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Phosphatidylcholine-Specific Phospholipase C as a Promising Drug Target

Eurtivong, Chatchakorn; Leung, Euphemia; Sharma, Nabangshu; Leung, Ivanhoe K. H.; Reynisson, Jóhannes


Chatchakorn Eurtivong

Euphemia Leung

Nabangshu Sharma

Ivanhoe K. H. Leung


Philippe M. Loiseau


Phosphatidylcholine-specific phospholipase C (PC-PLC) is an enzyme that catalyzes the formation of the important secondary messengers phosphocholine and diacylglycerol (DAG) from phosphatidylcholine. Although PC-PLC has been linked to the progression of many pathological conditions, including cancer, atherosclerosis, inflammation and neuronal cell death, studies of PC-PLC on the protein level have been somewhat neglected with relatively scarce data. To date, the human gene expressing PC-PLC has not yet been found, and the only protein structure of PC-PLC that has been solved was from Bacillus cereus (PC-PLCBc). Nonetheless, there is evidence for PC-PLC activity as a human functional equivalent of its prokaryotic counterpart. Additionally, inhibitors of PC-PLCBc have been developed as potential therapeutic agents. The most notable classes include 2-aminohydroxamic acids, xanthates, N, N′-hydroxyureas, phospholipid analogues, 1,4-oxazepines, pyrido[3,4-b]indoles, morpholinobenzoic acids and univalent ions. However, many medicinal chemistry studies lack evidence for their cellular and in vivo effects, which hampers the progression of the inhibitors towards the clinic. This review outlines the pathological implications of PC-PLC and highlights current progress and future challenges in the development of PC-PLC inhibitors from the literature.

Journal Article Type Article
Acceptance Date Jul 24, 2023
Online Publication Date Jul 25, 2023
Deposit Date Aug 14, 2023
Journal Molecules
Publisher MDPI
Peer Reviewed Peer Reviewed
Volume 28
Issue 15
Pages 5637
Keywords atherosclerosis, drug discovery, cancer, inhibitors, inflammation