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Drug-Target Interaction

Drug

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PubChem ID:5280445
Structure:
Synonyms:
"3′,4′,5,7-tetrahydroxyflavone"
2-(3,4-Dihydroxyphenyl)-5,7-dihydroxy-4-benzopyrone
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-1-benzopyran-4-one
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
2-(3,4-dihydroxyphenyl)-5,7-dihydroxychromen-4-one
23A002A4-B47B-46CD-848C-65042EACF3FF
3′,4′,5,7-Tetrahydroxyflavone
3',4',5,7-Tetrahydroxy-Flavone
3',4',5,7-Tetrahydroxyflavone
491-70-3
4H-1-Benzopyran-4-one, 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-
4H-1-Benzopyran-4-one, 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy- (9CI)
4H-Benzopyran-4-one, 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-
4H-Benzopyran-4-one, 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-;
5,7,3',4'-Tetrahydroxyflavone
5-18-05-00296 (Beilstein Handbook Reference)
AC-1125
AC1NQX1A
ACon1_000223
AIDS-001406
AIDS001406
AKOS002140588
BB_NC-1244
BIDD:ER0122
BIDD:PXR0059
BPBio1_001011
BRD-K05236810-001-05-9
BRN 0292084
BSPBio_000919
C.I. 75590
C.I. Natural Yellow 2
C01514
C15H10O6
CAS-491-70-3
CCRIS 3790
CHEBI:15864
CHEMBL151
Cyanidenon 1470
D047311
Digitoflavone
EINECS 207-741-0
Flacitran
FLAVONE, 3',4',5,7-TETRAHYDROXY-
HMS1570N21
HMS2097N21
HMS2220C06
I06-0436
IN1269
L 9283
L9283_SIGMA
LMPK12110006
Lopac0_000660
LS-69039
Luteolin
Luteolin, 3',4',5,7-Tetrahydroxyflavone, Luteoline, Luteolol
Luteolin-Supplied by Selleck Chemicals
Luteoline
Luteolol
MEGxp0_000143
MLS000697655
MLS000860038
MLS002154043
MolPort-000-706-683
NCGC00016467-01
NCGC00016467-02
NCGC00016467-03
NCGC00016467-04
NCGC00016467-05
NCGC00016467-06
NCGC00016467-07
NCGC00142375-01
NCGC00142375-02
NCGC00142375-03
NCGC00179375-01
NCGC00179375-02
Oprea1_849964
Prestwick0_000870
Prestwick1_000870
Prestwick2_000870
Prestwick3_000870
Prestwick_122
S00110
S2320_Selleck
Salifazide
SMP2_000042
SMR000326896
SPBio_002840
ST024703
STK801923
TNP00073
Weld Lake
Yama kariyasu
ZINC18185774

Target

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Uniprot ID:MK01_MOUSE
Synonyms:
ERK-2
ERT1
Extracellular signal-regulated kinase 2
MAP kinase 2
MAPK 2
Mitogen-activated protein kinase 1
Mitogen-activated protein kinase 2
p42-MAPK
EC-Numbers:2.7.11.24
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

12145106
Inhibition of LPS-stimulated pathways in macrophages by the flavonoid luteolin.. Angeliki Xagorari; Charis Roussos; Andreas Papapetropoulos (2002) British journal of pharmacology display abstract
1: We have previously shown that the flavonoid luteolin inhibits the expression of pro-inflammatory molecules induced by LPS. In the present study we tested the ability of luteolin to block signalling pathways implicated in LPS-induced inflammatory gene expression in macrophages. 2: Exposure of the murine macrophage cell line RAW 264.7 to LPS increased phosphorylation of the mitogen-activated protein kinase family members ERK1/2, p38 and JNK1/2 in a time-dependent manner. Pretreatment of RAW 264.7 with luteolin inhibited the LPS-induced ERK1/2 and p38, but not JNK1/2, phosphorylation, and blocked the LPS-induced TNF-alpha release. 3: To investigate which of these pathways contribute to the inhibitory effects of luteolin on TNF-alpha release, cells were pretreated with pharmacological inhibitors of these pathways; PD98059 and SB203580 when used alone failed to inhibit TNF-alpha release, whereas pretreatment with both agents attenuated TNF-alpha release. 4: We have previously shown that luteolin blocks Akt phosphorylation in response to LPS in RAW 264.7 macrophages. To determine the role of Akt in TNF-alpha release, cells were transiently transfected with a dominant negative form of Akt (K179M). Overexpression of K179M Akt did not alter LPS-induced TNF-alpha release, suggesting that inhibition of this kinase does not mediate the inhibitory action of luteolin. 5: In addition, DRB (a pharmacological inhibitor of CK2) blocked TNF-alpha release in a concentration-dependent manner, whereas co-treatment of cells with luteolin and DRB did not have an additive effect. 6: We conclude that luteolin interferes with LPS signalling by reducing the activation of several MAPK family members and that its inhibitory action on TNF-alpha release correlates with inhibition of ERK, p38 and CK2 activation.