Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals

Journal of Pharmacology and Experimental Therapeutics

Volumn 326, Issue 3, 2008, Pages 801-808

  Hawkins, Julie L ^a   Robbins, Michael D ^a   Warren, Laurie C ^a   Xia, Donghui ^a   Petras, Stephen F ^a   Valentine, James J ^a   Varghese, Alison H ^a   Wang, Ing Kae ^a   Subashi, Timothy A ^a   Shelly, Lorraine D ^a   Hay, Bruce A ^a   Landschulz, Katherine T ^a,b   Geoghegan, Kieran F ^a   Harwood Jr , H James ^a,c  

^a PFIZER INC   (United States)

^b ELI LILLY AND COMPANY   (United States)

^c Delphi BioMedical Consultants LLC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

25 HYDROXYCHOLESTEROL; CHOLESTEROL; FATTY ACID; FATTY ACID SYNTHASE; HYDROXYMETHYLGLUTARYL COENZYME A SYNTHASE; LACTATE DEHYDROGENASE; LOW DENSITY LIPOPROTEIN RECEPTOR; LUCIFERASE; PF 429242; PROPROTEIN CONVERTASE 1; SERINE PROTEINASE; SERINE PROTEINASE INHIBITOR; SREBP SITE 1 PROTEASE; STEROL REGULATORY ELEMENT BINDING PROTEIN; STEROL REGULATORY ELEMENT BINDING PROTEIN 2; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; MEMBRANE-BOUND TRANSCRIPTION FACTOR PEPTIDASE, SITE 1; PROTEINASE INHIBITOR;

AMINO ACID SEQUENCE; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CELL STRAIN HEK293; CELL STRAIN HEPG2; CHO CELL; CHOLESTEROL SYNTHESIS; CONTROLLED STUDY; DIABETES MELLITUS; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG CYTOTOXICITY; DRUG STRUCTURE; DYSLIPIDEMIA; FATTY ACID SYNTHESIS; GENE EXPRESSION; HUMAN; HUMAN CELL; IC 50; LIPOGENESIS; METABOLIC SYNDROME X; MOUSE; NONHUMAN; OBESITY; PRIORITY JOURNAL; PROTEIN PROCESSING; REPORTER GENE; TATA BOX; TRANSCRIPTION REGULATION; WESTERN BLOTTING; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOSYNTHESIS; CELL CULTURE; CELL LINE; CHEMISTRY; CHO CELL LINE; COMPARATIVE STUDY; CRICETULUS; DOSE RESPONSE; DRUG EFFECTS; GENE EXPRESSION REGULATION; GENETICS; HAMSTER; MALE; METABOLISM; PHYSIOLOGY;

ANIMALS; CELL LINE; CELLS, CULTURED; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; GENE EXPRESSION REGULATION, ENZYMOLOGIC; HUMANS; LIPOGENESIS; MALE; MICE; PROPROTEIN CONVERTASES; PROTEASE INHIBITORS; PROTEIN PROCESSING, POST-TRANSLATIONAL; SERINE ENDOPEPTIDASES; STEROL REGULATORY ELEMENT BINDING PROTEINS;

EID: 53849135232     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.108.139626     Document Type: Article

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