LAUSR

Simple Summary The protein kinase C (PKC) family belongs to serine-threonine kinases and consists of several subtypes. Increasing evidence suggests that PKCs are critical players in carcinogenesis. Interestingly, PKCs exert both promotive and suppressive effects on tumor cell growth and metastasis, which have attracted immense attention. Herein, we systematically review the current advances in the structure, regulation and biological functions of PKCs, especially the relationship of PKCs with anti-cancer therapy-induced cell death, including the current knowledge of PKCs function in tumor metabolism and microenvironment. Moreover, we discuss the potential role of PKCs as a target for therapeutic intervention in cancer from basic research and clinical trials. Abstract Protein kinase C (PKC) isoforms, a group of serine-threonine kinases, are important regulators in carcinogenesis. Numerous studies have demonstrated that PKC isoforms exert both positive and negative effects on cancer cell demise. In this review, we systematically summarize the current findings on the architecture, activity regulation and biological functions of PKCs, especially their relationship with anti-cancer therapy-induced cell death. Additionally, we elaborate on current knowledge of the effects of PKCs on tumor metabolism and microenvironment, which have gained increasing attention in oncology-related areas. Furthermore, we underscore the basic experimental and clinical implications of PKCs as a target for cancer therapy to evaluate their therapeutic benefits and potential applications.