膜在HIV融合抑制剂恩夫韦肽分子水平作用模式中的假定作用。
Putative role of membranes in the HIV fusion inhibitor enfuvirtide mode of action at the molecular level.
作者信息
Veiga Salomé, Henriques Sónia, Santos Nuno C, Castanho Miguel
机构信息
Centro de Química e Bioquímica, Faculdade de Ciências da Universidade de Lisboa, Campo Grande C8, 1749-016 Lisboa, Portugal.
出版信息
Biochem J. 2004 Jan 1;377(Pt 1):107-10. doi: 10.1042/BJ20031350.
Abstract
Partition of the intrinsically fluorescent HIV fusion inhibitor enfuvirtide into lipidic membranes is relatively high (Delta G =6.6 kcal x mol(-1)) and modulated by cholesterol. A shallow position in the lipidic matrix makes it readily available for interaction with gp41. No conformational energetic barrier prevents enfuvirtide from being active in both aqueous solution and lipidic membranes. Lipidic membranes may play a key role in the enfuvirtide biochemical mode of action.
摘要
具有内在荧光的HIV融合抑制剂恩夫韦肽在脂质膜中的分配相对较高（ΔG = 6.6千卡×摩尔⁻¹），且受胆固醇调节。其在脂质基质中的位置较浅，使其易于与gp41相互作用。不存在构象能垒阻止恩夫韦肽在水溶液和脂质膜中均具有活性。脂质膜可能在恩夫韦肽的生化作用模式中起关键作用。
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