Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.

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Hudson AR, Higuchi RI, Roach SL, Valdez LJ, Adams ME, Vassar A, Rungta D, Syka PM, Mais DE, Marschke KB, Zhi L

Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1654-7. doi: 10.1016/j.bmcl.2011.01.104. Epub 2011 Jan 27.

PubMed ID
21324689 [ View in PubMed
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Abstract

Continuing studies based on dihydroquinoline glucocorticoid receptor agonists lead to the discovery of a series of C4-oxime analogs. Representative compounds exhibited potent transrepression activity with minimal transactivation of phosphoenolpyruvate caboxykinase (PEPCK), a key protein in the gluconeogenesis pathway. These compounds represent promising leads in identifying GR agonists with high anti-inflammatory activity and attenuated potential for glucose elevation.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PrednisoloneGlucocorticoid receptorEC 50 (nM)5.3N/AN/ADetails
PrednisoloneGlucocorticoid receptorKi (nM)5.3N/AN/ADetails
PrednisoloneGlucocorticoid receptorIC 50 (nM)4.1N/AN/ADetails
PrednisoloneGlucocorticoid receptorIC 50 (nM)23N/AN/ADetails
PrednisoloneGlucocorticoid receptorEC 50 (nM)26N/AN/ADetails