Characterization of the human lymphocyte beta-adrenergic receptor by photoaffinity labeling. Alterations with desensitization.
Characterization of the human lymphocyte beta-adrenergic receptor by photoaffinity labeling. Alterations with desensitization.
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通过光亲和标记表征人淋巴细胞β-肾上腺素能受体。
DOI：
10.1161/01.res.58.3.384
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发表时间：
1986
影响因子：
20.1
通讯作者：
Lai,CY
中科院分区：
文献类型：
--
作者：
Feldman,RD;Lai,CY
白细胞β-受体系统的脱敏与β-受体复合物组分的功能性解偶联有关。为了确定是否脱敏和解偶联的白细胞β-受体的任何结构改变的β-受体，我们研究了标记的淋巴细胞使用光敏β-肾上腺素能拮抗剂p-叠氮基-m-[125 I]碘苄基carazolol。标记的肽通过十二烷基硫酸钠-聚丙烯酰胺凝胶电泳分离，并使用放射自显影技术检测。在破碎的细胞制备物中，在两个主要的肽带中证明了特异性标记：mol wt约等于68，000和mol wt约等于55，000。光标记的抑制是立体特异性的，并证明了与β 2-受体标记一致的激动剂的效力顺序。细胞与β-激动剂异丙肾上腺素预孵育，导致β-肾上腺素能介导的腺苷酸环化酶活性降低至对照组的60%，但[125 I]iodocyanopindolol结合测定的总结合位点无变化。在光标记研究中，与68，000 mol wt条带相比，脱敏与55，000 mol wt条带的比例标记降低至对照的58 +/- 3%以及上部条带的迁移率降低相关。这些研究表明，人类淋巴细胞β受体的结构改变与脱敏发生，类似于其他几种β受体模型系统的变化。此外，由于所描述的技术可以鉴定人β-受体结构的改变，因此可以利用这些方法来确定淋巴细胞β-受体的结构改变是否可能发生在人类疾病状态中。
Desensitization of the leukocyte beta-receptor system has been associated with a functional uncoupling of the components of the beta-receptor complex. In order to determine whether desensitization and uncoupling of the leukocyte beta-receptor is associated with any structural alterations in the beta-receptor, we studied labeling of lymphocytes using the photoactive beta-adrenergic antagonist p-azido-m-[125I]iodobenzylcarazolol. Labeled peptides were separated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and detected using autoradiographic techniques. In broken cell preparations, specific labeling was demonstrated in two major peptide bands: mol wt approximately equal to 68,000 and mol wt approximately equal to 55,000. Inhibition of photolabeling was stereospecific and demonstrated an order of potency for agonists consistent with labeling of a beta 2-receptor. Preincubation of cells with the beta-agonist, isoproterenol, resulted in a reduction in beta-adrenergic-mediated adenylate cyclase activity to 60% of control, but no change in total binding sites as determined by [125I]iodocyanopindolol binding. In photolabeling studies, desensitization was associated with a reduction in proportional labeling of the 55,000 mol wt band as compared to the 68,000 mol wt band to 58 +/- 3% of control and a reduction in mobility of the upper band. These studies suggest that structural alterations in the human lymphocyte beta-receptors occur with desensitization, analogous to changes in several other beta-receptor model systems. Also, since the techniques described can identify alterations in human beta-receptor structure, these methods may be exploited to determine whether structural alterations in lymphocyte beta-receptors may occur in human disease states.
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激动剂诱导的β-肾上腺素受体连接的腺苷酸环化酶的脱敏。
影响因子：
21.1
作者：
Harden,TK
通讯作者：
Harden,TK
腺苷酸环化酶的同源脱敏与β-肾上腺素能受体的磷酸化有关。
DOI：
10.1016/s0021-9258(18)89201-8
发表时间：
1985
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
D. Sibley;R. Strasser;M. Caron;R. Lefkowitz
通讯作者：
R. Lefkowitz
β-肾上腺素能受体的识别和调节
DOI：
--
发表时间：
1978
期刊：
影响因子：
--
作者：
R. Lefkowitz
通讯作者：
R. Lefkowitz
维拉帕米和去甲维拉帕米与β-肾上腺素能受体的相互作用。
影响因子：
37.8
作者：
Feldman,RD;Park,GD;Lai,CY
通讯作者：
Lai,CY
通过磷脂脂肪酸的酶促修饰来调节分离的淋巴细胞质膜中的酶活性。
DOI：
10.1016/s0021-9258(19)68449-8
发表时间：
1981
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
M. Szamel;K. Resch
通讯作者：
K. Resch