Structural basis of the function of endothelin receptor
Structural basis of the function of endothelin receptor
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DOI：
10.1023/a:1006986914326
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发表时间：
1999-01-01
影响因子：
4.3
通讯作者：
Okamoto, Y
中科院分区：
文献类型：
--
作者：
Masaki, T;Ninomiya, H;Okamoto, Y
内皮素受体是研究七螺旋G蛋白偶联受体功能的良好模型。在配体与七螺旋受体的结合中，受体具有两种功能，即“信息”和“地址”功能。每种功能被分配给受体的不同结构域。配体结构的不同部分也对应于受体的每个结构域。经典的受体分类是根据地址域的不同，即受体的亲和力差异来进行的。然而，目前的结果预测，受体的分类也可以根据信息域进行。配体刺激ET受体后，受体将信号传递给G蛋白。有几种G蛋白可能被激活。受体的不同结构域被分配给不同G α蛋白的偶联。激活的G蛋白将信息传递给效应器。每个G α蛋白作用于不同的靶分子，导致不同的反应。然而，每种G α蛋白的激活可能取决于其细胞内水平。即使相同的受体被相同的配体激活，最终的反应也会因细胞而异。因此，难以根据受体的功能对受体进行分类。(Mol Cell Biochem 190：153-156，1999）。
Endothelin receptor is a good model for analysis of the function of heptahelical G-protein coupled receptor. In ligand binding to the heptahelical receptor, the receptor has two functions, i.e. 'message' and 'address' functions. Each function has been assigned to different domain of the receptor. A different part of the ligand structure also corresponds to each domain of the receptor. Classically, classification of receptor has been done according to the difference of address domain, i.e. affinity difference of the receptor. However, present results predict that the classification of receptor is also possible according to the message domain.After stimulation of ET receptor by a ligand, the receptor transmits a signal to G-protein. Several kinds of G-proteins can possibly be activated. Different structural domains of the receptor an assigned to the coupling of the different G alpha-protein. Activated G-protein transmits the message to effector. Each G alpha-protein acts on different target molecules, resulting in different responses. However, the activation of each G alpha-protein presumably depends on its intracellular level. Even if the same receptor is activated with the same ligand, resulting final response is different from cell to cell. Therefore, classification of receptor according to the function of the receptor is difficult. (Mol Cell Biochem 190: 153-156, 1999).