2. Academic Validation
  3. Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation

Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation

  • Bioorg Med Chem Lett. 2011 Mar 15;21(6):1658-62. doi: 10.1016/j.bmcl.2011.01.106.
Steven L Roach 1,  Robert I Higuchi,  Andrew R Hudson,  Angie Vassar,  Virginia H S Grant,  Ryan Lamer,  Charlene Hooper,  Deepa Rungta,  Peter M Syka,  Dale E Mais,  Keith B Marschke,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. sroach@ligand.com
PMID: 21349714 DOI: 10.1016/j.bmcl.2011.01.106
Abstract

Continuing studies on tetrahydroquinoline Glucocorticoid Receptor anti-inflammatory agents lead to the identification of several tetrahydroquinolin-3-yl carbamates that exhibited steroid-like activity in in vitro transrepression assays with reduced transactivation of phosphoenol pyruvate carboxykinase (PEPCK), a key Enzyme in the gluconeogenesis pathway.

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