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L A SM O N O S US A N T O
POSGRADUATE BIOMEDICAL SCIENCE
UNIVERSITY SUMATERA UTARA
FACULTY OF MEDICINE
LUCOCORTICOSTEROIDS:
MECHANISM ACTION
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glucocorticoids,
corticosteroidsGlucocorticosteroids
steroids
Introduction
most effective anti-inflammatorytherapy for asthma
yet are relatively ineffectivein chronic obstructive
pulmonary disease
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Glucocorticoids suppress inflammation viaseveral molecular mechanisms
suppress the multiple inflammatory genes
reversing histone acetylation of activatedinflammatory genes
binding of ligand-bound glucocorticoid receptors (GR) toco-activator molecules
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recruitment ofhistonedeacetylase-2 tothe activatedinflammatory genetranscriptioncomplex
(transrepression)
higher concentrations ofglucocorticoids GRhomodimers interact withDNA recognition sites toactivate transcription
increased histoneacetylation ofanti-inflammatory
genes andtranscription ofseveral geneslinked toglucocorticoidside effects(trans-activation).
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CONCLUSION
Glucocorticoids most effective therapy forcontrolling asthma and suppress airwayinflammation
Antiinflammatory effects of corticosteroidsare due to transactivation of anti-inflammatory genes
The recognition different molecular mechanismsof glucocorticoid resistance has identified newtherapeutic
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Peter J. Barnes British Journal of Pharmacology (2011) 163 29–43
References:
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