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抑制性腺苷受体的特异性光亲和标记

Specific photoaffinity labelling of inhibitory adenosine receptors.

作者信息

Choca J I, Kwatra M M, Hosey M M, Green R D

出版信息

Biochem Biophys Res Commun. 1985 Aug 30;131(1):115-21. doi: 10.1016/0006-291x(85)91778-4.

DOI:10.1016/0006-291x(85)91778-4
PMID:2994642
Abstract

N6(L-phenylisopropyl)adenosine (L-PIA) and N6(3-iodo-4-azido benzyl)-adenosine (IAzBA) inhibit the adenylate cyclase activity in synaptic membranes of chick cerebellum via Ri adenosine receptors. [3H]L-PIA and [125I]AzBA bind to these membranes with Kd values of approximately 1 nM and Bmax values of approximately 1000 fmol/mg protein. Photolysis of [125I]AzBA bound to synaptic membranes results in the specific incorporation of radioactivity into a protein with Mr = 36,000. This photoincorporation is blocked by simultaneous exposure to L-PIA, theophylline, an adenosine receptor antagonist, or Gpp(NH)p, but not by cytosine, suggesting that the 36,000 dalton protein is the Ri adenosine receptor or a subunit of the receptor that contains the adenosine binding site.

摘要

N6-(L-苯异丙基)腺苷(L-PIA)和N6-(3-碘-4-叠氮苄基)腺苷(IAzBA)通过Ri型腺苷受体抑制鸡小脑突触膜中的腺苷酸环化酶活性。[3H]L-PIA和[125I]AzBA与这些膜结合,其解离常数(Kd)值约为1 nM,最大结合量(Bmax)值约为1000 fmol/mg蛋白质。与突触膜结合的[125I]AzBA经光解后,放射性特异性掺入一种分子量为36,000的蛋白质中。同时暴露于L-PIA、茶碱(一种腺苷受体拮抗剂)或鸟苷-5'-O-(3-硫代三磷酸)(Gpp(NH)p)可阻断这种光掺入,但胞嘧啶不能阻断,这表明36,000道尔顿的蛋白质是Ri型腺苷受体或包含腺苷结合位点的受体亚基。

相似文献

1
Specific photoaffinity labelling of inhibitory adenosine receptors.抑制性腺苷受体的特异性光亲和标记
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引用本文的文献

1
International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update.国际基础和临床药理学联合会。CXII:腺苷受体:进一步更新。
Pharmacol Rev. 2022 Apr;74(2):340-372. doi: 10.1124/pharmrev.121.000445.
2
A new high affinity, iodinated adenosine receptor antagonist as a radioligand/photoaffinity crosslinking probe.一种新型高亲和力碘化腺苷受体拮抗剂,用作放射性配体/光亲和交联探针。
Mol Pharmacol. 1987 Aug;32(1):184-8.
3
Hydrodynamic properties of adenosine Ri receptors solubilized from rat cerebral-cortical membranes.
从大鼠大脑皮层膜中溶解出的腺苷 Ri 受体的流体动力学特性。
Biochem J. 1987 Dec 15;248(3):635-42. doi: 10.1042/bj2480635.
4
Target size of the adenosine Ri receptor.腺苷 Ri 受体的靶标大小。
Biochem J. 1986 Apr 15;235(2):621-4. doi: 10.1042/bj2350621.
5
N6-functionalized congeners of adenosine with high potency at A2-adenosine receptors: potential ligands for affinity chromatography.在A2-腺苷受体上具有高效能的腺苷N6-官能化类似物:亲和色谱的潜在配体
Biochem Biophys Res Commun. 1986 May 14;136(3):1097-102. doi: 10.1016/0006-291x(86)90446-8.
6
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.腺苷受体:药理学、构效关系及治疗潜力
J Med Chem. 1992 Feb 7;35(3):407-22. doi: 10.1021/jm00081a001.
7
Adenosine A1 and A2 receptors: structure--function relationships.腺苷A1和A2受体:结构-功能关系
Med Res Rev. 1992 Sep;12(5):423-71. doi: 10.1002/med.2610120502.