Glucocorticoids are primary stress hormones that regulate a variety of physiologic processes and are essential for life. The actions of glucocorticoids are predominantly mediated through the classic glucocorticoid receptor (GR). GRs are expressed throughout the body, but there is considerable heterogeneity in glucocorticoid sensitivity and biologic responses across tissues. The conventional belief that glucocorticoids act through a single GR protein has changed dramatically with the discovery of a diverse collection of receptor isoforms. This article provides an overview of the molecular mechanisms that regulate glucocorticoid actions, highlights the dynamic nature of hormone signaling, and discusses the molecular properties of the GR isoforms.

Key points

  • An important challenge in the clinical application of glucocorticoids is the heterogeneity in glucocorticoid responsiveness among individuals with a significant portion of the population exhibiting some degree of glucocorticoid resistance.

  • Glucocorticoid sensitivity and specificity is influenced by GR isoform expression profile. Inflammatory and pathologic processes modulate cellular GR isoform profiles.

  • Assessing glucocorticoid sensitivity in individual patients is important for an optimal glucocorticoid treatment plan in the clinic.

  • Understanding the heterogeneity of GR signaling in health and disease aids in the development of safer and more effective glucocorticoid therapies with improved benefit/risk ratios for patients.

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Sep 28, 2017 | Posted by in RHEUMATOLOGY | Comments Off on Corticosteroids

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