| Autor: |
Zhao G; Metabolic Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA., Souers AJ, Voorbach M, Falls HD, Droz B, Brodjian S, Lau YY, Iyengar RR, Gao J, Judd AS, Wagaw SH, Ravn MM, Engstrom KM, Lynch JK, Mulhern MM, Freeman J, Dayton BD, Wang X, Grihalde N, Fry D, Beno DW, Marsh KC, Su Z, Diaz GJ, Collins CA, Sham H, Reilly RM, Brune ME, Kym PR |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2008 Feb 14; Vol. 51 (3), pp. 380-3. Date of Electronic Publication: 2008 Jan 10. |
| DOI: |
10.1021/jm7013887 |
| Abstrakt: |
A highly potent and selective DGAT-1 inhibitor was identified and used in rodent models of obesity and postprandial chylomicron excursion to validate DGAT-1 inhibition as a novel approach for the treatment of metabolic diseases. Specifically, compound 4a conferred weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depleted serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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