LGD-5552, an antiinflammatory glucocorticoid receptor ligand with reduced side effects, in vivo.

Abstract:

:Treatment of inflammation is often accomplished through the use of glucocorticoids. However, their use is limited by side effects. We have examined the activity of a novel glucocorticoid receptor ligand that binds the receptor efficiently and strongly represses inflammatory gene expression. This compound has potent antiinflammatory activity in vivo and represses the transcription of the inflammatory cytokine monocyte chemoattractant protein-1 and induces the antiinflammatory cytokine IL-10. The compound demonstrates differential gene regulation, compared with commonly prescribed glucocorticoids, effectively inducing some genes and repressing others in a manner different from the glucocorticoid prednisolone. The separation between the antiinflammatory effects of LGD-5552 and the side effects commonly associated with glucocorticoid treatment suggest that this molecule differs significantly from prednisolone and other steroids and may provide a safer therapeutic window for inflammatory conditions now commonly treated with steroidal glucocorticoids.

journal_name

Endocrinology

journal_title

Endocrinology

authors

López FJ,Ardecky RJ,Bebo B,Benbatoul K,De Grandpre L,Liu S,Leibowitz MD,Marschke K,Rosen J,Rungta D,Viveros HO,Yen WC,Zhi L,Negro-Vilar A,Miner JN

doi

10.1210/en.2007-1353

subject

Has Abstract

pub_date

2008-05-01 00:00:00

pages

2080-9

issue

5

eissn

0013-7227

issn

1945-7170

pii

en.2007-1353

journal_volume

149

pub_type

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