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Drug-Target Interaction

Drug

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PubChem ID:6742
Structure:
Synonyms:
17-beta-(1-Methyl-3-carboxypropyl)-etiocholane-3-alpha,12-alpha-diol
3,12-Dihydroxycholan-24-oic acid, (3alpha,5beta,12alpha)-
3,12-Dihydroxycholanic acid
3-alpha,12-alpha-Dihydroxy-5-beta-cholan-24-oic acid
3-alpha,12-alpha-Dihydroxy-5-beta-cholanoic acid
3-alpha,12-alpha-Dihydroxycholansaeure
3-alpha,12-alpha-Dihydroxycholansaeure [German]
302-95-4
302-95-4 (mono-hydrochloride salt))
3alpha,12alpha-Dihydroxy-5beta-cholan-24-oic acid
3alpha,12alpha-Dihydroxy-5beta-cholanic acid
4-10-00-01608 (Beilstein Handbook Reference)
4-[(3R,5R,8R,9S,10S,12S,13R,14S,17R)-3,12-dihydroxy-10,13-dimethyl-2,3,4,5
5-beta-Cholan-24-oic acid, 3-alpha,12-alpha-dihydroxy-
5-beta-Deoxycholic acid
5beta-Cholan-24-oic acid, 3alpha,12alpha-dihydroxy-
5beta-Cholan-24-oic acid, 3alpha,12alpha-dihydroxy- (8CI)
71888-65-8
71888-65-8 (magnesium (2:1) salt)
728917-93-9
7alpha-Deoxycholic acid
83-44-3
AC1L1N7D
Ambotz83-44-3
BRN 3219882
C24H40O4
CCRIS 1627
Cholan-24-oic acid, 3,12-dihydroxy-, (3-alpha,5-beta,12-alpha)-
Cholan-24-oic acid, 3,12-dihydroxy-, (3-alpha,5-beta,12-alpha)- (9CI)
Cholan-24-oic acid, 3,12-dihydroxy-, (3alpha,5beta,12alpha)-
Cholan-24-oic, 3,12-dihydroxy-(3alpha,5beta,12alpha)-
Choleic acid
Cholerebic
Cholic acid, deoxy-
Cholorebic
CID6742
Degalol
Deoxy cholic acid
Deoxycholatic acid
DEOXYCHOLIC ACID
Desoxycholic acid
Desoxycholsaeure
Desoxycholsaeure [German]
Dihydroxycholanoic acid
Droxolan
EINECS 201-478-5
HSDB 293
l7-beta-(1-Methyl-3-carboxypropyl)-etiocholane-3-alpha,12-alpha-diol
LS-53035
NSC 8797
Pyrochol
Septochol
UNII-005990WHZZ

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.