Zhenjin Su, Fangming Liu, Yiyu Lin, Xinyu Hong, Haiying Cui, Rongjian Sun, Bin Qi
Prenylation is an important post-translational lipid modification that enhances protein hydrophobicity and regulates subcellular localization. It plays a critical role in multiple signaling pathways and metabolic processes and is closely associated with the development and progression of various diseases, particularly in tumor initiation, progression, and metastasis. However, its systemic regulatory roles and therapeutic vulnerabilities in cancer remain incompletely understood. In this review, we summarize the molecular mechanisms of protein prenylation and its biological functions, with a particular focus on its roles in tumorigenesis and tumor progression. We further discuss therapeutic strategies targeting prenylation, including both monotherapy and combination approaches. Overall, protein prenylation represents a key regulatory hub linking signal transduction, metabolic reprogramming, and tumorigenesis. Future studies should focus on elucidating the mechanisms underlying therapeutic response and resistance, as well as advancing clinical translation through biomarker development and well-designed clinical trials.