Title of article
Identification of dissociated non-steroidal glucocorticoid receptor agonists
Author/Authors
Daniel Kuzmich، نويسنده , , Tom Kirrane، نويسنده , , John Proudfoot، نويسنده , , Younes Bekkali، نويسنده , , Renee Zindell، نويسنده , , Laura Beck، نويسنده , , Richard Nelson، نويسنده , , Cheng-Kon Shih، نويسنده , , Alison J. Kukulka، نويسنده , , Zofia Paw، نويسنده , , Patty Reilly، نويسنده , , Rodney Deleon، نويسنده , , Mario Cardozo، نويسنده , , Gerald Nabozny، نويسنده , , David Thomson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
7
From page
5025
To page
5031
Abstract
A new series of ligands for the glucocorticoid receptor (GR) is described. SAR development was guided by docking 3 into the GR active site and optimizing an unsubstituted phenyl ring for key interactions found in the steroid A-ring binding pocket. To identify compounds with an improved side effect profile over marketed steroids the functional activity of compounds was evaluated in cell based assays for transactivation (aromatase) and transrepression (IL-6). Through this effort, 36 has been identified as a partial agonist with a dissociated profile in these cell based assays.
Keywords
aromatase , IL-6 , Glucocorticoid receptor , anti-inflammatory , Glucocorticoid receptor agonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798546
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