期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 19, 页码 5811-5814出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.129
关键词
MIF; Inhibitor design; Protein-protein interactions; Cytokine; Inflammatory disease
资金
- Keck Biotechnology Facility
- National Institutes of Health [AIO42310, AR049610, AR050498, GM032136]
The cytokine MIF is involved in inflammation and cell proliferation via pathways initiated by its binding to the transmembrane receptor CD74. MIF also exhibits keto-enol tautomerase activity, believed to be vestigial in mammals. Starting from a 1 mu M hit from virtual screening, substituted benzoxazol-2-ones have been discovered as antagonists with IC50 values as low as 7.5 nM in a tautomerase assay and 80 nM in a MIF-CD74 binding assay. Additional studies for one of the potent inhibitors demonstrated that it is not a covalent inhibitor of MIF and that it attenuates MIF-dependent ERK1/2 phosphorylation in human synovial fibroblasts. (C) 2010 Elsevier Ltd. All rights reserved.
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