Putative role of membranes in the HIV fusion inhibitor enfuvirtide mode of action at the molecular level

被引:58
作者
Veiga, S
Henriques, S
Santos, NC
Castanho, M [1 ]
机构
[1] Univ Lisbon, Fac Ciencias, Ctr Quim & Bioquim, P-1699 Lisbon, Portugal
[2] Fac Vet Med Lisbon, Inst Mol Med, Inst Bioquim, P-1649028 Lisbon, Portugal
[3] Inst Super Tecn, Ctr Quim Fis Mol, P-1049001 Lisbon, Portugal
关键词
AIDS; enfuvirtide; fusion inhibitor; fuzeon; HIV; T20;
D O I
10.1042/BJ20031350
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Partition of the intrinsically fluorescent HIV fusion inhibitor enfuvirtide into lipidic membranes is relatively high (DeltaG=6.6 kcal (.) 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.
引用
收藏
页码:107 / 110
页数:4
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