Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.

@article{SerranoWu2012IntestinallyTD,
  title={Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.},
  author={Michael H. Serrano-Wu and G. Coppola and Y. Gong and A. Neubert and R. Chatelain and K. B. Clairmont and R. Commerford and Theresa Cosker and Thomas G Daniels and Ying Hou and Monish Jain and Marlene Juedes and Lisha Li and Tara L Mullarkey and Erik C. Rocheford and M. Sung and A. Tyler and Qing Yang and T. Yoon and B. Hubbard},
  journal={ACS medicinal chemistry letters},
  year={2012},
  volume={3 5},
  pages={
          411-5
        }
}
High DGAT1 expression levels in the small intestine highlight the critical role this enzyme plays in nutrient absorption. Identification of inhibitors which predominantly inhibit DGAT1 in the gut is an attractive drug discovery strategy with anticipated benefits of reduced systemic toxicity. In this report we describe our discovery and optimization of DGAT1 inhibitors whose plasma exposure is minimized by the action of transporters, including the P-glycoprotein transporter. The impact of this… Expand
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