Insights into Lasalocid A Ring Formation by Chemical Chain Termination In Vivo

Angewandte Chemie International Edition
2011.0

Abstract

To investigate the timing of epoxidation, aromatic ring formation, and the role of downstream epoxidase in the biosynthesis of lasalocid A (a polyether antibiotic from Streptomyces lasaliensis), we employed a chemical strategy using carba(dethia) mimics of malonyl units to intercept truncated biosynthetic intermediates from polyketide synthases (PKSs). Wild-type and engineered mutant strains (with deletions of epoxidase LasC/epoxide hydrolase LasB or point-mutated acyl carrier protein (ACP) domains) were grown in the presence of carba(dethia) N-acetyl cysteamine esters. Micro LC/HRMS analyses of bacterial extracts identified PKS-bound intermediates, including putative undecaketide dienes (8a–c), their oxidized counterparts (9a–c, 11a for ΔlasB mutants), and fully oxidized dodecaketide species (7a,b, 10a). These intermediates provide novel insights: epoxidation occurs on enzyme-bound substrates (likely ACP11/ACP10-bound precursors), aromatization may follow ether ring formation, and the epoxidase LasC is crucial for complete assembly of the polyketide backbone. This method of sampling PKS-bound intermediates in vivo advances understanding of lasalocid A ring formation mechanisms, particularly the relative timing of key biosynthetic steps and the role of downstream enzymes in polyketide processing.

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