2, 4-diacetylphloroglucinol (2,4-DAPG) is secondary metabolites produced by soil rhizophsere bacterium Pseudomonas fluorescens with ability to against bacteria,fungi, oomycetes and nematodes. Pseudomonas aeruginos is considered to be one cause of nosocomial infection due to its multi-drug resistance. We found aromatic polyketide antibiotic2,4-DAPG promotes the expression ofmultidrug efflux pumpsgenes pltIJK by blocking the interaction between pltI promoter andTetR family transcription factor PltZin P. aeruginosa; and our proteomics data estsblished thatPltZ is involved in diverse physiological process including metabolism of amino acids, biosynthesis of virulence factors, motility, ion transporting, carbohydrate and lipid transporting.We described asophisticated ATP-binding cassette(ABC)transportsystems regulation mechanismwhich affords insights into the role ofaromatic polyketide antibiotics.