Cholinephosphotransferase 1 (CHPT1)

Cholinephosphotransferase 1 (CHPT1) is a critical integral membrane enzyme that catalyzes the final, committed step of the CDP-choline pathway, also known as the Kennedy pathway, for the de novo synthesis of phosphatidylcholine (PC) [UniProt: Q8WUD6]. PC is the most abundant phospholipid in eukaryotic cell membranes and is essential for structural integrity, intracellular signaling, and the production of lung surfactant [PubMed: 26563956]. The enzyme specifically facilitates the transfer of a phosphocholine group from CDP-choline to 1,2-diacylglycerol (DAG), yielding PC and CMP [NCBI Gene: 56994]. In the field of oncology, CHPT1 is frequently overexpressed in various malignancies, including breast and lung cancers, to support the high demand for membrane biogenesis required for rapid cell proliferation [PubMed: 31235865]. While CHPT1 represents a promising therapeutic target for inhibiting tumor growth, its fundamental role in normal cellular homeostasis and surfactant production presents significant challenges for achieving a favorable safety profile and therapeutic index [PubMed: 12145310, PubMed: 15132995].

Other names

Diacylglycerol cholinephosphotransferaseCDP-choline:1,2-diacylglycerol cholinephosphotransferaseCPT11,2-diacylglycerol cholinephosphotransferase

Inhibition of de novo phosphatidylcholine synthesis by blocking the transfer of the phosphocholine moiety from CDP-choline to 1,2-diacylglycerol.