Department of Life Science and Biochemical Engineering, Sun Moon University, 70 Sunmoon-ro 221, Tangjeong-myeon, Asan-si, 31460, Chungnam, Republic of Korea.
Department of Pharmaceutical Engineering and Biotechnology, Sun Moon University, 70 Sunmoon-ro 221, Tangjeong-myeon, Asan-si, 31460, Chungnam, Republic of Korea.
Microb Cell Fact. 2019 Aug 13;18(1):137. doi: 10.1186/s12934-019-1184-z.
Actinobacteria are characterized as the most prominent producer of natural products (NPs) with pharmaceutical importance. The production of NPs from these actinobacteria is associated with particular biosynthetic gene clusters (BGCs) in these microorganisms. The majority of these BGCs include polyketide synthase (PKS) or non-ribosomal peptide synthase (NRPS) or a combination of both PKS and NRPS. Macrolides compounds contain a core macro-lactone ring (aglycone) decorated with diverse functional groups in their chemical structures. The aglycon is generated by megaenzyme polyketide synthases (PKSs) from diverse acyl-CoA as precursor substrates. Further, post-PKS enzymes are responsible for allocating the structural diversity and functional characteristics for their biological activities. Macrolides are biologically important for their uses in therapeutics as antibiotics, anti-tumor agents, immunosuppressants, anti-parasites and many more. Thus, precise genetic/metabolic engineering of actinobacteria along with the application of various chemical/biological approaches have made it plausible for production of macrolides in industrial scale or generation of their novel derivatives with more effective biological properties. In this review, we have discussed versatile approaches for generating a wide range of macrolide structures by engineering the PKS and post-PKS cascades at either enzyme or cellular level in actinobacteria species, either the native or heterologous producer strains.
放线菌的特征是最主要的天然产物(NPs)生产者,具有药物重要性。这些放线菌的 NPs 的产生与这些微生物中特定的生物合成基因簇(BGCs)有关。这些 BGC 中的大多数包含聚酮合酶(PKS)或非核糖体肽合酶(NRPS)或两者的组合。大环内酯类化合物含有一个核心大环内酯环(糖苷),其化学结构中带有不同的官能团。糖苷由不同的酰基辅酶 A 作为前体底物,由巨型酶聚酮合酶(PKSs)生成。此外,PKS 后的酶负责分配结构多样性和功能特征,以发挥其生物活性。大环内酯类化合物因其在治疗学中的应用而具有重要的生物学意义,如抗生素、抗肿瘤剂、免疫抑制剂、抗寄生虫药等。因此,通过对放线菌进行精确的遗传/代谢工程以及应用各种化学/生物学方法,使其能够在工业规模上生产大环内酯类化合物或产生具有更有效生物学特性的新型衍生物。在这篇综述中,我们讨论了通过工程化 PKS 和 PKS 后级联酶或细胞水平,在天然或异源生产菌株的放线菌物种中,产生广泛的大环内酯结构的多种方法,无论是在酶还是细胞水平上。