Centro de Biología Molecular Severo Ochoa (UAM-CSIC). Facultad de Ciencias. Universidad Autónoma de Madrid, Madrid, Spain.
Methods Mol Biol. 2023;2704:313-328. doi: 10.1007/978-1-0716-3385-4_19.
Manufactured steroid compounds have many applications in the pharmaceutical industry. Due to the chemical complexity and chirality of steroids, there is an increasing demand for enzyme-based bioconversion processes to replace those based on chemical synthesis. In this context, thermostability of the involved enzymes is a highly desirable property as both the increased half-life of the enzyme and the enhanced solubility of substrates and products will improve the yield of the reactions. Metagenomic libraries from thermal environments are potential sources of thermostable enzymes of prokaryotic origin, but the number of expected hits could be quite low for enzymes handling substrates such as steroids, rarely found in prokaryotes. An alternative to metagenome screening is the selection of thermostable variants of well-known steroid-processing enzymes. Here we review and detail a protocol for such selection, where error-prone PCR (epPCR) is used to introduce random mutations into a gene to create a variants library for further selection of thermostable variants in the thermophile Thermus thermophilus. The method involves the use of folding interference vectors where the proper folding of the enzyme of interest at high temperature is linked to the folding of a reporter encoding a selectable property such as thermostable resistance to kanamycin, leading to a life-or-death selection of variants of reinforced folding independently of the activity of the enzyme.
人工合成的甾体化合物在制药工业中有许多应用。由于甾体的化学复杂性和手性,越来越需要基于酶的生物转化过程来替代基于化学合成的过程。在这种情况下,所涉及的酶的热稳定性是一个非常理想的特性,因为酶的半衰期延长和底物及产物的溶解度提高都会提高反应的产率。来自热环境的宏基因组文库是具有原核来源的耐热酶的潜在来源,但对于处理甾体等很少在原核生物中发现的底物的酶,预期的命中数可能相当低。宏基因组筛选的一种替代方法是选择已知的甾体处理酶的耐热变体。在这里,我们回顾并详细介绍了这样一种选择的方案,其中易错 PCR(epPCR)用于将随机突变引入基因中,以创建一个变体文库,然后在嗜热菌 Thermus thermophilus 中进一步选择耐热变体。该方法涉及使用折叠干扰载体,其中感兴趣的酶在高温下的正确折叠与报告基因的折叠相关联,该报告基因编码一种可选择的特性,如对卡那霉素的耐热抗性,从而导致折叠增强变体的生死选择,而与酶的活性无关。