Lipid metabolism involves multiple biological processes. As one of the most important
lipid metabolic pathways,
fatty acid oxidation (FAO) and its key rate-limiting
enzyme, the
carnitine palmitoyltransferase (
CPT) system, regulate host immune responses and thus are of great clinical significance. The effect of the
CPT system on different tissues or organs is complex: the deficiency or over-activation of
CPT disrupts the immune homeostasis by causing energy metabolism disorder and inflammatory oxidative damage and therefore contributes to the development of various acute and chronic inflammatory disorders and
cancer. Accordingly, agonists or antagonists targeting the
CPT system may become novel approaches for the treatment of diseases. In this review, we first briefly describe the structure, distribution, and physiological action of the
CPT system. We then summarize the pathophysiological role of the
CPT system in
chronic obstructive pulmonary disease,
bronchial asthma,
acute lung injury,
chronic granulomatous disease,
nonalcoholic fatty liver disease, hepatic
ischemia-reperfusion injury, kidney
fibrosis,
acute kidney injury, cardiovascular disorders, and
cancer. We are also concerned with the current knowledge in either preclinical or clinical studies of various
CPT activators/inhibitors for the management of diseases. These compounds range from traditional Chinese medicines to novel nanodevices. Although great efforts have been made in studying the different kinds of
CPT agonists/antagonists, only a few pharmaceuticals have been applied for clinical uses. Nevertheless, research on
CPT activation or inhibition highlights the pharmacological modulation of
CPT-dependent FAO, especially on different
CPT isoforms, as a promising anti-inflammatory/antitumor therapeutic strategy for numerous disorders.