How lipophilic cannabinergic ligands reach their receptor sites
How lipophilic cannabinergic ligands reach their receptor sites
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DOI：
10.1016/j.prostaglandins.2004.01.010
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发表时间：
2005-09-01
影响因子：
2.9
通讯作者：
Guo, HX
中科院分区：
文献类型：
--
作者：
Makriyannis, A;Tian, XY;Guo, HX
据推测，亲脂性配体通过跨膜双层的快速侧向扩散到达膜结合功能蛋白的作用部位。我们已经用核磁共振实验证明，当这些配体被结合到膜系统中时，会呈现出优先的取向和构象。当这些分子占据双层中的特定位置时，它们会经历快速的横向扩散，这使得它们能够与各自的蛋白质作用部位进行富有成效的相互作用。使用一组经典和非经典大麻素以及内源性大麻素配体ANANDAME对所提出的模型进行了讨论。(C)2005 Elsevier Inc.保留所有权利。
It is postulated that lipophilic ligands reach their sites of action on membrane-bound functional proteins through fast lateral diffusion across the membrane bilayer. We have shown using NMR experiments that such ligands when incorporated in a membrane system assume a preferred orientation and conformation. While occupying a specific location within the bilayer, these molecules undergo fast lateral diffusion which allows them to engage in productive interactions with their respective protein sites of action. The proposed model is discussed using a group of classical and non-classical cannabinoids as well as the endogenous cannabinoid ligand anandamide. (c) 2005 Elsevier Inc. All rights reserved.