Kandaswamy Jayachithra, Hariharan Parameswaran, Kumar Thallapuranam Krishnaswamy Suresh, Yu Chin, Lu Ta-Jung, Chin Der-Hang
Department of Chemistry, National Chung Hsing University, Taichung 40227, Taiwan, ROC.
Anal Biochem. 2008 Oct 1;381(1):18-26. doi: 10.1016/j.ab.2008.06.017. Epub 2008 Jun 14.
Most conjugate proteins undergo both conformational and stability changes on ligand removal. When architecture remains unchanged in the protein holo and apo forms, it is uncertain whether the protein stability also remains unaltered in both of the forms. Neocarzinostatin (NCS), a chromoprotein possessing a potent enediyne chromophore stands for such an instance. Protein-chromophore interaction has not been thoroughly explored previously due to a lack of strategies to independently and simultaneously monitor changes in the NCS conjugates. Here we report a method by which one can detect the signal exclusively from only one of the NCS conjugates without the spectral interference from the other. Stability of the NCS protein is significantly correlated to the protein-bound chromophore, irrespective of denaturation by heat, pH, urea, or ethanol. Despite the similarity in protein backbone conformation, protein stability of the NCS holo form diminishes and equalizes to that of the apo form when the chromophore is released and degraded. Although the enediyne chromophore is highly unstable, it intriguingly protects the protein by which it is protected. Significant mutual reliance between the carrier protein and its naturally associated ligand unveils important information on the NCS drug stability.
大多数结合蛋白在去除配体后会发生构象和稳定性变化。当蛋白质全酶形式和脱辅基形式的结构保持不变时,尚不确定这两种形式下蛋白质稳定性是否也保持不变。新制癌菌素(NCS),一种具有强效烯二炔发色团的色蛋白,就是这样一个例子。由于缺乏独立且同时监测NCS结合物变化的策略,蛋白质 - 发色团相互作用此前尚未得到充分探索。在此我们报告一种方法,通过该方法可以仅从一种NCS结合物中检测信号,而不受另一种结合物的光谱干扰。NCS蛋白的稳定性与结合在蛋白质上的发色团显著相关,无论热、pH、尿素或乙醇引起的变性如何。尽管蛋白质主链构象相似,但当发色团释放并降解时,NCS全酶形式的蛋白质稳定性降低并与脱辅基形式的稳定性相等。尽管烯二炔发色团高度不稳定,但有趣的是它能保护与之结合的蛋白质。载体蛋白与其天然相关配体之间存在显著的相互依赖性,这揭示了有关NCS药物稳定性的重要信息。