Detail Information of Xenobiotics

General Information of Xenobiotics (ID: XEO00241)
Xenobiotics Name
Cyclosporine
Xenobiotics Type
Pharmaceutical Agent(s)
Classification
Approved/Marketed Drug
Structure
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3D MOL 2D MOL
PubChem CID
2909
DME(s) Modulated by This Xenobiotics
DME(s) Inhibited by This Xenobiotics
Tartrate-resistant acid ATPase (ACP5) DME Info Homo sapiens [1]
Acid phosphatase-like protein 1 (ACP6) DME Info Homo sapiens [2]
Alcohol dehydrogenase class-I beta (ADH1B) DME Info Homo sapiens [3]
Alcohol dehydrogenase class-I gamma (ADH1C) DME Info Homo sapiens [3]
Alcohol dehydrogenase class-II (ADH4) DME Info Homo sapiens [1]
Alcohol dehydrogenase class-III (ADH5) DME Info Homo sapiens [2]
Alcohol dehydrogenase class-V (ADH6) DME Info Homo sapiens [1]
Aldo-keto reductase 1C3 (AKR1C3) DME Info Homo sapiens [2]
Aldo-keto reductase 1C4 (AKR1C4) DME Info Homo sapiens [3]
Aldo-keto reductase 1D1 (AKR1D1) DME Info Homo sapiens [1]
Succinic semialdehyde reductase (AKR7A2) DME Info Homo sapiens [3], [2]
Porphobilinogen synthase (ALAD) DME Info Homo sapiens [2]
Aldehyde dehydrogenase 1 (ALDH1) DME Info Homo sapiens [1]
Aldehyde dehydrogenase 5 (ALDHX) DME Info Homo sapiens [1]
Succinate-semialdehyde dehydrogenase (ALDH5A1) DME Info Homo sapiens [1]
Aminomuconic semialdehyde dehydrogenase (ALDH12) DME Info Homo sapiens [1]
Alanyl aminopeptidase (ANPEP) DME Info Homo sapiens [1]
Amiloride-sensitive amine oxidase (AOC1) DME Info Homo sapiens [3]
Copper amine oxidase (AOC3) DME Info Homo sapiens [2]
Aldehyde oxidase (AOX1) DME Info Homo sapiens [4], [3]
Arsenite methyltransferase (AS3MT) DME Info Homo sapiens [3], [2]
Bile acid-CoA thioesterase (BAAT) DME Info Homo sapiens [2]
Butyrylcholine esterase (BCHE) DME Info Homo sapiens [3], [1]
Carbonic anhydrase II (CA2) DME Info Homo sapiens [3]
Catalase (CAT) DME Info Homo sapiens [1]
NADPH-dependent carbonyl reductase 1 (CBR1) DME Info Homo sapiens [3], [2]
Carboxylesterase 2 (CES2) DME Info Homo sapiens [3], [2]
Choline dehydrogenase (CHDH) DME Info Homo sapiens [2]
Cathepsin A (CTSA) DME Info Homo sapiens [2]
Microsomal cytochrome MCB5 (CYB5A) DME Info Homo sapiens [3], [2]
Steroid 17-alpha-monooxygenase (CYP17A1) DME Info Homo sapiens [2]
Aromatase (CYP19A1) DME Info Homo sapiens [2]
Cytochrome P450 1A1 (CYP1A1) DME Info Homo sapiens [3], [5]
Cytochrome P450 1B1 (CYP1B1) DME Info Homo sapiens [5]
Steroid 21-hydroxylase (CYP21A2) DME Info Homo sapiens [1]
Vitamin D(3) 25-hydroxylase (CYP27A1) DME Info Homo sapiens [6], [7]
Cytochrome P450 2A6 (CYP2A6) DME Info Homo sapiens [3]
Cytochrome P450 2B6 (CYP2B6) DME Info Homo sapiens [3]
Cytochrome P450 2C18 (CYP2C18) DME Info Homo sapiens [3]
Mephenytoin 4-hydroxylase (CYP2C19) DME Info Homo sapiens [8]
Cytochrome P450 2C8 (CYP2C8) DME Info Homo sapiens [3]
Cytochrome P450 2C9 (CYP2C9) DME Info Homo sapiens [8]
Cytochrome P450 2E1 (CYP2E1) DME Info Homo sapiens [1]
Cytochrome P450 2J2 (CYP2J2) DME Info Homo sapiens [3], [2]
Cytochrome P450 3A4 (CYP3A4) DME Info Homo sapiens [9]
Cytochrome P450 3A43 (CYP3A43) DME Info Homo sapiens [3]
Cytochrome P450 3A5 (CYP3A5) DME Info Homo sapiens [3], [2]
Cytochrome P450 3A7 (CYP3A7) DME Info Homo sapiens [1]
Cholesterol 24-hydroxylase (CYP46A1) DME Info Homo sapiens [3]
Cytochrome P450 4B1 (CYP4B1) DME Info Homo sapiens [3]
Cytochrome P450 4F12 (CYP4F12) DME Info Homo sapiens [3], [2]
Cytochrome P450 4F2 (CYP4F2) DME Info Homo sapiens [1]
Dicarbonyl/L-xylulose reductase (DCXR) DME Info Homo sapiens [3], [2]
DOPA decarboxylase (DDC) DME Info Homo sapiens [2]
Delta(24)-sterol reductase (DHCR24) DME Info Homo sapiens [3], [2]
Short-chain dehydrogenase/reductase retSDR1 (DHRS3) DME Info Homo sapiens [3]
Dehydropeptidase-I (DPEP1) DME Info Homo sapiens [3]
Dipeptidyl peptidase IV (DPP4) DME Info Homo sapiens [1]
Dihydrothymine dehydrogenase (DPYD) DME Info Homo sapiens [4], [3]
Thymidylate kinase (DTYMK) DME Info Homo sapiens [3], [2]
Bifunctional epoxide hydrolase 2 (EPHX2) DME Info Homo sapiens [2]
Dimethylaniline oxidase 1 (FMO1) DME Info Homo sapiens [1]
Dimethylaniline oxidase 2 (FMO2) DME Info Homo sapiens [3]
Dimethylaniline oxidase 3 (FMO3) DME Info Homo sapiens [3], [1]
Sodium/potassium-transporting ATPase gamma (FXYD2) DME Info Homo sapiens [10]
Galactose kinase (GALK1) DME Info Homo sapiens [3], [2]
Glutamyl-tRNA(Gln) amidotransferase B (GATB) DME Info Homo sapiens [2]
Gamma-Glu-X carboxypeptidase (GGH) DME Info Homo sapiens [3], [2]
L-glutamine amidohydrolase (GLS) DME Info Homo sapiens [1]
Glutamine synthetase (GLUL) DME Info Homo sapiens [2]
Glutathione S-transferase alpha-1 (GSTA1) DME Info Homo sapiens [2]
Glutathione S-transferase omega-1 (GSTO1) DME Info Homo sapiens [3]
Glutathione S-transferase theta-1 (GSTT1) DME Info Homo sapiens [2]
HMG-CoA reductase (HMGCR) DME Info Homo sapiens [2]
Histamine N-methyltransferase (HNMT) DME Info Homo sapiens [1]
Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1) DME Info Homo sapiens [3]
Corticosteroid 11-beta-dehydrogenase 2 (HSD11B2) DME Info Homo sapiens [2]
Ketoacyl-CoA reductase (HSD17B12) DME Info Homo sapiens [2]
Estradiol 17-beta-dehydrogenase 2 (HSD17B2) DME Info Homo sapiens [1]
Testicular 17-beta-hydroxysteroid dehydrogenase (HSD17B3) DME Info Homo sapiens [3]
Peroxisomal multifunctional enzyme 2 (HSD17B4) DME Info Homo sapiens [4], [3]
Alpha-L-iduronidase (IDUA) DME Info Homo sapiens [3]
Kynurenine aminotransferase I (KYAT1) DME Info Homo sapiens [3]
Monoamine oxidase type A (MAO-A) DME Info Homo sapiens [3]
Monoamine oxidase type B (MAO-B) DME Info Homo sapiens [1]
S-adenosylmethionine synthase 1 (MAT1A) DME Info Homo sapiens [3], [2]
S-adenosylmethionine synthase 2 (MAT2A) DME Info Homo sapiens [2]
Microsomal glutathione S-transferase 2 (MGST2) DME Info Homo sapiens [3], [2]
Neprilysin (MME) DME Info Homo sapiens [3]
Methylsterol monooxygenase 1 (MSMO1) DME Info Homo sapiens [3], [2]
Methionine-R-sulfoxide reductase B1 (MSRB1) DME Info Homo sapiens [3]
Methionine-R-sulfoxide reductase B2 (MSRB2) DME Info Homo sapiens [3]
Vitamin B12 methionine synthase (MTR) DME Info Homo sapiens [2]
Methionine synthase reductase (MTRR) DME Info Homo sapiens [2]
Mevalonate pyrophosphate decarboxylase (MPD) DME Info Homo sapiens [3], [11]
Methylarsonite methyltransferase N6AMT1 (N6AMT1) DME Info Homo sapiens [12]
Glutamine-dependent NAD(+) synthetase (NADSYN1) DME Info Homo sapiens [2]
Alpha-N-acetylglucosaminidase (NAG) DME Info Homo sapiens [2]
N-acetyltransferase 1 (NAT1) DME Info Homo sapiens [4], [3]
N-acetyltransferase 2 (NAT2) DME Info Homo sapiens [3], [1]
Cysteinyl-conjugate N-acetyltransferase (NAT8) DME Info Homo sapiens [1]
NADH-ubiquinone oxidoreductase 49 kDa (NDUFS2) DME Info Homo sapiens [3]
NADH-ubiquinone oxidoreductase 30 kDa (NDUFS3) DME Info Homo sapiens [3], [1]
NADH-ubiquinone oxidoreductase 20 kDa (NDUFS7) DME Info Homo sapiens [3]
Quinone reductase 1 (NQO1) DME Info Homo sapiens [1], [12]
Propionyl-CoA carboxylase beta (PCCB) DME Info Homo sapiens [3]
Phosphorylethanolamine transferase (PCYT2) DME Info Homo sapiens [3], [2]
Phosphodiesterase 5A (PDE5A) DME Info Homo sapiens [1]
Phosphoribosylformylglycinamidine synthase (PFAS) DME Info Homo sapiens [2]
Phosphoglucomutase 1 (PGM1) DME Info Homo sapiens [2]
Cytosolic phospholipase A2 (PLA2G4A) DME Info Homo sapiens [3]
Choline phosphatase 1 (PLD1) DME Info Homo sapiens [3], [2]
Pyridoxamine-phosphate oxidase (PNPO) DME Info Homo sapiens [3], [2]
Serum paraoxonase/arylesterase 1 (PON1) DME Info Homo sapiens [3], [1]
Serum paraoxonase/lactonase 3 (PON3) DME Info Homo sapiens [3], [2]
NADPH-cytochrome P450 reductase (CPR) DME Info Homo sapiens [3]
Proline dehydrogenase 1 (PRODH) DME Info Homo sapiens [3]
Xylosyl phosphatase (PXYLP1) DME Info Homo sapiens [3], [11]
Putrescine acetyltransferase (SSAT1) DME Info Homo sapiens [3], [5]
Selenocysteine lyase (SCLY) DME Info Homo sapiens [2]
Superoxide dismutase 1 (SOD1) DME Info Homo sapiens [2]
Steroid 5-alpha-reductase 2 (SRD5A2) DME Info Homo sapiens [3]
Steroid 5-alpha-reductase 3 (SRD5A3) DME Info Homo sapiens [5]
Sulfotransferase 1A1 (SULT1A1) DME Info Homo sapiens [3], [2]
Sulfotransferase 1A2 (SULT1A2) DME Info Homo sapiens [3], [2]
Sulfotransferase 1B1 (SULT1B1) DME Info Homo sapiens [1]
Sulfotransferase 2A1 (SULT2A1) DME Info Homo sapiens [7]
Tryptophan oxygenase (TRPO) DME Info Homo sapiens [1]
Transglutaminase K (TGM1) DME Info Homo sapiens [1]
Transglutaminase H (TGM2) DME Info Homo sapiens [1]
Thiopurine methyltransferase (TPMT) DME Info Homo sapiens [4], [3]
Thymidylate synthase (TYMS) DME Info Homo sapiens [2]
UDP-glucuronosyltransferase 1A6 (UGT1A6) DME Info Homo sapiens [3], [1]
UDP-glucuronosyltransferase 2A3 (UGT2A3) DME Info Homo sapiens [1]
UDP-glucuronosyltransferase 2B15 (UGT2B15) DME Info Homo sapiens [1]
UDP-glucuronosyltransferase 2B17 (UGT2B17) DME Info Homo sapiens [1]
UDP-glucuronosyltransferase 2B4 (UGT2B4) DME Info Homo sapiens [1], [2]
Uridine 5'-monophosphate synthase (UMPS) DME Info Homo sapiens [2]
Uracil phosphoribosyltransferase (UPRT) DME Info Homo sapiens [2]
Vitamin K1 2,3-epoxide reductase 1 (VKOR) DME Info Homo sapiens [3]
DME(s) Induced by This Xenobiotics
Acetylcholinesterase (ACHE) DME Info Homo sapiens [3]
Acetyl-CoA synthetase (ACSS2) DME Info Homo sapiens [1]
Adenosine aminohydrolase (ADA) DME Info Homo sapiens [2]
Alcohol dehydrogenase class-I alpha (ADH1A) DME Info Homo sapiens [9]
Hydroxyacid-oxoacid transhydrogenase (ADHFE1) DME Info Homo sapiens [1]
Aldo-keto reductase 1B1 (AKR1B1) DME Info Homo sapiens [3]
Small intestine reductase (AKR1B10) DME Info Homo sapiens [2]
Aldo-keto reductase 1C1 (AKR1C1) DME Info Homo sapiens [2]
Aldo-keto reductase 1C2 (AKR1C2) DME Info Homo sapiens [5]
Aldehyde dehydrogenase 2 (ALDH2) DME Info Homo sapiens [13], [1]
Alkaline phosphatase (ALPL) DME Info Homo sapiens [14]
Aquaporin adipose (AQP7) DME Info Homo sapiens [2]
Asparagine synthetase (ASNS) DME Info Homo sapiens [9]
Cytosolic branched aminotransferase (BCAT1) DME Info Homo sapiens [1]
NADPH-dependent carbonyl reductase 3 (CBR3) DME Info Homo sapiens [3], [1]
Serine sulfhydrase (CBS) DME Info Homo sapiens [1]
Cytidine aminohydrolase (CDA) DME Info Homo sapiens [2]
Carboxylesterase 1 (CES1) DME Info Homo sapiens [13]
Vitamin D(3) 24-hydroxylase (CYP24A1) DME Info Homo sapiens [2]
Calcidiol 1-monooxygenase (CYP27B1) DME Info Homo sapiens [3]
Vitamin D 25-hydroxylase (CYP2R1) DME Info Homo sapiens [3], [1]
Cytochrome P450 2S1 (CYP2S1) DME Info Homo sapiens [2]
Deoxycytidylate deaminase (DCTD) DME Info Homo sapiens [3]
Friedreich ataxia protein (FXN) DME Info Homo sapiens [1]
Gamma-glutamyltranspeptidase 5 (GGT5) DME Info Homo sapiens [2]
Glutathione reductase (GSR) DME Info Homo sapiens [2]
N-acetyl-beta-glucosaminidase beta (HEXB) DME Info Homo sapiens [2]
Hypoxanthine phosphoribosyltransferase (HPRT1) DME Info Homo sapiens [1]
Iduronate 2-sulfatase (IDS) DME Info Homo sapiens [2]
Metallothionein-2A (MT2A) DME Info Homo sapiens [5]
Nitric oxide synthase inducible (NOS2) DME Info Homo sapiens [15]
Nitric oxide synthase endothelial (NOS3) DME Info Homo sapiens [16], [2]
Deoxy-5'-nucleotidase 1 (NT5C) DME Info Homo sapiens [1]
Ecto-5'-nucleotidase (NT5E) DME Info Homo sapiens [11]
Phosphorylcholine transferase A (PCYT1A) DME Info Homo sapiens [3], [1]
Purine nucleoside phosphorylase (PNP) DME Info Homo sapiens [2]
Prostaglandin reductase 1 (PTGR1) DME Info Homo sapiens [2]
Thioredoxin reductase TR1 (TXNRD1) DME Info Homo sapiens [3], [5]
Thymidine phosphorylase (TYMP) DME Info Homo sapiens [3]
Uridine phosphorylase 1 (UPP1) DME Info Homo sapiens [1]
Tryptophanyl-tRNA synthetase mitochondrial (WARS2) DME Info Homo sapiens [2]
Xanthine dehydrogenase/oxidase (XDH) DME Info Homo sapiens [1]
Xenobiotics-DME Activity Data
Xenobiotics-DME Activity Data Mephenytoin 4-hydroxylase (CYP2C19) DME Info IC50 = 7 microM [8]
Cytochrome P450 2C9 (CYP2C9) DME Info IC50 = 38.8 microM [8]
Cytochrome P450 3A4 (CYP3A4) DME Info IC50 > 10 microM [9]
References
1 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
2 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
3 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
4 Cyclosporine A treated in vitro models induce cholestasis response through comparison of phenotype-directed gene expression analysis of in vivo Cyclosporine A-induced cholestasis. Toxicol Lett. 2013 Aug 29;221(3):225-36.
5 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
6 Compared effect of immunosuppressive drugs cyclosporine A and rapamycin on cholesterol homeostasis key enzymes CYP27A1 and HMG-CoA reductase. Basic Clin Pharmacol Toxicol. 2007 Jun;100(6):392-7.
7 Cellular accumulation and toxic effects of bile acids in cyclosporine A-treated HepaRG hepatocytes. Toxicol Sci. 2015 Oct;147(2):573-87.
8 SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro. Antimicrob Agents Chemother. 2010 Feb;54(2):660-72.
9 Comparison of base-line and chemical-induced transcriptomic responses in HepaRG and RPTEC/TERT1 cells using TempO-Seq. Arch Toxicol. 2018 Aug;92(8):2517-2531.
10 Evidence for a role of claudin 2 as a proximal tubular stress responsive paracellular water channel. Toxicol Appl Pharmacol. 2014 Sep 1;279(2):163-72.
11 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
12 Cyclosporine A--induced oxidative stress in human renal mesangial cells: a role for ERK 1/2 MAPK signaling. Toxicol Sci. 2012 Mar;126(1):101-13.
13 Proteomics investigations of drug-induced hepatotoxicity in HepG2 cells. Toxicol Sci. 2011 Mar;120(1):109-22.
14 Bone-alkaline phosphatase as indicator of bone formation. Clin Chim Acta. 1991 Sep 14;201(1-2):27-33.
15 Nitric oxide mediates cyclosporine-induced apoptosis in cultured renal cells. Kidney Int. 2000 Apr;57(4):1549-59.
16 Oxidative stress in kidney transplant patients with calcineurin inhibitor-induced hypertension: effect of ramipril. J Cardiovasc Pharmacol. 2002 Oct;40(4):625-31.

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