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ASTHMA AND COPD: MECHANISM OF ACTION OF GLUCOCORTICOIDS, β2-AGONISTS AND THEIR COMBINATION
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Introduction
 
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Combination Therapy With LABAs and ICSs: Scientific Rationale > Molecular interaction (asthma and COPD) >
Effects of β2-agonists on glucocorticosteroids receptors (GRs)
Effects of β2-agonists on glucocorticosteroids receptors (GRs)

As regards LABAs’ effects on GRs, they have been suggested to prime GRs and affect their nuclear localisation.

In fact β2-agonists seem to favour, via specific phosphorylating enzyme called mitogen-activated protein kinases (MAPKs), the phosporylation of particular aminoacids of GRs. This process induces conformational modifications of GRs that increase receptor sensitivity to steroid-dependent activation.13

In addition, other studies have demonstrated that translocation of GRs from the cytosol to the nucleus of the cell, a fundamental step in the anti-inflammatory activity of corticosteroids, is increased by the addition of a LABA.14,15

β2-agonists may also increase the sensitivity of the molecular pathways that are utilised by corticosteroids to suppress inflammation.

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