Fluorescence studies of the beta-adrenergic receptor topology.
Fluorescence studies of the beta-adrenergic receptor topology.
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β-肾上腺素能受体拓扑结构的荧光研究。
DOI：
10.1021/bi00518a007
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发表时间：
1981
期刊：
影响因子：
2.9
通讯作者：
J. Zadunaisky
中科院分区：
文献类型：
--
作者：
B. Cherksey;R. Murphy;J. Zadunaisky
利用普萘洛尔的内源荧光作为探针，研究了β-肾上腺素能受体的普萘洛尔结合位点的性质。此外，普萘洛尔结合位点和膜色氨酸之间的空间关系已被检查通过利用I-猝灭的固有色氨酸荧光，膜色氨酸的化学修饰，和单重态之间的单重态能量转移膜结合普萘洛尔和色氨酸。普萘洛尔，在特定的β-受体结合的浓度一致，保护约42%的膜色氨酸荧光从I-淬灭。此外，在普萘洛尔的存在下，表观猝灭常数（kq）从3.6到21.8 M-1。在存在和不存在普萘洛尔的情况下，膜碎片与2-羟基-5-硝基苄基溴（Koshland试剂I）的反应表明，低浓度的普萘洛尔保护约45%的膜色氨酸不受试剂的影响。用敏化发射光谱法测定了色氨酸与普萘洛尔的单重态-单重态能量转移。这两个物种之间的距离被发现小于20 A。这些结果已被解释为表明，普萘洛尔，当结合到β-肾上腺素能受体，是这样定位的，其萘基部分插入到一个富含色氨酸的疏水口袋的受体。
The nature of the propranolol binding site of the beta-adrenergic receptor has been examined by utilizing the intrinsic fluorescence of propranolol as a probe. Additionally, the spatial relationship between the propranolol binding site and membrane tryptophan has been examined by utilizing I-quenching of intrinsic tryptophan fluorescence, chemical modification of membrane tryptophan, and singlet-singlet energy transfer between membrane-bound propranolol and tryptophan. Propranolol, at concentrations consistent with specific beta-receptor binding, protected approximately 42% of the membrane tryptophan fluorescence from I-quenching. Further, in the presence of propranolol, the apparent quenching constant (kq) was altered from 3.6 to 21.8 M-1. Reaction of the membrane fragments with 2-hydroxy-5-nitrobenzyl bromide (Koshland's reagent I) in the presence and absence of propranolol indicated that low concentrations of propranolol protected approximately 45% of the membrane tryptophan from the reagent. The singlet-singlet energy transfer from tryptophan to propranolol was determined by sensitized emission. The distance between these two species was found to be less than 20 A. These results have been interpreted to indicate that propranolol, when bound to the beta-adrenergic receptor, is situated such that its naphthyl moiety is inserted into a tryptophan-rich hydrophobic pocket of the receptor.
光响应 N 混合液晶，介电常数可实现 10^4 至 10^2 的剧烈变化
DOI：
--
发表时间：
2019
期刊：
影响因子：
--
作者：
森川響二朗;竹内智章;北森武彦;西川浩矢
通讯作者：
西川浩矢