Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile.

ABSTRACT:

Background and purpose

Glucocorticoids are highly effective therapies for a range of inflammatory diseases. Advances in the understanding of the diverse molecular mechanisms underpinning glucocorticoid action suggest that anti-inflammatory molecules with reduced side effect liabilities can be discovered. Here we set out to explore whether modification of the 17α position of the steroid nucleus could generate molecules with a unique pharmacological profile and to determine whether such molecules would retain anti-inflammatory activity.

Experimental approach

The pharmacological properties of GW870086 were compared with fluticasone propionate (FP) using a range of cellular and in vivo model systems, including extensive gene expression profiling.

Key results

GW870086 repr

SUBMITTER: Uings IJ 

PROVIDER: S-EPMC3831715 | biostudies-literature | 2013 Jul

REPOSITORIES: biostudies-literature