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Interaction of trifluoperazine with Tetrahymena calmodulin
[摘要]

We have used 19F NMR to study interactions of trifluoperazine (TFP), a potent calmodulin (CaM) antagonist, with Tetrahymena calmodulin (Tet. CaM). Changes in chemical shift and bandwidth of TFP caused by adding Tet. CaM in the presence of excess Ca2+ were much smaller than those by adding porcine CaM. The spectral features of the TFP—Tet. CaM solution in the presence of excess Ca2+ were quite similar to those of the TFP—porcine CaM solution in the absence of Ca2+. The exchange rate of TFP from Tet. CaM was estimated to be nearly 20 s−1. The TFP—Tet. CaM solution in the absence of Ca2+ showed a pronounced pH dependence of the 19F NMR chemical shift, whereas the solution in the presence of excess Ca2+ showed a smaller pH dependence. Thus, it was suggested that TFP is located near a hydrophilic region of the Tet. CaM molecule in the absence of Ca2+, while TFP is located near a hydrophobic region of the Tet. CaM in the presence of excess Ca2+.

[发布日期]  [发布机构] 
[效力级别]  [学科分类] 生物化学/生物物理
[关键词] Trifluoperazine;Tetrahymena;Calmodulin;19F NMR;Tet. CaM;calmodulin purified from Tetrahymena pyriformis;CaM;calmodulin;TFP;trifluoperazine;CD;circular dichroism;SIS;solvent-induced shift [时效性] 
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