| Literature DB >> 27213958 |
Michael J Genin1, Isabel C Gonzalez Valcarcel1, William G Holloway1, Jason Lamar1, Marian Mosior1, Eric Hawkins1, Thomas Estridge1, Jeffrey Weidner1, Thomas Seng1, David Yurek1, Lisa A Adams1, Jennifer Weller1, Vincent L Reynolds1, Joseph T Brozinick1.
Abstract
To develop novel treatments for type 2 diabetes and dyslipidemia, we pursued inhibitors of serine palmitoyl transferase (SPT). To this end compounds 1 and 2 were developed as potent SPT inhibitors in vitro. 1 and 2 reduce plasma ceramides in rodents, have a slight trend toward enhanced insulin sensitization in DIO mice, and reduce triglycerides and raise HDL in cholesterol/cholic acid fed rats. Unfortunately these molecules cause a gastric enteropathy after chronic dosing in rats.Entities:
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Year: 2016 PMID： 27213958 DOI： 10.1021/acs.jmedchem.5b01851
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446