Hadjiivanova N, Flint N, Evans W H, Dix C, Cooke B A
Biochem J. 1984 Sep 15;222(3):749-54. doi: 10.1042/bj2220749.
The internalization of beta-adrenergic receptors was investigated in rat livers perfused with an agonist ([3H]isoprenaline) or an antagonist ([125I]iodocyanopindolol). Analytical centrifugation of liver homogenates indicated that the ligands were transferred rapidly to endosomal and lysosomal positions in sucrose gradients. Endosome fractions contained beta-adrenergic binding sites, but adenylate cyclase activity was low and poorly activated by isoprenaline. The results indicate that the receptor-regulatory-protein-adenylate cyclase complex was disassembled during uptake of beta-adrenergic ligands, with the adenylate cyclase being retained at the plasma membrane.
在灌注激动剂([3H]异丙肾上腺素)或拮抗剂([125I]碘氰吲哚洛尔)的大鼠肝脏中研究了β-肾上腺素能受体的内化。肝脏匀浆的分析离心表明,配体在蔗糖梯度中迅速转移至内体和溶酶体位置。内体部分含有β-肾上腺素能结合位点,但腺苷酸环化酶活性较低,且异丙肾上腺素对其激活作用较弱。结果表明,在β-肾上腺素能配体摄取过程中,受体-调节蛋白-腺苷酸环化酶复合物发生了解离,腺苷酸环化酶保留在质膜上。