本文選題：分枝桿菌膜蛋白 + 結(jié)核分枝桿菌��； 參考：《藥學(xué)學(xué)報(bào)》2017年09期

【摘要】：分枝桿菌膜蛋白3(mycobacterial membrane protein large 3,Mmp L3)屬于抗瘤細(xì)胞分裂(RND)蛋白超家族,它主要參與結(jié)核分枝桿菌中海藻糖單霉菌酸酯的轉(zhuǎn)運(yùn)過程,對(duì)Mmp L3的抑制可以影響結(jié)核分枝桿菌細(xì)胞壁的合成。近年來,通過表型篩選已發(fā)現(xiàn)并確證了7類不同化學(xué)骨架的Mmp L3抑制劑,擬用于耐藥結(jié)核病的治療。本文將簡(jiǎn)要論述這幾類Mmp L3抑制劑及其構(gòu)效關(guān)系,介紹靶標(biāo)確證的方法,并進(jìn)一步探討Mmp L3抑制劑的作用機(jī)制。
[Abstract]:Mycobacterium membrane protein 3(mycobacterial membrane protein large _ 3 / MMP _ L _ 3 belongs to the superfamily of anti-tumor cell division (RND) protein, which is mainly involved in the transport of mycobacterium alginate monophosphate in Mycobacterium tuberculosis, and the inhibition of MMP L _ 3 can affect the synthesis of cell wall of Mycobacterium tuberculosis. In recent years, seven kinds of MMP L3 inhibitors with different chemical cytoskeleton have been identified and confirmed by phenotypic screening, which can be used in the treatment of drug-resistant tuberculosis. This paper briefly discusses these MMP L3 inhibitors and their structure-activity relationships, introduces the methods of target identification, and further discusses the mechanism of MMP L3 inhibitors.
【作者單位】： 中國醫(yī)學(xué)科學(xué)院北京協(xié)和醫(yī)學(xué)院藥物研究所活性物質(zhì)發(fā)現(xiàn)與適藥化研究北京市重點(diǎn)實(shí)驗(yàn)室;
【基金】：國家科技重大專項(xiàng)“重大新藥創(chuàng)制”子課題2015ZX09102007“抗耐藥結(jié)核新藥TBI-001的臨床前研究”
【分類號(hào)】：R978

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