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

Karolien De Bosscher UGent, Ilse Beck, Dariusz Ratman, Wim Vanden Berghe UGent and Claude Libert UGent (2016) TRENDS IN PHARMACOLOGICAL SCIENCES. 37(1). p.4-16
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.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (review)
publication status
published
subject
keyword
SEPTIC SHOCK, C-JUN, TARGET GENES, GENE-EXPRESSION, TRANSCRIPTION FACTORS, IN-VIVO, DNA-BINDING, DIMERIZATION, MECHANISMS, SEPSIS
journal title
TRENDS IN PHARMACOLOGICAL SCIENCES
Trends Pharmacol. Sci.
volume
37
issue
1
pages
4 - 16
Web of Science type
Review
Web of Science id
000368203600002
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
12.797 (2016)
JCR rank
5/256 (2016)
JCR quartile
1 (2016)
ISSN
0165-6147
DOI
10.1016/j.tips.2015.09.002
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
7073736
handle
http://hdl.handle.net/1854/LU-7073736
date created
2016-02-05 09:46:50
date last changed
2017-04-07 11:16:22
@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},
}

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.