Carnitine O-palmitoyltransferase 1 (CPT1) (CPT1)

Carnitine O-palmitoyltransferase 1 (CPT1) is a key regulatory enzyme located on the outer mitochondrial membrane that catalyzes the rate-limiting step of long-chain fatty acid beta-oxidation [UniProt]. It facilitates the conversion of long-chain acyl-CoAs into acylcarnitines, allowing them to be transported across the mitochondrial membranes via the carnitine shuttle system [StatPearls]. There are three tissue-specific isoforms: CPT1A (liver), CPT1B (muscle), and CPT1C (brain) [PubMed]. In diseases like type 2 diabetes and heart failure, modulating CPT1 activity can shift cellular energy metabolism from fatty acid oxidation to glucose oxidation, which is more oxygen-efficient [NCBI]. However, pharmacological inhibition of CPT1 has faced challenges due to side effects like hepatotoxicity and cardiotoxicity [DrugBank]. Recent research also highlights CPT1 as a potential target in various cancers where fatty acid oxidation supports rapid cell proliferation and survival [Nature Reviews Cancer].

Other names

Carnitine palmitoyltransferase ICPTICPT1-LCPT1-MCPT1-BCarnitine shuttle systemCarnitine O-palmitoyltransferase 1 / carnitine shuttle system

Inhibition of CPT1 activity to prevent the conversion of long-chain acyl-CoAs to acylcarnitines, thereby blocking their entry into the mitochondria for beta-oxidation and shifting cellular metabolism toward glucose oxidation.