Deep-Sea Genome Mining Reveals Cooperative ATP-Grasp Ligase-Directed Biosynthesis of Pentacyclic Myxomiditides with Potent Protease Inhibition

深海基因组挖掘揭示了具有强效蛋白酶抑制作用的五环粘液霉素的协同ATP-Grasp连接酶导向生物合成

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Abstract

Microviridins are ribosomally synthesized and post-translationally modified peptides, typically featuring a conserved tricyclic structure formed by two ATP-grasp ligases. However, the diversity and evolution of these enzymes remain incompletely understood. Here, we identify a distinct ATP-grasp ligase subclade (MyxF) that specifically modifies the conserved (KxxE)(n) motif, defining a new subclass of microviridins with the (KxxE)(n)TxKxPSDx-(D/E)-(D/E) sequence signature. Guided by SSN analysis, we discovered a deep-sea myx biosynthetic gene cluster from 10,000 m sediments and heterologously expressed two pentacyclic microviridin-like peptides, Myxomiditide A and B. Using mass spectrometry and NMR, we fully elucidated their chemical structures, revealing not only the conserved tricyclic core but also two additional N-terminal lactam rings within the KxxEKxxE motif, distinguishing them from known microviridins. Combined in vivo coexpression and in vitro reconstitution uncovered a noncanonical division of labor among four ATP-grasp ligases involved in myxomiditide biosynthesis. MyxF and MyxD1 act as functional isozymes responsible for installation of the N-terminal lactam moieties, whereas MyxD2catalytically inactive on its ownrequires the synergistic presence of both MyxF and MyxD1 to enable formation of the C-terminal lactone rings. The pathway is finalized by MyxC, which catalyzes the terminal lactam macrocyclization, collectively revealing a highly cooperative enzymatic assembly mechanism governing myxomiditide maturation. Furthermore, MyxF exhibited remarkable catalytic plasticity, catalyzing multiple lactam macrocyclizations beyond its native substrate architecture. Notably, Myxomiditide A potently inhibited elastase with nanomolar IC(50) values. Collectively, this study expands the enzymatic landscape of ATP-grasp ligases and highlights the deep sea as a rich source of evolutionary innovation in RiPP biosynthesis.

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