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

Drug-Target Interaction

Drug

show drug details
PubChem ID:5352624
Structure:
Synonyms:
(Z)-5-Fluoro-2-methyl-1-((4-(methylthio)phenyl)methylene)-1H-indene-3-acet
(Z)-5-Fluoro-2-methyl-1-((4-(methylthio)phenyl)methylene)-1H-indene-3-acetic acid
(Z)-5-Fluoro-2-methyl-1-[p-(methylthio)benzylidene]indene-3-acetic acid
(Z)-Sulindac sulfide
1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-((4-(methylthio)phenyl)methylene)-, (Z)-
49627-27-2
5-fluoro-2-methyl-1-(4-methylthiobenzylidene)inden-3-ylacetic acid
AC-20512
AC1NS2PY
CHEBI:121650
CHEMBL18797
EINECS 256-403-9
NCGC00161601-01
S3131_SIGMA
Sulindac sulfide
UNM-0000306137
UPCMLD-DP020
UPCMLD-DP020:001

Target

show target details
Uniprot ID:Q6LCE7_HUMAN
Synonyms:
Cyclooxygenase-1
EC-Numbers:1.14.99.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

11029586
Coordinate up- and down-regulation of glutathione-dependent prostaglandin E synthase and cyclooxygenase-2 in A549 cells. Inhibition by NS-398 and leukotriene C4.. S Thorén; P J Jakobsson (2000) European journal of biochemistry / FEBS display abstract
Recently, a microsomal protein with 38% sequence identity to microsomal glutathione S-transferase 1 was shown to constitute an inducible, glutathione-dependent prostaglandin E synthase (PGES). To investigate the relationship between cyclooxygenase and PGES, a time-course study on protein expression was performed in A549 cells after treatment with interleukin-1beta. The result demonstrated a tandem expression of cyclooxygenase-2 and PGES. The observed induction of PGES protein correlated with microsomal PGES activity. No comparable PGES activity was observed in the absence of glutathione or in the cytosolic fraction. In addition, tumour necrosis factor-alpha was found to induce PGES in these cells. Dexamethasone was found to completely suppress the effect of both cytokines on PGES induction. We also describe a quantitative method, based on RP-HPLC with UV detection for the measurements of PGES activity. This method was used to screen potential PGES inhibitors. Several nonsteroidal anti-inflammatory drugs, stable prostaglandin H2 analogues and cysteinyl leukotrienes were screened for inhibition of PGES activity. NS-398, sulindac sulfide and leukotriene C4 were all found to inhibit PGES activity with IC50 values of 20 microM, 80 microM and 5 microM, respectively. In conclusion, it appears that PGES and cyclooxygenase-2 are functionally coupled in A549 cells and that a required coordinate expression of these enzymes allows for efficient biosynthesis of prostaglandin E2.