Detail Information of Xenobiotics

General Information of Xenobiotics (ID: XEO00047)
Xenobiotics Name
Indomethacin
Xenobiotics Type
Pharmaceutical Agent(s)
Classification
Approved/Marketed Drug
Structure
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3D MOL 2D MOL
PubChem CID
3715
DME(s) Modulated by This Xenobiotics
DME(s) Inhibited by This Xenobiotics
Aldo-keto reductase 1C1 (AKR1C1) DME Info Homo sapiens [1]
Aldo-keto reductase 1C2 (AKR1C2) DME Info Homo sapiens [2]
Aldo-keto reductase 1C3 (AKR1C3) DME Info Homo sapiens [2]
Aldo-keto reductase 1C4 (AKR1C4) DME Info Homo sapiens [1]
Aromatase (CYP19A1) DME Info Homo sapiens [3]
L-glutamine amidohydrolase (GLS) DME Info Homo sapiens [4]
Glutamine synthetase (GLUL) DME Info Homo sapiens [5]
Corticosteroid 11-beta-dehydrogenase 2 (HSD11B2) DME Info Homo sapiens [6]
Prostaglandin reductase 1 (PTGR1) DME Info Homo sapiens [7]
Prostaglandin G/H synthase 1 (COX-1) DME Info Homo sapiens [8]
Prostaglandin G/H synthase 2 (COX-2) DME Info Homo sapiens [9]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME Info Homo sapiens [10]
DME(s) Induced by This Xenobiotics
Asparagine synthetase (ASNS) DME Info Homo sapiens [5]
Carbonic anhydrase II (CA2) DME Info Homo sapiens [11]
Serine sulfhydrase (CBS) DME Info Homo sapiens [5]
Methylsterol monooxygenase 1 (MSMO1) DME Info Homo sapiens [5]
Ecto-5'-nucleotidase (NT5E) DME Info Homo sapiens [12]
Putrescine acetyltransferase (SSAT1) DME Info Homo sapiens [13]
Uridine phosphorylase 1 (UPP1) DME Info Homo sapiens [4]
Xanthine dehydrogenase/oxidase (XDH) DME Info Homo sapiens [14]
Xenobiotics-DME Activity Data
Xenobiotics-DME Activity Data Aldo-keto reductase 1C1 (AKR1C1) DME Info IC50 = 130 microM [1]
Aldo-keto reductase 1C2 (AKR1C2) DME Info IC50 = 36.53 microM [2]
Aldo-keto reductase 1C3 (AKR1C3) DME Info IC50 = 0.1 microM [2]
Aldo-keto reductase 1C4 (AKR1C4) DME Info IC50 = 54 microM [1]
Prostaglandin G/H synthase 1 (COX-1) DME Info IC50 = 0.002 microM [8]
Prostaglandin G/H synthase 2 (COX-2) DME Info IC50 < 0.2 microM [9]
References
1 Selective inhibition of human type-5 17beta-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis. J Nat Prod. 2012 Apr 27;75(4):716-21.
2 Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. J Med Chem. 2013 Mar 28;56(6):2429-46.
3 Translational studies on aromatase, cyclooxygenases, and enzyme inhibitors in breast cancer. J Steroid Biochem Mol Biol. 2005 May;95(1-5):129-36.
4 Mechanisms of indomethacin-induced alterations in the choline phospholipid metabolism of breast cancer cells. Neoplasia. 2006 Sep;8(9):758-71.
5 Anti-inflammatory agent indomethacin reduces invasion and alters metabolism in a human breast cancer cell line. Neoplasia. 2007 Mar;9(3):222-35.
6 Prostaglandins and leukotriene B4 are potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 2 activity in human choriocarcinoma JEG-3 cells. Biol Reprod. 1999 Jul;61(1):40-5.
7 Human prostaglandin reductase 1 (PGR1): Substrate specificity, inhibitor analysis and site-directed mutagenesis. Chem Biol Interact. 2015 Jun 5;234:105-13.
8 Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. J Med Chem. 2003 Jul 31;46(16):3463-75.
9 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors. Bioorg Med Chem Lett. 1999 Jun 21;9(12):1715-20.
10 In vitro inhibitory effects of non-steroidal antiinflammatory drugs on UDP-glucuronosyltransferase 1A1-catalysed estradiol 3beta-glucuronidation in human liver microsomes. Biopharm Drug Dispos. 2005 Jan;26(1):35-9.
11 Indomethacin activates carbonic anhydrase and antagonizes the effect of the specific carbonic anhydrase inhibitor acetazolamide, by a direct mechanism of action. Int J Clin Pharmacol Ther. 2001 Jun;39(6):265-70.
12 Indomethacin stimulates activity and expression of ecto-5'-nucleotidase/CD73 in glioma cell lines. Eur J Pharmacol. 2007 Aug 13;569(1-2):8-15.
13 Induction of spermidine/spermine N1-acetyltransferase (SSAT) by aspirin in Caco-2 colon cancer cells. Biochem J. 2006 Feb 15;394(Pt 1):317-24.
14 Activation of phospholipase A2 is involved in indomethacin-induced damage in Caco-2 cells. Toxicol In Vitro. 2009 Aug;23(5):887-96.

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