Motivation: The design of enzymes is as challenging as it is consequential for making chemical synthesis in medical and industrial applications more efficient, cost-effective and environmentally friendly. While several aspects of this complex problem are computationally assisted, the drafting of catalytic mechanisms, i.e. the specification of the chemical steps-and hence intermediate states-that the enzyme is meant to implement, is largely left to human expertise. The ability to capture specific chemistries of multi-step catalysis in a fashion that enables its computational construction and design is therefore highly desirable and would equally impact the elucidation of existing enzymatic reactions whose mechanisms are unknown. Results: We use the mathematical framework of graph transformation to express the distinction between rules and reactions in chemistry. We derive about 1000 rules for amino acid side chain chemistry from the M-CSA database, a curated repository of enzymatic mechanisms. Using graph transformation we are able to propose hundreds of hypothetical catalytic mechanisms for a large number of unrelated reactions in the Rhea database. We analyze these mechanisms to find that they combine in chemically sound fashion individual steps from a variety of known multi-step mechanisms, showing that plausible novel mechanisms for catalysis can be constructed computationally.
翻译:激励: 酶的设计既具有挑战性,也具有使医学和工业应用中的化学合成更有效率、成本效益更高和环保性更有利于环境的影响。虽然这一复杂问题的几个方面得到了计算方面的协助,但起草催化机制,即具体化学步骤以及酶要执行的中间状态-基本上由人类专门知识决定。能够捕捉多步骤催化的具体化学,使其能进行计算构造和设计,因此是非常可取的,同样会影响现有各种机制未知的酶反应的解析。结果:我们使用图表转换的数学框架来表达化学规则和反应之间的区别。我们从M-CSA数据库(一个固化的酶机制储存库)中得出大约1000条关于氨酸链化学的规则。我们可以用图表转换为Rhea数据库中大量不相干的反应提出数以百计的假设催化机制。我们分析了这些机制,以便发现它们能够从各种已知的多步机制中以化学方式将单个步骤结合起来。我们从各种已知的多步机制中得出了可信的新模型。