Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
J Am Chem Soc. 2012 Jul 11;134(27):11261-8. doi: 10.1021/ja3038273. Epub 2012 Jun 29.
Enzymatic reactions typically involve complex dynamics during substrate binding, conformational rearrangement, chemistry, and product release. The noncovalent steps provide kinetic checkpoints that contribute to the overall specificity of enzymatic reactions. DNA polymerases perform DNA replication with outstanding fidelity by actively rejecting noncognate nucleotide substrates early in the reaction pathway. Substrates are delivered to the active site by a flexible fingers subdomain of the enzyme, as it converts from an open to a closed conformation. The conformational dynamics of the fingers subdomain might also play a role in nucleotide selection, although the precise role is currently unknown. Using single-molecule Förster resonance energy transfer, we observed individual Escherichia coli DNA polymerase I (Klenow fragment) molecules performing substrate selection. We discovered that the fingers subdomain actually samples through three distinct conformations--open, closed, and a previously unrecognized intermediate conformation. We measured the overall dissociation rate of the polymerase-DNA complex and the distribution among the various conformational states in the absence and presence of nucleotide substrates, which were either correct or incorrect. Correct substrates promote rapid progression of the polymerase to the catalytically competent closed conformation, whereas incorrect nucleotides block the enzyme in the intermediate conformation and induce rapid dissociation from DNA. Remarkably, incorrect nucleotide substrates also promote partitioning of DNA to the spatially separated 3'-5' exonuclease domain, providing an additional mechanism to prevent misincorporation at the polymerase active site. These results reveal the existence of an early innate fidelity checkpoint, rejecting incorrect nucleotide substrates before the enzyme encloses the nascent base pair.
酶反应通常在底物结合、构象重排、化学反应和产物释放过程中涉及复杂的动力学。非共价步骤提供了动力学检查点,有助于酶反应的整体特异性。DNA 聚合酶通过在反应途径的早期积极拒绝非互补核苷酸底物,以出色的保真度进行 DNA 复制。底物通过酶的柔性手指亚基传递到活性位点,因为它从开放构象转变为闭合构象。手指亚基的构象动力学也可能在核苷酸选择中发挥作用,尽管确切的作用目前尚不清楚。使用单分子Förster 共振能量转移,我们观察到单个大肠杆菌 DNA 聚合酶 I(Klenow 片段)分子进行底物选择。我们发现,手指亚基实际上会通过三种不同的构象进行采样——开放、闭合和以前未被识别的中间构象。我们测量了聚合酶-DNA 复合物的整体解离速率以及在有无核苷酸底物的情况下各种构象状态之间的分布,这些底物要么是正确的,要么是不正确的。正确的底物促进聚合酶快速进入催化活性的闭合构象,而不正确的核苷酸则将酶阻挡在中间构象中,并诱导其与 DNA 快速解离。值得注意的是,不正确的核苷酸底物还促进 DNA 向空间分离的 3'-5'核酸外切酶结构域的分配,为防止在聚合酶活性位点发生错误掺入提供了另一种机制。这些结果揭示了早期固有保真度检查点的存在,即在酶封闭新生碱基对之前拒绝不正确的核苷酸底物。