Laboratory of Molecular and Bioinformatics Modeling, Department of Exact and Biological Sciences (DECEB), Universidade Federal de São João Del-Rei, Campus Sete Lagoas, Sete Lagoas 35701-970, Brazil.
Laboratory of Bioinformatics and Systems (LBS), Department of Computer Science, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, Brazil.
Molecules. 2019 Sep 4;24(18):3215. doi: 10.3390/molecules24183215.
β-Glucosidases are enzymes with high importance for many industrial processes, catalyzing the last and limiting step of the conversion of lignocellulosic material into fermentable sugars for biofuel production. However, β-glucosidases are inhibited by high concentrations of the product (glucose), which limits the biofuel production on an industrial scale. For this reason, the structural mechanisms of tolerance to product inhibition have been the target of several studies. In this study, we performed in silico experiments, such as molecular dynamics (MD) simulations, free energy landscape (FEL) estimate, Poisson-Boltzmann surface area (PBSA), and grid inhomogeneous solvation theory (GIST) seeking a better understanding of the glucose tolerance and inhibition mechanisms of a representative GH1 β-glucosidase and a GH3 one. Our results suggest that the hydrophobic residues Y180, W350, and F349, as well the polar one D238 act in a mechanism for glucose releasing, herein called "slingshot mechanism", dependent also on an allosteric channel (AC). In addition, water activity modulation and the protein loop motions suggest that GH1 β-Glucosidases present an active site more adapted to glucose withdrawal than GH3, in consonance with the GH1s lower product inhibition. The results presented here provide directions on the understanding of the molecular mechanisms governing inhibition and tolerance to the product in β-glucosidases and can be useful for the rational design of optimized enzymes for industrial interests.
β-葡萄糖苷酶在许多工业过程中具有重要意义,可催化木质纤维素材料转化为可发酵糖用于生物燃料生产的最后且具有限制作用的步骤。然而,β-葡萄糖苷酶会被产物(葡萄糖)的高浓度抑制,这限制了工业规模的生物燃料生产。出于这个原因,对耐受产物抑制的结构机制进行了几项研究。在这项研究中,我们进行了分子动力学 (MD) 模拟、自由能景观 (FEL) 估计、泊松-玻尔兹曼表面积 (PBSA) 和非均匀网格溶剂化理论 (GIST) 等计算实验,旨在更好地了解代表性 GH1β-葡萄糖苷酶和 GH3 酶的葡萄糖耐受和抑制机制。我们的结果表明,疏水性残基 Y180、W350 和 F349 以及极性残基 D238 参与了一种称为“弹弓机制”的葡萄糖释放机制,该机制还依赖于变构通道 (AC)。此外,水活性调节和蛋白质环运动表明,GH1β-葡萄糖苷酶的活性位点更适合葡萄糖的脱离,而 GH3 则不适合,这与 GH1s 对产物的抑制作用较低相一致。这里提出的结果为理解β-葡萄糖苷酶中产物抑制和耐受的分子机制提供了方向,并且对于工业利益的优化酶的合理设计可能是有用的。