Phorbol diesters promote beta-adrenergic receptor phosphorylation and adenylate cyclase desensitization in duck erythrocytes.
Phorbol diesters promote beta-adrenergic receptor phosphorylation and adenylate cyclase desensitization in duck erythrocytes.
复制标题
佛波二酯促进鸭红细胞中 β-肾上腺素能受体磷酸化和腺苷酸环化酶脱敏。
DOI：
10.1016/0006-291x(84)90772-1
复制
发表时间：
1984
影响因子：
3.1
通讯作者：
Lefkowitz,RJ
中科院分区：
文献类型：
--
作者：
Sibley,DR;Nambi,P;Peters,JR;Lefkowitz,RJ
鸭红细胞与促肿瘤的佛波醇二酯或儿茶酚胺预孵育导致腺苷酸环化酶活性减弱。12-O-十四烷酰基佛波醇-13-乙酸酯（TPA）和佛波醇12，13-二丁酸酯处理分别诱导异丙肾上腺素刺激的腺苷酸环化酶活性的38%和30%脱敏。相反，无活性的佛波醇二酯，4α-佛波醇12，13-二癸酸酯，在促进腺苷酸环化酶脱敏中没有效果。异丙肾上腺素引起51%的脱敏。用TPA孵育32 Pi标记的红细胞促进β-肾上腺素能受体磷酸化增加3- 4倍，与异丙肾上腺素孵育一样。用TPA和异丙肾上腺素一起处理细胞导致脱敏和受体磷酸化，其不大于用单独的试剂观察到的那些。这些数据表明蛋白激酶C在调节β-肾上腺素能受体功能中的潜在作用。
Preincubation of duck erythrocytes with tumor promoting phorbol diesters or catecholamines leads to attenuation of adenylate cyclase activity. 12-O-Tetradecanoyl phorbol-13-acetate (TPA) and phorbol 12,13-dibutyrate treatment induced a 38% and 30% desensitization of isoproterenol-stimulated adenylate cyclase activity, respectively. In contrast, the inactive phorbol diester, 4α-phorbol 12,13-didecanoate, was without effect in promoting adenylate cyclase desensitization. The catecholamine isoproterenol induced a 51% desensitization. Incubation of32Pi labeled erythrocytes with TPA promoted a 3- to 4-fold increase in phosphorylation of the β-adrenergic receptor as did incubation with isoproterenol. Treatment of the cells with both TPA and isoproterenol together resulted in desensitization and receptor phosphorylation which were no greater than those observed with either agent alone. These data suggest a potential role for protein kinase C in regulating β-adrenergic receptor function.