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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:Q9UE37_HUMAN
Synonyms:
Glutathione transferase
EC-Numbers:2.5.1.18
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

15300575
Glutathione-S-transferase P1-1 protects aberrant crypt foci from apoptosis induced by deoxycholic acid.. Atsushi Nobuoka; Tetsuji Takayama; Koji Miyanishi; Tsutomu Sato; Kunihiro Takanashi; Tsuyoshi Hayashi; Takehiro Kukitsu; Yasushi Sato; Minoru Takahashi; Tetsuro Okamoto; Takuya Matsunaga; Junji Kato; Masayuki Oda; Takachika Azuma; Yoshiro Niitsu (2004) Gastroenterology display abstract
BACKGROUND & AIMS: Aberrant crypt foci, precursors of colonic adenoma, are frequently positive for glutathione-S-transferase P1-1. Because deoxycholic acid is an apoptosis-inducing xenobiotic in the colon, we examined the possibility that aberrant crypt foci, through the cytoprotecting function of glutathione-S-transferase P1-1, resist deoxycholic acid-induced apoptosis, thereby surviving to become adenomas and subsequently cancer. METHODS: Glutathione-S-transferase P1-1 or cyclooxygenase-2 expression and the percentage of apoptotic cells in aberrant crypt foci were examined by immunohistochemistry and by terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick-end labeling, respectively. Glutathione-S-transferase P1-1 was transfected into colon cancer cells (M7609) and human lung fibroblasts, and deoxycholic acid-induced apoptosis was evaluated by a dye-uptake assay and flow cytometry. Binding of deoxycholic acid to glutathione-S-transferase P1-1 was analyzed by circular dichroism and immunoprecipitation. Caspase activities were determined by colorimetric protease assay, and sulindac binding to glutathione-S-transferase P1-1 was determined by inhibition assay of glutathione-S-transferase P1-1 activity. RESULTS: Aberrant crypt foci showed positive immunostaining for glutathione-S-transferase P1-1 but negative staining for cyclooxygenase-2. The percentage of apoptotic cells in aberrant crypt foci was significantly lower than in healthy epithelium, and the difference became more apparent with deoxycholic acid treatment. The impaired sensitivity of aberrant crypt foci to deoxycholic acid was restored by the glutathione-S-transferase P1-1-specific inhibitor gamma-glutamyl-S-(benzyl)cysteinyl-R-phenylglycine diethylester. By transfection of glutathione-S-transferase P1-1, M7609 cells became more resistant to deoxycholic acid-induced apoptosis than mock transfectants. Direct binding of glutathione-S-transferase P1-1 to deoxycholic acid was proven by circular dichroism and by immunoprecipitation. The aberrant crypt foci in adenoma patients treated with sulindac, which was shown to bind to glutathione-S-transferase P1-1, underwent apoptosis in 4 days and mostly regressed in 2-3 months. CONCLUSIONS: Glutathione-S-transferase P1-1 protects aberrant crypt foci from deoxycholic acid-induced apoptosis and may play a pivotal role in early colon carcinogenesis.