降膽固醇藥物新靶標(biāo)前蛋白轉(zhuǎn)化酶枯草溶菌素9的研究進(jìn)展
發(fā)布時(shí)間:2018-05-07 07:42
本文選題:膽固醇代謝 + 低密度脂蛋白膽固醇 ; 參考:《第二軍醫(yī)大學(xué)學(xué)報(bào)》2017年11期
【摘要】:他汀類藥物主要用于降低血低密度脂蛋白膽固醇(LDL-C)以及預(yù)防心血管疾病,但其臨床療效和機(jī)體的耐受性尚存在不穩(wěn)定性。人類前蛋白轉(zhuǎn)化酶枯草溶菌素9(PCSK9)屬于前蛋白轉(zhuǎn)化酶家族,主要由肝臟產(chǎn)生并分泌入血,可促進(jìn)肝臟中低密度脂蛋白受體(LDLR)的降解,從而參與調(diào)控血LDL-C水平。人群中PCSK9的功能獲得型或缺失型基因突變與血LDL-C含量、心血管疾病患病率密切相關(guān)。可通過負(fù)反饋機(jī)制上調(diào)PCSK9,促進(jìn)LDLR的降解,從而降低他汀類藥物的療效。因此,抑制PCSK9活性可望成為治療高膽固醇血癥的一種新的有效方法。本文主要綜述PCSK9調(diào)節(jié)膽固醇代謝及其臨床應(yīng)用的研究進(jìn)展。
[Abstract]:Statins are mainly used to reduce LDL-C and prevent cardiovascular disease, but the clinical efficacy and tolerance are still unstable. Human proprotein converting enzyme lysogenin 9 (PCSK9) belongs to the proprotein converting enzyme family, which is mainly produced and secreted into blood by the liver, which can promote the degradation of low density lipoprotein receptor (LDLR) in the liver and thus participate in the regulation of blood LDL-C level. The mutation of PCSK9 functional acquisition type or deletion type gene is closely related to the blood LDL-C content and the prevalence of cardiovascular disease. PCSK9 can be upregulated by negative feedback mechanism to promote the degradation of LDLR and reduce the efficacy of statins. Therefore, inhibition of PCSK9 activity is expected to be a new and effective method for the treatment of hypercholesterolemia. This article reviews the progress in the regulation of cholesterol metabolism by PCSK9 and its clinical application.
【作者單位】: 第二軍醫(yī)大學(xué)基礎(chǔ)醫(yī)學(xué)部病理生理學(xué)教研室;
【基金】:國家重點(diǎn)基礎(chǔ)研究發(fā)展計(jì)劃(“973計(jì)劃”,2013CB530603) 國家自然科學(xué)基金(31730042)~~
【分類號】:R96
【相似文獻(xiàn)】
相關(guān)期刊論文 前2條
1 李艷芳;蔣志麗;郭彥青;宋俊迎;;β_3腎上腺素受體對前蛋白轉(zhuǎn)化酶枯草溶菌素9和低密度脂蛋白受體表達(dá)的影響[J];中華老年心腦血管病雜志;2014年06期
2 李長永;白元;秦永文;;前蛋白轉(zhuǎn)化酶枯草溶菌素9抑制劑的研究進(jìn)展[J];藥學(xué)服務(wù)與研究;2013年04期
,本文編號:1856009
本文鏈接:http://sikaile.net/yixuelunwen/yiyaoxuelunwen/1856009.html
最近更新
教材專著