Elenewski Justin E, Hackett John C
Department of Physiology and Biophysics and The Massey Cancer Center, School of Medicine, Virginia Commonwealth University, 401 College Street, Richmond, Virginia 23219-1540, USA.
J Chem Phys. 2015 Feb 14;142(6):064307. doi: 10.1063/1.4907733.
The iron(IV)-oxo porphyrin π-cation radical known as Compound I is the primary oxidant within the cytochromes P450, allowing these enzymes to affect the substrate hydroxylation. In the course of this reaction, a hydrogen atom is abstracted from the substrate to generate hydroxyiron(IV) porphyrin and a substrate-centered radical. The hydroxy radical then rebounds from the iron to the substrate, yielding the hydroxylated product. While Compound I has succumbed to theoretical and spectroscopic characterization, the associated hydroxyiron species is elusive as a consequence of its very short lifetime, for which there are no quantitative estimates. To ascertain the physical mechanism underlying substrate hydroxylation and probe this timescale, ab initio molecular dynamics simulations and free energy calculations are performed for a model of Compound I catalysis. Semiclassical estimates based on these calculations reveal the hydrogen atom abstraction step to be extremely fast, kinetically comparable to enzymes such as carbonic anhydrase. Using an ensemble of ab initio simulations, the resultant hydroxyiron species is found to have a similarly short lifetime, ranging between 300 fs and 3600 fs, putatively depending on the enzyme active site architecture. The addition of tunneling corrections to these rates suggests a strong contribution from nuclear quantum effects, which should accelerate every step of substrate hydroxylation by an order of magnitude. These observations have strong implications for the detection of individual hydroxylation intermediates during P450 catalysis.
被称为化合物I的铁(IV)-氧代卟啉π-阳离子自由基是细胞色素P450中的主要氧化剂,使这些酶能够影响底物的羟基化反应。在该反应过程中,一个氢原子从底物上被夺取,生成羟基铁(IV)卟啉和一个以底物为中心的自由基。然后羟基自由基从铁原子反弹到底物上,生成羟基化产物。虽然化合物I已经通过理论和光谱表征得到了研究,但相关的羟基铁物种由于其极短的寿命而难以捉摸,目前尚无定量估计。为了确定底物羟基化反应背后的物理机制并探究这个时间尺度,我们对化合物I催化模型进行了从头算分子动力学模拟和自由能计算。基于这些计算的半经典估计表明,氢原子夺取步骤极其迅速,在动力学上与碳酸酐酶等酶相当。通过一组从头算模拟发现,生成的羟基铁物种寿命同样很短,在300飞秒到3600飞秒之间,推测这取决于酶活性位点的结构。对这些速率加上隧道效应校正表明核量子效应有很大贡献,这应该会使底物羟基化的每一步加速一个数量级。这些观察结果对在P450催化过程中检测单个羟基化中间体具有重要意义。