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Characterization of ZK 245186, a novel, selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases
Author(s) -
Schäcke H,
Zollner TM,
Döcke WD,
Rehwinkel H,
Jaroch S,
Skuballa W,
Neuhaus R,
May E,
Zügel U,
Asadullah K
Publication year - 2009
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2009.00238.x
Subject(s) - glucocorticoid receptor , pharmacology , glucocorticoid , agonist , in vivo , cytokine , receptor , medicine , chemistry , immunology , biology , microbiology and biotechnology
Glucocorticoids are highly effective in the therapy of inflammatory diseases. Their value, however, is limited by side effects. The discovery of the molecular mechanisms of the glucocorticoid receptor and the recognition that activation and repression of gene expression could be addressed separately opened the possibility of achieving improved safety profiles by the identification of ligands that predominantly induce repression. Here we report on ZK 245186, a novel, non-steroidal, low-molecular-weight, glucocorticoid receptor-selective agonist for the topical treatment of inflammatory dermatoses.