Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.
Article Details
- CitationCopy to clipboard
Roach SL, Higuchi RI, Hudson AR, Vassar A, Grant VH, Lamer R, Hooper C, Rungta D, Syka PM, Mais DE, Marschke KB, Zhi L
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. Epub 2011 Jan 27.
- PubMed ID
- 21349714 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Prednisolone Glucocorticoid receptor EC 50 (nM) 5.3 N/A N/A Details Prednisolone Glucocorticoid receptor Ki (nM) 5.3 N/A N/A Details Prednisolone Glucocorticoid receptor IC 50 (nM) 4.1 N/A N/A Details Prednisolone Glucocorticoid receptor IC 50 (nM) 23 N/A N/A Details Prednisolone Glucocorticoid receptor EC 50 (nM) 26 N/A N/A Details