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
Endocrinologyjournal_title
Endocrinologyauthors
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 JNdoi
10.1210/en.2007-1353subject
Has Abstractpub_date
2008-05-01 00:00:00pages
2080-9issue
5eissn
0013-7227issn
1945-7170pii
en.2007-1353journal_volume
149pub_type
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