Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor

Journal of Medicinal Chemistry

Volumn 51, Issue 3, 2008, Pages 380-383

  Zhao, Gang ^a   Souers, Andrew J ^a   Voorbach, Martin ^a   Falls, H Doug ^a   Droz, Brian ^a   Brodjian, Sevan ^a   Yau, Yi Lau ^a   Iyengar, Rajesh R ^a   Gao, Ju ^a   Judd, Andrew S ^a   Wagaw, Seble H ^a   Ravn, Matthew M ^a   Engstrom, Kenneth M ^a   Lynch, John K ^a   Mulhern, Mathew M ^a   Freeman, Jennifer ^a   Dayton, Brian D ^a   Wang, Xiaojun ^a   Grihalde, Nelson ^a   Fry, Dennis ^a   Beno, David W A ^a   Marsh, Kennan C ^a   Su, Z M ^a   Diaz, Gilbert J ^a   Collins, Christine A ^a   Sham, Hing ^b   Reilly, Regina M ^a   Brune, Michael E ^a   Kym, Philip R ^a   more..

^a ABBOTT LABORATORIES   (United States)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

ACYLTRANSFERASE INHIBITOR; CHYLOMICRON; DEXFENFLURAMINE; DIACYLGLYCEROLACYLTRANSFERASE 1 INHIBITOR; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; DYSLIPIDEMIA; ENZYME INHIBITION; MOUSE; NONHUMAN; OBESITY; STRUCTURE ACTIVITY RELATION; TRIACYLGLYCEROL BLOOD LEVEL; WEIGHT REDUCTION;

ANIMALS; ANTI-OBESITY AGENTS; ANTILIPEMIC AGENTS; BIPHENYL COMPOUNDS; CYCLOHEPTANES; DIACYLGLYCEROL O-ACYLTRANSFERASE; EATING; HUMANS; ISOENZYMES; KETO ACIDS; LIVER; MICE; MICE, MUTANT STRAINS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRIGLYCERIDES; UREA; WEIGHT LOSS;

EID: 39149122218     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm7013887     Document Type: Article

References (15)

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13. Cross-reactivity assays were performed by CEREP; www.cerep.com.
14. Liver triglycerides were determined on day 28 only.
15. The 30 mg/kg dose decreases the plasma triglyceride levels to those of the saline-gavaged animals. Thus, the percentage inhibition of the 0.3 and 3.0 mg/kg doses are relative to the 30 mg/kg dose.