Chitin, an essential component of the cell wall, exists widely in pathogenic fungi. Chitin synthase (CHS) is a key enzyme for biosynthesis of chitin, and its activity is strictly regulated; therefore it can be inferred that CHS and its regulation factors are potential targets of anti-fungal therapy. This article reviews the recent research progress on classification, function, and regulation of CHS, and discusses the possibilities of using CHS and its regulation factors as anti-fungal targets.