A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation

Cell Chemical Biology

Volumn 23, Issue 11, 2016, Pages 1362-1371

  Petersen, Donna N ^a   Hawkins, Julie ^a   Ruangsiriluk, Wanida ^a   Stevens, Kimberly A ^a   Maguire, Bruce A ^a   O'Connell, Thomas N ^a   Rocke, Benjamin N ^a   Boehm, Markus ^a   Ruggeri, Roger B ^a   Rolph, Tim ^a   Hepworth, David ^a   Loria, Paula M ^a   Carpino, Philip A ^a  

^a PFIZER INC   (United States)

Author keywords

anti secretagogue; high throughput screen (HTS); LDL; LDL receptor; PCSK9; phenotypic screening; R IMPP; ribosome; secretion; translation

Indexed keywords

ALKALINE PHOSPHATASE; COMPLEMENTARY DNA; G PROTEIN COUPLED RECEPTOR; LOW DENSITY LIPOPROTEIN CHOLESTEROL; LOW DENSITY LIPOPROTEIN RECEPTOR; MOLECULE TRANSPORT AGENT; MOTILIN RECEPTOR; N (ISOQUINOLIN 1 YL) 3 (4 METHOXYPHENYL) N (PIPERIDIN 3 YL)PROPANAMIDE; PROPROTEIN CONVERTASE SUBTILISIN KEXIN TYPE 9; PROTEIN; RIBOSOME RNA; RNA 80S; SIGNAL PEPTIDE; TRANSFERRIN; UNCLASSIFIED DRUG; ISOQUINOLINE DERIVATIVE; MOLECULAR LIBRARY; PCSK9 PROTEIN, HUMAN; PROPROTEIN CONVERTASE 9;

AMINO ACID SEQUENCE; ARTICLE; CARBOXY TERMINAL SEQUENCE; CELL LYSATE; CELL VIABILITY; CONTROLLED STUDY; CYTOTOXICITY; DRUG MECHANISM; ENANTIOMER; ESCHERICHIA COLI; GENE OVEREXPRESSION; HEPATOMA CELL; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; HYPERCHOLESTEROLEMIA; LIPID TRANSPORT; LUCIFERASE ASSAY; NONHUMAN; PHENOTYPE; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN SECRETION; PROTEIN SYNTHESIS; RIBOSOME; RNA TRANSLATION; WESTERN BLOTTING; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY; TUMOR CELL LINE;

CELL LINE, TUMOR; HUMANS; ISOQUINOLINES; PROPROTEIN CONVERTASE 9; PROTEIN BIOSYNTHESIS; RIBOSOMES; SMALL MOLECULE LIBRARIES;

EID: 84995776316     PISSN: 24519456     EISSN: 24519448     Source Type: Journal    
DOI: 10.1016/j.chembiol.2016.08.016     Document Type: Article

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