Shi She-Po, Wanibuchi Kiyofumi, Morita Hiroyuki, Endo Kohei, Noguchi Hiroshi, Abe Ikuro
School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka 422-8526, Japan.
Org Lett. 2009 Feb 5;11(3):551-4. doi: 10.1021/ol802606w.
A C(19) hexaketide stilbene and a C(21) heptaketide chalcone were synthesized by Aloe arborescens octaketide synthase (OKS), a plant-specific type III polyketide synthase (PKS). Remarkably, the C(21) chalcone-forming activity was dramatically increased in a structure-guided OKS N222G mutant that produces a C(20) decaketide SEK15 from 10 molecules of malonyl-CoA. The findings suggested further strategies for production of unnatural polyketides by combination of the precursor-directed biosynthesis and the structure-guided engineering of type III PKS.
一种C(19)六酮基二苯乙烯和一种C(21)七酮基查耳酮由木立芦荟八酮合成酶（OKS）合成，OKS是一种植物特有的III型聚酮合酶（PKS）。值得注意的是，在一个结构导向的OKS N222G突变体中，C(21)查耳酮形成活性显著提高，该突变体可从10分子丙二酰辅酶A产生C(20)十酮基SEK15。这些发现为通过前体导向生物合成与III型PKS的结构导向工程相结合来生产非天然聚酮提供了进一步的策略。
