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Drug-Target Interaction

Drug

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PubChem ID:1548887
Structure:
Synonyms:
(Z)-5-Fluoro-2-methyl-1-((p-(methylsulfinyl)phenyl)methylene)-1H-indene-3-
(Z)-5-Fluoro-2-methyl-1-((p-(methylsulfinyl)phenyl)methylene)-1H-indene-3-acetic acid
1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-((4-(methylsulfinyl)phenyl)methylene)-, (Z)-
32004-68-5
38194-50-2
5-Fluoro-2-methyl-1-((4-(methylsulphinyl)phenyl)methylene)-1H-indene-3-acetic acid
9000-14-0
AB00513800
Aclin
Alphapharm Brand of Sulindac
Apo Sulin
Apo-Sulin
Apotex Brand of Sulindac
Arthrobid
Arthrocine
BPBio1_000315
BRN 2951842
BSPBio_000285
BSPBio_002890
C01531
C20H17FO3S
Cahill May Roberts Brand of Sulindac
CAS-38194-50-2
CCRIS 3305
CHEBI:9352
Chemia Brand of Sulindac
Chibret
cis-5-Fluoro-2-methyl-1-((4-(methylsulfinyl)phenyl)methylene)-1H-indene-3-acetic acid
cis-5-Fluoro-2-methyl-1-((p-methylsulfinyl)benzylidene)indene-3-acetic acid
Clinoril
Clinoril (TN)
cMAP_000021
Copal
Copal resin
Copal rosin varnish
Copals
D00120
D013467
EINECS 232-527-9
EINECS 250-893-8
EINECS 253-819-2
EU-0101070
Gum copal
IDI1_000601
Kenalin
Kendrick Brand of Sulindac
Klinoril
Lopac-S-8139
Lopac0_001070
LS-81610
Merck Brand of Sulindac
Merck Sharp & Dohme Brand of Sulindac
MK 231
MK-231
MK231
MLS001056554
Mobilin
NCGC00015970-01
NCGC00015970-02
NCGC00025268-01
NCGC00025268-02
NCGC00025268-03
NCGC00094349-01
NCGC00094349-02
Novo Sundac
Novo-Sundac
Novopharm Brand of Sulindac
Nu Pharm Brand of Sulindac
Nu Sulindac
Nu-Pharm Brand of Sulindac
Nu-Sulindac
Prestwick3_000073
Resin copal
SMR000326718
SPECTRUM1500556
Spectrum5_001024
Sulindac
Sulindac (JAN/USP/INN)
Sulindac sulfoxide
Sulindac [USAN:BAN:INN:JAN]
Sulindaco
Sulindaco [INN-Spanish]
Sulindacum
Sulindacum [INN-Latin]
Sulindal
Tocris-1707
{(1Z)-5-fluoro-2-methyl-1-[4-(methylsulfinyl)benzylidene]-1H-inden-3-yl}acetic acid
ATC-Codes:

Target

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Uniprot ID:PGES2_HUMAN
Synonyms:
Microsomal prostaglandin E synthase 2
mPGES-2
Prostaglandin E synthase 2
EC-Numbers:5.3.99.3
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.