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Activation of the glucocorticoid receptor in acute inflammation : the SEDIGRAM concept

Karolien De Bosscher (UGent) , Ilse Beck (UGent) , Dariusz Ratman (UGent) , Wim Vanden Berghe (UGent) and Claude Libert (UGent)
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Abstract
Since the 1950s, glucocorticoids (GCs) have been a mainstay therapy for acute and chronic inflammatory disorders, although adverse effects limit their chronic use. Following the notion that the anti-inflammatory therapeutic and metabolic endocrine adverse effects of GCs may be based on different glucocorticoid receptor (GR)-dependent mechanisms, subsequent attempts to separate these mechanisms by trying to develop selective GR agonists and modulators (SEGRAMs) with an improved therapeutic benefit have yielded only a few molecules effective in clinical use. Recent new insights into the pro- and anti-inflammatory activities of GR support a more sophisticated drug discovery model. Here, we suggest that the way forward may include a need to redefine the pharmacological SEGRAM concept into selective monomerizing GR agonists and modulators (SEMOGRAMs) and selective dimerizing GR agonists or modulators (SEDIGRAMs) for selective therapeutic applications against chronic or acute inflammatory disorders, respectively.
Keywords
SEPTIC SHOCK, C-JUN, TARGET GENES, GENE-EXPRESSION, TRANSCRIPTION FACTORS, IN-VIVO, DNA-BINDING, DIMERIZATION, MECHANISMS, SEPSIS

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Chicago
De Bosscher, Karolien, Ilse Beck, Dariusz Ratman, Wim Vanden Berghe, and Claude Libert. 2016. “Activation of the Glucocorticoid Receptor in Acute Inflammation : the SEDIGRAM Concept.” Trends in Pharmacological Sciences 37 (1): 4–16.
APA
De Bosscher, K., Beck, I., Ratman, D., Vanden Berghe, W., & Libert, C. (2016). Activation of the glucocorticoid receptor in acute inflammation : the SEDIGRAM concept. TRENDS IN PHARMACOLOGICAL SCIENCES, 37(1), 4–16.
Vancouver
1.
De Bosscher K, Beck I, Ratman D, Vanden Berghe W, Libert C. Activation of the glucocorticoid receptor in acute inflammation : the SEDIGRAM concept. TRENDS IN PHARMACOLOGICAL SCIENCES. 2016;37(1):4–16.
MLA
De Bosscher, Karolien, Ilse Beck, Dariusz Ratman, et al. “Activation of the Glucocorticoid Receptor in Acute Inflammation : the SEDIGRAM Concept.” TRENDS IN PHARMACOLOGICAL SCIENCES 37.1 (2016): 4–16. Print.
@article{7073736,
  abstract     = {Since the 1950s, glucocorticoids (GCs) have been a mainstay therapy for acute and chronic inflammatory disorders, although adverse effects limit their chronic use. Following the notion that the anti-inflammatory therapeutic and metabolic endocrine adverse effects of GCs may be based on different glucocorticoid receptor (GR)-dependent mechanisms, subsequent attempts to separate these mechanisms by trying to develop selective GR agonists and modulators (SEGRAMs) with an improved therapeutic benefit have yielded only a few molecules effective in clinical use. Recent new insights into the pro- and anti-inflammatory activities of GR support a more sophisticated drug discovery model. Here, we suggest that the way forward may include a need to redefine the pharmacological SEGRAM concept into selective monomerizing GR agonists and modulators (SEMOGRAMs) and selective dimerizing GR agonists or modulators (SEDIGRAMs) for selective therapeutic applications against chronic or acute inflammatory disorders, respectively.},
  author       = {De Bosscher, Karolien and Beck, Ilse and Ratman, Dariusz and Vanden Berghe, Wim and Libert, Claude},
  issn         = {0165-6147},
  journal      = {TRENDS IN PHARMACOLOGICAL SCIENCES},
  keyword      = {SEPTIC SHOCK,C-JUN,TARGET GENES,GENE-EXPRESSION,TRANSCRIPTION FACTORS,IN-VIVO,DNA-BINDING,DIMERIZATION,MECHANISMS,SEPSIS},
  language     = {eng},
  number       = {1},
  pages        = {4--16},
  title        = {Activation of the glucocorticoid receptor in acute inflammation : the SEDIGRAM concept},
  url          = {http://dx.doi.org/10.1016/j.tips.2015.09.002},
  volume       = {37},
  year         = {2016},
}

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