Penicillin is a kind ofβ-lactam drug which has been applied in the clinical treatment firstly in the world, and it has still been widely used at present. The synthesis and regulation mechanism of Penicillium chrysogenum, which is used to produce penicillin, has been studied quite maturely, but its proteomics research started relatively late and fewer reports were published. This paper reviews the synthesis and application of penicillin, transformation of Penicillium chrysogenum, and the research progress of its proteomics. On this basis, the study highlights the advantages of proteomics in the research of protein expression.