Yoo, Euna; Schulze, Christopher J.; Stokes, Barbara H.; Onguka, Ouma; Yeo, Tomas; Mok, Sachel; Gnadig, Nina F.; Zhou, Yani; Kurita, Kenji; Foe, Ian T.; Terrell, Stephanie M.; Boucher, Michael J.; Cieplak, Piotr; Kumpornsin, Krittikorn; Lee, Marcus C. S.; Linington, Roger G.; Long, Jonathan Z.; Uhlemann, Anne-Catrin; Weerapana, Eranthie; Fidock, David A.; Bogyo, Matthew published the artcile< The Antimalarial Natural Product Salinipostin A Identifies Essential α/β Serine Hydrolases Involved in Lipid Metabolism in P. falciparum Parasites>, Application In Synthesis of 96829-58-2, the main research area is Plasmodium falciparum; Salinipostin A; activity-based probes; chemical proteomics; lipid metabolism; malaria; natural products; serine hydrolases.
Salinipostin A (Sal A) is a potent antiplasmodial marine natural product with an undefined mechanism of action. Using a Sal A-derived activity-based probe, we identify its targets in the Plasmodium falciparum parasite. All of the identified proteins contain α/β serine hydrolase domains and several are essential for parasite growth. One of the essential targets displays a high degree of homol. to human monoacylglycerol lipase (MAGL) and is able to process lipid esters including a MAGL acylglyceride substrate. This Sal A target is inhibited by the anti-obesity drug Orlistat, which disrupts lipid metabolism Resistance selections yielded parasites that showed only minor reductions in sensitivity and that acquired mutations in a PRELI domain-containing protein linked to drug resistance in Toxoplasma gondii. This inability to evolve efficient resistance mechanisms combined with the non-essentiality of human homologs makes the serine hydrolases identified here promising antimalarial targets.
Cell Chemical Biology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics