Chlorogenic acid(CGA)is an important phenolic acid secondary metabolite widely found in plant kingdom. CGA plays an important role in plant growth and development, resistance to biotic and abiotic stresses. In addition, it has a multiple biological activities and pharmacological functions, and plays an important role in application potential in anti-inflammatory, antibacterial and hypoglycemic. However, the content of CGA is usually very low in plants, which seriously restricts its development and utilization values. Therefore, effectively improving CGA content in plants is particularly crucial. Recently, many researchers have made important advances on improving the CGA content in plants by genetic engineering, stress and hormone treatment. On this basis, researchers have also initiated new explorations on the biosynthesis of CGA and its molecular mechanism. This would provide new ideas for improving the CGA content in plants. In view of this, this paper reviews the research progresses on the structure and function, biosynthesis and regulation of CGA, and systematically analyzes the effects of key rate-limiting enzymes, such as PAL, C4H and 4CL, is involved in the synthesis of CGA. Moreover, we elucidate the role of transcription factors MYB, WRKY and bHLH in regulating the biosynthesis of CGA. Meanwhile, we comprehensively summarize the effects of exogenous factors, e.g., biotic/abiotic stresses, plant hormones, light quality and photoperiod on the CGA content and biosynthesis in plants,and introduce the mechanism of CGA in improving animal and human health. Finally, we explore and prospect the unsolved problems and future research directions in the CGA. It is aimed to offer some valuable references for the rational development and utilization of CGA and the improvement of crop resistance.