Linked Life Data

21108268

Source:http://linkedlifedata.com/resource/pubmed/id/21108268

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
18
pubmed:dateCreated
2010-12-8
pubmed:abstractText
A series of 42 naturally occurring flavonoids and one flavonoid glucuronide were tested for their ability to inhibit p38? mitogen-activated protein kinase (p38?) and c-Jun-N-terminal kinase 3 (JNK3). Potent inhibitors with IC(50) values in the low micromolar range were identified. Structure-activity relationships were evaluated and the most promising compounds were docked into the ATP binding site of these kinases. Among the different classes of flavonoids, the flavonol group showed better inhibition of p38?. Of this class, kaempferol-7,4'-dimethylether was a potent p38? inhibitor, displaying 13-fold selectivity for p38? over JNK3. The flavone compounds without a 6-methoxy group preferentially inhibited JNK3. The flavone glycoside, luteolin-7-O-glycoside, was identified as a potent inhibitor with the greatest selectivity toward JNK3. In contrast, the flavanol compounds displayed similar inhibitory activities toward both kinases.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
1439-7633
pubmed:author
pubmed:issnType
Electronic
pubmed:day
10
pubmed:volume
11
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2579-88
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Biological evaluation and structural determinants of p38? mitogen-activated-protein kinase and c-Jun-N-terminal kinase 3 inhibition by flavonoids.
pubmed:affiliation
Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Eberhard Karls University of Tuebingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't