期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 24, 页码 5769-5776出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.10.037
关键词
RORc; ROR gamma; ROR gamma t; IL-17; Inflammation; X-ray structure
资金
- National Institutes of Health
- National Institute of General Medical Sciences
- Office of Science, Office of Basic Energy Sciences
- U. S. Department of Energy [DE-AC02-05CH11231]
The identification of a new series of RORc inverse agonists is described. Comprehensive structure-activity relationship studies of this reversed sulfonamide series identified potent RORc inverse agonists in biochemical and cellular assays which were also selective against a panel of nuclear receptors. Our work has contributed a compound that may serve as a useful in vitro tool to delineate the complex biological pathways involved in signalling through RORc. An X-ray co-crystal structure of an analogue with RORc has also provided useful insights into the binding interactions of the new series. (C) 2014 Elsevier Ltd. All rights reserved.
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