Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor

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

doi:10.1021/jm7013887

journal article Open Access Jan 10, 2008

Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor

Gang Zhao

Andrew J. Souers Martin Voorbach H. Doug Falls Brian Droz Sevan Brodjian Yau Yi Lau Rajesh R. Iyengar Ju Gao

Andrew S. Judd Seble H. Wagaw Matthew M. Ravn Kenneth M. Engstrom

John K. Lynch Mathew M. Mulhern Jennifer Freeman

Brian D. Dayton Xiaojun Wang

Nelson Grihalde Dennis Fry David W. A. Beno Kennan C. Marsh Zhi Su Gilbert J. Diaz Christine A. Collins Hing Sham Regina M. Reilly Michael E. Brune Philip R. Kym

Journal of Medicinal Chemistry Vol. 51 No. 3 pp. 380-383 · American Chemical Society (ACS)

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Cross-reactivity assays were performed by CEREP;www.cerep.com.

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Liver triglycerides were determined on day 28 only.

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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.

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Details

Published: Jan 10, 2008
Vol/Issue: 51(3)
Pages: 380-383

Authors

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Gang Zhao