2008
DOI: 10.1177/1087057108319738
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A High-Throughput Screen for Endothelial Lipase Using HDL as Substrate

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Cited by 19 publications
(9 citation statements)
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“…Recently, an indirect assay for EL activity has been described using HDL as a substrate by monitoring the liberation of free fatty acids in coupled enzymatic and detection reactions ( 39 ). Even though this assay incorporates HDL, which is the more physiologically relevant substrate for EL, the complex coupled reactions it requires would make analyses of the mode of inhibition diffi cult and thus inappropriate for guiding chemical optimization of small molecule inhibitors of EL.…”
Section: Discussionmentioning
confidence: 99%
“…Recently, an indirect assay for EL activity has been described using HDL as a substrate by monitoring the liberation of free fatty acids in coupled enzymatic and detection reactions ( 39 ). Even though this assay incorporates HDL, which is the more physiologically relevant substrate for EL, the complex coupled reactions it requires would make analyses of the mode of inhibition diffi cult and thus inappropriate for guiding chemical optimization of small molecule inhibitors of EL.…”
Section: Discussionmentioning
confidence: 99%
“…With this in mind, we next investigated the potential of targeting FA synthesis and exogenous FA uptake simultaneously using our FASNi compound 41 and GSK264220A, a urea-based inhibitor of lipoprotein lipase (LPL) and endothelial lipase (Keller et al, 2008;Nomura and Casida, 2016). LPL is the major enzyme for extracellular hydrolysis of triglyceride transported in lipoprotein particles, and thus renders this source of FAs accessible to cells (Kuemmerle et al, 2011;Kinlaw et al, 2016).…”
Section: Synthesismentioning
confidence: 99%
“…We hypothesized that supplementing LPL at the time of DiI-VLDL uptake would increase lipoprotein binding and internalization by BC cells, and found that this was, in fact the case. Addition of bovine LPL (1 µg/mL) significantly increased DiI-VLDL uptake by MDA-MB-231 cells, and was unaffected by treatment with GSK264220A (GSK), an inhibitor of the catalytic activity of LPL [47,48] (Figure 7A). This significant increase in DiI-VLDL uptake upon LPL supplementation was observed across BC cell lines (Figure 7B), albeit with variability potentially related to differences in basal LPL expression (BT-474 highest, MDA-MB-231; MCF-7 and T47-D as non-expressing cells).…”
Section: Lpl Supplementation Increases Dii-vldl Uptake In Bc Cell Linesmentioning
confidence: 99%