Carnitine O-palmitoyltransferase 1, liver isoform (CPT1A)

Carnitine O-palmitoyltransferase 1, liver isoform (CPT1A), is an integral enzyme localized to the outer mitochondrial membrane and belongs to the carnitine acyltransferase family[2][1]. CPT1A catalyzes the transfer of long-chain fatty acyl groups from acyl-CoA to carnitine, enabling their transport into the mitochondrial matrix for beta-oxidation[1][7]. This process is the rate-limiting step in mitochondrial fatty acid oxidation, crucial for energy production during fasting and metabolic stress[7][2]. Malonyl-CoA acts as an allosteric inhibitor, providing key metabolic regulation. CPT1A is most highly expressed in the liver but also found in kidney, pancreas, and other tissues[7][3]. Genetic deficiency leads to impaired fatty acid oxidation and severe metabolic disturbances. CPT1A is an established therapeutic target in metabolic disease and cardiovascular research, though safety concerns limit clinical translation of enzyme inhibitors[8][1].

Other names

Carnitine palmitoyltransferase 1ACarnitine acyltransferase ICPTICAT1CoA:carnitine acyl transferase (CCAT)PalmitoylCoA transferase IL-CPT-1

Inhibition of CPT1A reduces mitochondrial fatty acid import and oxidation, shifting cellular energy substrate preference away from fatty acids Inhibition can increase glucose utilization, proposed to have cardioprotective/metabolic benefits in diabetes and heart failure[8][1]