Division of Pharmaceutical Sciences, University of Wisconsin, Madison, Wisconsin 53705-2222, USA.
J Biol Chem. 2010 Dec 10;285(50):38853-60. doi: 10.1074/jbc.M110.147744. Epub 2010 Oct 6.
Fredericamycin (FDM) A is a pentadecaketide natural product that features an amide linkage. Analysis of the fdm cluster from Streptomyces griseus ATCC 43944, however, failed to reveal genes encoding the types of amide synthetases commonly seen in natural product biosynthesis. Here, we report in vivo and in vitro characterizations of FdmV, an asparagine synthetase (AS) B-like protein, as an amide synthetase that catalyzes the amide bond formation in FDM A biosynthesis. This is supported by the findings that (i) inactivation of fdmV in vivo afforded the ΔfdmV mutant strain SB4027 that abolished FDM A and FDM E production but accumulated FDM C, a biosynthetic intermediate devoid of the characteristic amide linkage; (ii) FdmV in vitro catalyzes conversion of FDM C to FDM B, a known intermediate for FDM A biosynthesis (apparent K(m) = 162 ± 67 μM and k(cat) = 0.11 ± 0.02 min(-1)); and (iii) FdmV also catalyzes the amidation of FDM M-3, a structural analog of FDM C, to afford amide FDM M-6 in vitro, albeit at significantly reduced efficiency. Preliminary enzymatic studies revealed that, in addition to the common nitrogen sources (L-Gln and free amine) of class II glutamine amidotransferases (to which AS B belongs), FdmV can also utilize L-Asn as a nitrogen donor. The amide bond formation in FDM A biosynthesis is proposed to occur after C-8 hydroxylation but before the carbaspirocycle formation.
弗雷德里卡霉素(FDM)A 是一种十五元环肽天然产物,具有酰胺键。然而,对来自灰色链霉菌 ATCC 43944 的 fdm 簇的分析未能揭示出编码天然产物生物合成中常见的酰胺合成酶类型的基因。在这里,我们报告了 FdmV 的体内和体外特性,FdmV 是一种天冬酰胺合成酶(AS)B 样蛋白,作为酰胺合成酶,催化 FDM A 生物合成中的酰胺键形成。这一发现得到了以下发现的支持:(i)体内失活 fdmV 赋予了 ΔfdmV 突变株 SB4027,该突变株消除了 FDM A 和 FDM E 的产生,但积累了 FDM C,这是一种缺乏特征性酰胺键的生物合成中间体;(ii)FdmV 在体外催化 FDM C 转化为 FDM B,这是 FDM A 生物合成的已知中间体(表观 K(m) = 162 ± 67 μM 和 k(cat) = 0.11 ± 0.02 min(-1));(iii)FdmV 还催化 FDM M-3 的酰胺化,FDM M-3 是 FDM C 的结构类似物,在体外提供酰胺 FDM M-6,但效率明显降低。初步酶学研究表明,除了 AS B 所属的 II 类谷氨酰胺酰胺转移酶的常见氮源(L-Gln 和游离胺)外,FdmV 还可以利用 L-Asn 作为氮供体。FDM A 生物合成中的酰胺键形成发生在 C-8 羟化之后但在碳杂螺环形成之前。