R-IMPP is a potent and selective inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) secretion that stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP binds selectively to human ribosomes and causes transcript-dependent inhibition of PCSK9 translation.
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Cell chemical biology, 23(11), 1362-1371 (2016-10-18)
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secreted protein that downregulates low-density lipoprotein (LDL) receptor (LDL-R) levels on the surface of hepatocytes, resulting in decreased clearance of LDL-cholesterol (LDL-C). Phenotypic screening of a small-molecule compound collection was used to identify an
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