| Literature DB >> 34043961 |
Ouma Onguka1, Brett M Babin1, Markus Lakemeyer1, Ian T Foe1, Neri Amara1, Stephanie M Terrell2, Kenneth M Lum3, Piotr Cieplak4, Micah J Niphakis3, Jonathan Z Long2, Matthew Bogyo5.
Abstract
The intracellular protozoan parasite Toxoplasma gondii must scavenge cholesterol and other lipids from the host to facilitate intracellular growth and replication. Enzymes responsible for neutral lipid synthesis have been identified but there is no evidence for enzymes that catalyze lipolysis of cholesterol esters and esterified lipids. Here, we characterize several T. gondii serine hydrolases with esterase and thioesterase activities that were previously thought to be depalmitoylating enzymes. We find they do not cleave palmitoyl thiol esters but rather hydrolyze short-chain lipid esters. Deletion of one of the hydrolases results in alterations in levels of multiple lipids species. We also identify small-molecule inhibitors of these hydrolases and show that treatment of parasites results in phenotypic defects reminiscent of parasites exposed to excess cholesterol or oleic acid. Together, these data characterize enzymes necessary for processing lipids critical for infection and highlight the potential for targeting parasite hydrolases for therapeutic applications.Entities:
Keywords: CDP-DAG; Plasmodium falciparum; Toxoplasma gondii; cholesterol; depalmitoylases; lipid metabolism; oleic acid; phosphatidic acid; serine hydrolases; α/β-hydrolase superfamily
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Year: 2021 PMID: 34043961 PMCID: PMC8542566 DOI: 10.1016/j.chembiol.2021.05.001
Source DB: PubMed Journal: Cell Chem Biol ISSN: 2451-9448 Impact factor: 9.039