Binding of trifluoperazine and fluorene-containing compounds to calmodulin and adducts.
Binding of trifluoperazine and fluorene-containing compounds to calmodulin and adducts.
复制标题
三氟拉嗪和含芴化合物与钙调蛋白和加合物的结合。
DOI：
10.1016/0006-2952(86)90754-9
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发表时间：
1986
影响因子：
5.8
通讯作者：
Puett,D
中科院分区：
文献类型：
--
作者：
Jackson,AE;Puett,D
仅在Lys 75或在Lys 75和Lys 148，钙调素可以与含荧烯的疏水自旋标记试剂特异性地酰化。用Hummel-Dreyer程序测定了三氟拉嗪与钙调素和两个加合物的结合，发现吩噻嗪的结合具有明显的正协同性和明显的极限化学计量比，每个蛋白质分子约有7个结合位点。合成了两种非反应性的荧类化合物，两种试剂与钙调蛋白的结合比三氟拉嗪小得多。其中一个也被检测为与单标记加合物结合，这种结合大约是钙调蛋白观察到的一半，并且是非合作的。因此，疏水基团与钙调蛋白的定性和定量结合参数可能有很大不同。
Calmodulin can be specifically acylated with a fluorene-containing hydrophobic spin-labeling reagent at just Lys 75 or at Lys 75 and Lys 148. The binding of trifluoperazine to calmodulin and the two adducts was determined using a Hummel-Dreyer procedure, and binding of the phenothiazine was found to be characterized by apparent positive cooperativity and an apparent limiting stoichiometry of about seven binding sites per protein molecule. Two non-reactive fluorene-containing compounds were synthesized, and both reagents exhibited far less binding to calmodulin than did trifluoperazine. One of these was also assayed for binding to the monolabeled adduct, and this binding was about half that observed with calmodulin and was non-cooperative. Thus, the qualitative andquantitative binding parameters of hydrophobic groups to calmodulin can be quite different.