Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:2061
Structure:
Synonyms:
((3,4,5-Trihydroxyphenyl)methylene)propanedinitrile
(3,4,5-Trihydroxybenzylidene)-malononitrile
(3,4,5-Trihydroxybenzylidene)malononitrile
(4,5-Trihydroxybenzylidene)malononitrile
118409-58-8
158129-55-6
1608-93-1
2-(3,4,5-Trihydroxybenzylidene)malononitrile
2-[(3,4,5-trihydroxyphenyl)methylidene]propanedinitrile
AC1L1CTU
AC1Q4PY5
AG 82
AIDS-080804
AIDS080804
alpha-Cyano-(3,4,5-trihydroxy)cinnamonitrile
AR-1A3814
benzylidenemalononitrile (BMN) deriv. 25
BiomolKI2_000022
BiomolKI_000012
BMK1-B12
BRD-K03670461-001-03-8
C10H6N2O3
CCG-100616
CHEMBL310798
EC-000.2087
EU-0101190
HSCI1_000114
IN1437
KST-1A1833
Lopac-T-7290
Lopac0_001190
LS-172379
NCGC00016046-01
NCGC00016046-02
NCGC00016046-03
NCGC00016046-04
NCGC00016046-05
NCGC00094443-01
NCGC00094443-02
NCGC00094443-03
NSC 676484
NSC676484
Propanedinitrile, ((3,4,5-trihydroxyphenyl)methylene)-
RG-50875
T 7290
Tyrphostin 25
Tyrphostin A 25
Tyrphostin A25
Tyrphostin-25
ZINC00057523

Target

show target details
Uniprot ID:Q9Y354_HUMAN
Synonyms:
Matrix metalloproteinase 9
EC-Numbers:3.4.24.35
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

16720051
Protein tyrosine kinase and p38 MAP kinase pathways are involved in stimulation of matrix metalloproteinase-9 by TNF-alpha in human monocytes.. Juliette Nguyen; Jean Gogusev; Perrine Knapnougel; Brigitte Bauvois (2006) Immunology letters display abstract
Matrix metalloproteinase-9 (MMP-9), through its catalytic and non-catalytic activities, plays critical roles in inflammation, tumor invasion and angiogenesis. Human monocytes actively involved in inflammatory and tumoral states secrete proMMP-9 (92kDa). Endogenous TNF-alpha stimulates MMP-9 gene transcription in monocytes through NF-kappaB activation. In this study, we investigated the intracellular signaling pathways underlying TNF-alpha/NF-kappaB-dependent expression of MMP-9 in monocytes using chemical inhibitors that specifically inhibit distinct kinase pathways. We confirmed the expression of MMP-9 by reverse transcription chain reaction (RT-PCR), ELISA and gelatin zymography. PGE2/cAMP inhibitor indomethacin, PI-3K inhibitor wortmannin, PKC inhibitor bisindolylmaleimide and PKA inhibitor H-89 did not affect the levels of released MMP-9. In contrast, MMP-9 mRNA and protein expression was down-regulated by p38 MAPK inhibitor SB203580 and protein tyrosine kinase (PTK) inhibitor tyrphostin 25. These inhibitors increased IkappaB-alpha levels, which correlate with decreased NF-kappaB activation. Although SB203580 induced a decrease in TNF-alpha release, addition of exogenous TNF-alpha did not reverse the inhibitory effect of SB203580 toward MMP-9 thus suggesting that SB203580 could modulate down-stream effects of TNF-alpha. In parallel, TIMP-1 levels decreased in the presence of SB203580. Both kinase inhibitors did not influence the maturation pathway of monocytes. Our results indicate that these two inhibitors of p38 MAPK and PTK pathways could be used as combined targets for inhibiting MMP-9 expression in inflamed tissues.