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Hepatol Commun. 2017 May 12;1(4):311-325. doi: 10.1002/hep4.1042. eCollection 2017 Jun.

CAT-2003: A novel sterol regulatory element-binding protein inhibitor that reduces steatohepatitis, plasma lipids, and atherosclerosis in apolipoprotein E*3-Leiden mice.

Hepatology communications

Michael Zimmer, Pradeep Bista, Ericka L Benson, Diana Y Lee, Feng Liu, Dominic Picarella, Rick B Vega, Chi B Vu, Maisy Yeager, Min Ding, Guosheng Liang, Jay D Horton, Robert Kleemann, Teake Kooistra, Martine C Morrison, Peter Y Wielinga, Jill C Milne, Michael R Jirousek, Andrew J Nichols

Affiliations

  1. Catabasis Pharmaceuticals Cambridge MA.
  2. Department of Molecular Genetics University of Texas Southwestern Medical Center at Dallas Dallas TX.
  3. Department of Internal Medicine University of Texas Southwestern Medical Center at Dallas Dallas TX.
  4. Center for Human Nutrition University of Texas Southwestern Medical Center at Dallas Dallas TX.
  5. Netherlands Organization for Applied Scientific Research, Department of Metabolic Health Research Leiden the Netherlands.

PMID: 29404461 PMCID: PMC5721391 DOI: 10.1002/hep4.1042

Abstract

CAT-2003 is a novel conjugate of eicosapentaenoic acid (EPA) and niacin designed to be hydrolyzed by fatty acid amide hydrolase to release EPA inside cells at the endoplasmic reticulum. In cultured liver cells, CAT-2003 blocked the maturation of sterol regulatory element-binding protein (SREBP)-1 and SREBP-2 proteins and decreased the expression of multiple SREBP target genes, including

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