本文關(guān)鍵詞： 蛋白降解 PROTACs 藥物設(shè)計(jì) 靶點(diǎn) 進(jìn)展　出處：《中國(guó)新藥雜志》2017年22期 　論文類(lèi)型：期刊論文

【摘要】：利用小分子蛋白降解靶向嵌合體(PROTACs)誘導(dǎo)蛋白降解的新型腫瘤治療策略能夠通過(guò)細(xì)胞內(nèi)泛素-蛋白酶體降解系統(tǒng)而調(diào)控靶蛋白水平,從而克服傳統(tǒng)小分子抑制劑的缺陷。因此針對(duì)小分子PROTACs的設(shè)計(jì)、合成及表征成為當(dāng)前藥物化學(xué)研究的前沿之一。本文簡(jiǎn)介小分子PROTACs的功能及作用機(jī)制,著重綜述小分子PROTACs的最新研究成果,展望其應(yīng)用前景和亟需解決的問(wèn)題。
[Abstract]:A novel tumor therapy strategy for protein degradation induced by small molecular protein degradation target chimera (PROTACs) can regulate target protein level through intracellular ubiquitin proteasome degradation system. Therefore, the design, synthesis and characterization of small molecular PROTACs have become one of the frontiers in the field of drug chemistry. In this paper, the function and mechanism of small molecule PROTACs are briefly introduced. The latest research results of small molecule PROTACs are reviewed, and its application prospect and problems that need to be solved are prospected.
【作者單位】： 中國(guó)藥科大學(xué)藥學(xué)院;
【基金】：國(guó)家自然科學(xué)基金(21372260)
【分類(lèi)號(hào)】：R979.1
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本文編號(hào)：1522713