rdf:type |
|
lifeskim:mentions |
umls-concept:C0005456,
umls-concept:C0060441,
umls-concept:C0182400,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0243071,
umls-concept:C0332256,
umls-concept:C0700287,
umls-concept:C1257890,
umls-concept:C1707689,
umls-concept:C1883254,
umls-concept:C2603343
|
pubmed:issue |
8
|
pubmed:dateCreated |
2005-3-22
|
pubmed:abstractText |
Flavone-8-acetic acid (FAA) is a potent immunomodulatory small molecule that is uniquely characterized as being active on mouse but not human cells. Although FAA is a potent inducer of murine cytokine, chemokine and interferon gene expression, its mode of action remains unknown. In this report, we describe the synthesis of a new flavone acetic acid (FAA) analogue, (2-[2-(4-azidophenyl)-4-oxochromen-8-yl-]acetic acid (compound 2). We demonstrate that compound 2 is equally active as the parent FAA in inducing chemokine gene expression and that the azide functional group is capable of reacting with a reporter molecule, such as the FLAG peptide-phosphine, under mild conditions. This reaction will be useful for detecting the drug-bound protein active complex utilizing an anti-FLAG antibody.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
0968-0896
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
15
|
pubmed:volume |
13
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2717-22
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:15781383-Animals,
pubmed-meshheading:15781383-Azides,
pubmed-meshheading:15781383-Binding Sites,
pubmed-meshheading:15781383-Cell Line,
pubmed-meshheading:15781383-Chemokines,
pubmed-meshheading:15781383-Drug Design,
pubmed-meshheading:15781383-Flavonoids,
pubmed-meshheading:15781383-Gene Expression,
pubmed-meshheading:15781383-Macrophages,
pubmed-meshheading:15781383-Mice,
pubmed-meshheading:15781383-Mice, Inbred C57BL,
pubmed-meshheading:15781383-Molecular Structure,
pubmed-meshheading:15781383-Peptides,
pubmed-meshheading:15781383-Phosphines,
pubmed-meshheading:15781383-RNA,
pubmed-meshheading:15781383-Structure-Activity Relationship
|
pubmed:year |
2005
|
pubmed:articleTitle |
Synthesis and biological study of a flavone acetic acid analogue containing an azido reporting group designed as a multifunctional binding site probe.
|
pubmed:affiliation |
Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute-Frederick, Center for Cancer Research, Frederick, MD 21702-1201, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|