蛋白质-配体相互作用：亚硝胺与烟碱型乙酰胆碱受体的相互作用

Protein-ligand interactions: interaction of nitrosamines with nicotinic acetylcholine receptor.

作者信息

Kapp E A, Daya S, Whiteley C G

机构信息

Department of Chemistry and Biochemistry, Rhodes University, Grahamstown, South Africa.

出版信息

Biochem Biophys Res Commun. 1990 Mar 30;167(3):1383-92. doi: 10.1016/0006-291x(90)90676-e.

DOI:10.1016/0006-291x(90)90676-e

PMID:2322280

Abstract

Fluorimetry and spectrophotometry have been used to study the binding of dimethyl, dipropyl, dibutyl and diphenylnitrosamine to nicotinic acetylcholine receptor isolated, and purified, from Torpedo fuscomaculata. Scatchard analysis indicates that all four ligands are true agonists of the receptor exhibiting positive cooperative binding with the existence of more than one class of binding site. The number of binding sites for the nitrosamines approximates 2. Diphenylnitrosamine binds to the receptor more tightly at low concentrations (Kd1 = 1.3 microM) than the aliphatic nitrosamine (Kd1 = 8-12 microM). Yet at high concentrations all nitrosamines behaved with similar Kd values (27-38 microM).

摘要

荧光分析法和分光光度法已被用于研究二甲基、二丙基、二丁基和二苯基亚硝胺与从黄斑电鳐分离并纯化的烟碱型乙酰胆碱受体的结合情况。斯卡查德分析表明，所有这四种配体都是该受体的真正激动剂，表现出正协同结合，存在不止一类结合位点。亚硝胺的结合位点数约为2个。在低浓度时（Kd1 = 1.3微摩尔），二苯基亚硝胺比脂肪族亚硝胺（Kd1 = 8 - 12微摩尔）与受体的结合更紧密。然而，在高浓度时，所有亚硝胺的Kd值相似（27 - 38微摩尔）。