Wang Menghua, Wei Zi-Wang, Ryan Katherine S
Department of Chemistry, The University of British Columbia, Vancouver, British Columbia, Canada.
Nat Chem Biol. 2025 May 1. doi: 10.1038/s41589-025-01898-0.
Negamycin, a hydrazine-containing dipeptide-like antibiotic, was first isolated in 1970 from three strains of Streptomyces purpeofuscus. Its pronounced antibacterial properties render it an appealing candidate for combating multi-drug-resistant Gram-negative bacteria. Additionally, the unique readthrough-promoting activity makes it a subject for research as a potential therapeutic agent for Duchenne muscular dystrophy and other hereditary diseases. Here we use the unusual (R)-β-lysine found in negamycin as a guide to identify the biosynthetic pathway of negamycin and then carry out gene deletion and chemical complementation, stable isotope feeding and enzyme assays to elucidate the key precursors for negamycin assembly. Our work identified NegB as a lysine-2,3-aminomutase that converts lysine into (R)-β-lysine and NegJ as a heme-dependent, N-N bond-forming enzyme. We show that NegJ, together with a ferredoxin encoded outside of the negamycin gene cluster, directly forms hydrazinoacetic acid from glycine and nitrite. NegJ is a novel biocatalyst for N-N bond formation, and our work highlights its potential for genome mining of N-N bond-containing natural products.
Negamycin是一种含肼的二肽类抗生素,于1970年首次从三株紫色链霉菌中分离出来。其显著的抗菌特性使其成为对抗多重耐药革兰氏阴性菌的有吸引力的候选药物。此外,其独特的通读促进活性使其成为作为杜氏肌营养不良症和其他遗传性疾病潜在治疗剂研究的对象。在这里,我们以Negamycin中发现的不寻常的(R)-β-赖氨酸为指导,确定Negamycin的生物合成途径,然后进行基因缺失和化学互补、稳定同位素标记和酶分析,以阐明Negamycin组装的关键前体。我们的工作确定NegB为一种赖氨酸-2,3-氨基变位酶,可将赖氨酸转化为(R)-β-赖氨酸,NegJ为一种依赖血红素的、形成N-N键的酶。我们表明,NegJ与Negamycin基因簇外编码的一种铁氧化还原蛋白一起,直接从甘氨酸和亚硝酸盐形成肼基乙酸。NegJ是一种用于形成N-N键的新型生物催化剂,我们的工作突出了其在含N-N键天然产物基因组挖掘中的潜力。