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Phospholipase A2 inhibitors.

机译:磷脂酶A2抑制剂。

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PURPOSE OF REVIEW: As the role of lipids and inflammation in the genesis and progression of the atherosclerosis disease is unquestionable, novel treatment modalities that target both aspects are currently under investigation. RECENT FINDINGS: For a long time atherosclerosis was regarded as a lipid-driven disease, but now it is evident that it also involves the simultaneous and combined effect of inflammation and immunological pathways. The secreted PLA2s and the lipoprotein-associated phospholipase A2 (Lp-PLA2) have been associated with atherogenesis and its complications. These two enzymes produce biologically active metabolites that are involved in several phases of the atherosclerosis process. SUMMARY: In animal, pathological and epidemiological studies, the increased levels of these two phospholipases (i.e. PLA2s and Lp-PLA2) have been related with an increase in complex coronary lesions and increase in major cardiovascular clinical events, respectively. Therefore, inhibition of these enzymes has become the focus of research in this last decennium. Novel pharmacological inhibitors of those enzymes such as darapladib and varespladib emerge as promising therapeutical options for treating patients with coronary artery disease. Ongoing mechanistic and clinical outcome trials will further elucidate their role in this context.
机译:审查的目的:由于脂质和炎症在动脉粥样硬化疾病的发生和发展中的作用是毋庸置疑的,目前正在研究针对这两个方面的新型治疗方法。最近的发现:长期以来,动脉粥样硬化被认为​​是脂质驱动的疾病,但现在很明显,它还涉及炎症和免疫途径的同时和联合作用。分泌的PLA2和脂蛋白相关的磷脂酶A2(Lp-PLA2)与动脉粥样硬化及其并发症有关。这两种酶产生具有生物活性的代谢产物,参与了动脉粥样硬化过程的多个阶段。摘要:在动物,病理学和流行病学研究中,这两种磷脂酶(即PLA2s和Lp-PLA2)水平的升高分别与复杂冠状动脉病变的增加和主要心血管临床事件的增加有关。因此,抑制这些酶已成为最近十年的研究重点。那些酶的新型药理抑制剂,例如达拉帕地布和varespladib,作为治疗冠心病患者的有前途的治疗选择而出现。正在进行的机械和临床结果试验将进一步阐明其在这种情况下的作用。

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