
通过小合成分子对基因表达进行外部控制是化学领域的一个挑战。在这里，我们讨论小分子转录因子模拟物的合成方面，包括我们称为 STF1 (1) 的分子。 STF1 刺激由特定 DNA 元件控制的报告基因的转录，其行为就像天然存在的转录因子一样。然而，尽管发夹-聚酰胺-FITC 缀合物和扳手洛尔 (2) 作为单独的化合物具有细胞渗透性，但 STF1 的细胞渗透性有限。 STF1类似物（STF）的系统合成探索，通过优化分子的物理性质，有望提高其细胞通透性，用于生物学研究。
External control of gene expression by small synthetic molecules represents a challenge in chemistry. Here we discuss the synthetic aspects of small molecule transcription factor mimics including a molecule we call STF1 (1). STF1 stimulates the transcription of a reporter gene controlled by specific DNA elements and behaves just as a naturally occurring transcription factor. However, STF1 had limited cell permeability, even though the hairpin-polyamide-FITC conjugate and the wrenchnolol (2) are cell permeable as separate compounds. Systematic synthetic exploration of STF1 analogs (STFs), by optimizing the physical properties of the molecule, is expected to increase its cell permeability for biological studies.