本文選題：突變異檸檬酸脫氫酶(mIDH) + D--羥戊二酸(D-HG)��； 參考：《中國(guó)新藥雜志》2017年11期

【摘要】：異檸檬酸脫氫酶(IDH)可以催化異檸檬酸轉(zhuǎn)化為α-酮戊二酸(α-KG),突變IDH則會(huì)將α-KG轉(zhuǎn)化為致瘤代謝物D-2-羥戊二酸(D-2HG),同時(shí)導(dǎo)致DNA或組蛋白過(guò)甲基化。IDH抑制劑能夠通過(guò)抑制作用使D-2HG減少,誘導(dǎo)組蛋白去甲基化,從而抑制腫瘤發(fā)展。本文對(duì)現(xiàn)有IDH抑制劑的結(jié)構(gòu)、作用機(jī)制、臨床研究進(jìn)行全面綜述。
[Abstract]:Isocitrate dehydrogenase (IDH) can catalyze the conversion of isocitric acid to 偽 -ketoglutaric acid (偽 -KGG), while mutant IDH can transform 偽 -KG into D-2HGG, which leads to the reduction of D-2HG by inhibiting DNA or histone hypermethylation. Histone demethylation is induced to inhibit tumor progression. In this review, the structure, mechanism and clinical study of idh inhibitors were reviewed.
【作者單位】： 中國(guó)醫(yī)藥工業(yè)研究總院上海醫(yī)藥工業(yè)研究院創(chuàng)新藥物與制藥工藝國(guó)家重點(diǎn)實(shí)驗(yàn)室;
【分類號(hào)】：R979.1
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本文編號(hào)：2014370