Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093, United States.
ACS Chem Biol. 2023 Sep 15;18(9):2014-2022. doi: 10.1021/acschembio.3c00238. Epub 2023 Sep 6.
Carrier-protein-dependent metabolic pathways biosynthesize fatty acids, polyketides, and non-ribosomal peptides, producing metabolites with important pharmaceutical, environmental, and industrial properties. Recent findings demonstrate that these pathways rely on selective communication mechanisms involving protein-protein interactions (PPIs) that guide enzyme reactivity and timing. While rational design of these PPIs could enable pathway design and modification, this goal remains a challenge due to the complex nature of protein interfaces. Computational methods offer an encouraging avenue, though many score functions fail to predict experimental observables, leading to low success rates. Here, we improve upon the Rosetta score function, leveraging experimental data through iterative rounds of computational prediction and mutagenesis, to design a hybrid fatty acid-non-ribosomal peptide initiation pathway. By increasing the weight of the electrostatic score term, the computational protocol proved to be more predictive, requiring fewer rounds of iteration to identify mutants with high in vitro activity. This allowed efficient design of new PPIs between a non-ribosomal peptide synthetase adenylation domain, PltF, and a fatty acid synthase acyl carrier protein, AcpP, as validated by activity and structural studies. This method provides a promising platform for customized pathway design, establishing a standard for carrier-protein-dependent pathway engineering through PPI optimization.
载体蛋白依赖的代谢途径生物合成脂肪酸、聚酮化合物和非核糖体肽,产生具有重要药物、环境和工业特性的代谢物。最近的研究结果表明,这些途径依赖于选择性的通讯机制,包括涉及酶反应性和时间的蛋白质-蛋白质相互作用(PPIs)。虽然这些 PPIs 的合理设计可以实现途径的设计和修饰,但由于蛋白质界面的复杂性,这一目标仍然是一个挑战。计算方法提供了一个有希望的途径,尽管许多评分函数未能预测实验可观察到的结果,导致成功率较低。在这里,我们通过迭代的计算预测和突变分析,利用实验数据改进了 Rosetta 评分函数,设计了一种混合脂肪酸-非核糖体肽起始途径。通过增加静电评分项的权重,计算方案被证明更具预测性,需要更少的迭代次数来识别具有高体外活性的突变体。这使得在非核糖体肽合成酶腺苷酸化结构域 PltF 和脂肪酸合成酶酰基载体蛋白 AcpP 之间设计新的 PPI 变得高效,这通过活性和结构研究得到了验证。该方法为定制途径设计提供了一个有前途的平台,通过 PPI 优化为载体蛋白依赖的途径工程建立了标准。